File No: NA/944

                                                                   November 2001



                  NATIONAL INDUSTRIAL CHEMICALS NOTIFICATION
                            AND ASSESSMENT SCHEME

                                     FULL PUBLIC REPORT


      1,6-dichloro-1,6-dideoxy--D-fructofuranosyl-4-chloro-4-deoxy--D-galactose




This Assessment has been compiled in accordance with the provisions of the Industrial Chemicals
(Notification and Assessment) Act 1989 (the Act) and Regulations. This legislation is an Act of the
Commonwealth of Australia. The National Industrial Chemicals Notification and Assessment
Scheme (NICNAS) is administered by the National Occupational Health and Safety Commission
which also conducts the occupational health & safety assessment. The assessment of environmental
hazard is conducted by the Department of the Environment and the assessment of public health is
conducted by the Department of Health and Aged Care.
For the purposes of subsection 78(1) of the Act, copies of this full public report may be inspected by
the public at the Library, National Occupational Health and Safety Commission, Plaza level, Alan
Woods Building, 25 Constitution Avenue, Canberra ACT 2600 between 9 AM and 5 PM Monday to
Friday.
Copies of this full public report may also be requested, free of charge, by contacting the
Administration Coordinator on the fax number below.

For enquiries please contact the Administration Section at:

Street Address: 92 -94 Parramatta Rd CAMPERDOWN NSW 2050, AUSTRALIA
Postal Address: GPO Box 58, SYDNEY NSW 2001, AUSTRALIA
Telephone:      (61) (02) 9577 9514 FAX (61) (02) 9577 9465


Director
Chemicals Notification and Assessment

                                                 TABLE OF CONTENTS

SPLENDA/SUCRALOSE........................................................ Error! Bookmark not defined.
FULL PUBLIC REPORT...........................................................................................................3
SPLENDA/SUCRALOSE..........................................................................................................3
  1. APPLICANT ..................................................................................................................3
  2. IDENTITY OF THE CHEMICAL .................................................................................3
  3. PHYSICAL AND CHEMICAL PROPERTIES.............................................................4
    3.1      Comments on Physico-Chemical Properties ..........................................................4
  4. PURITY OF THE CHEMICAL .....................................................................................5
  5. USE, VOLUME AND FORMULATION ......................................................................6
  6. OCCUPATIONAL EXPOSURE ...................................................................................7
  7. PUBLIC EXPOSURE ....................................................................................................7
  8. ENVIRONMENTAL EXPOSURE ................................................................................7
    8.1      Release ...................................................................................................................8
    8.2      Fate .........................................................................................................................8
  9. EVALUATION OF TOXICOLOGICAL DATA...........................................................9
    9.1. Pharmacokinetics and Metabolism.........................................................................9
    9.2      Acute toxicity .........................................................................................................9
    9.3      Genotoxicity ...........................................................................................................9
    9.4      Repeated dose toxicity..........................................................................................12
       9.4.1       Bodyweight gain/food consumption.............................................................12
       9.4.2       Chronic toxicity/carcinogenicity studies ......................................................13
       9.4.3       Immunotoxicity ............................................................................................14
       9.4.4       Neurotoxicity................................................................................................14
    9.5      Reproductive/Developmental Toxicity ................................................................14
    9.6      Studies in humans ................................................................................................16
       9.6.1       Diabetic studies ............................................................................................16
       9.6.2       Clinical trials ................................................................................................16
    9.7     Overall Assessment of Toxicological Data ..........................................................17
  10.     ASSESSMENT OF ENVIRONMENTAL EFFECTS .............................................18
  11.     ASSESSMENT OF ENVIRONMENTAL HAZARD .............................................19
  12.    ASSESSMENT OF PUBLIC AND OCCUPATIONAL HEALTH AND SAFETY
  EFFECTS .............................................................................................................................20
  13.     RECOMMENDATIONS .........................................................................................21
  14.    MATERIAL SAFETY DATA SHEET ....................................................................22
  15.     REFERENCES .........................................................................................................22

                                                                                  NA/944


                               FULL PUBLIC REPORT

                              SPLENDA/SUCRALOSE
     1,6-dichloro-1,6-dideoxy--D-fructofuranosyl-4-chloro-4-deoxy--D-galactose




1.   APPLICANT

Johnson & Johnson Pacific Pty Ltd (ACN 001 121 446) of Stephen Road BOTANY NSW
2019 has submitted a limited notification statement in support of their application for an
assessment certificate for 1,6-dichloro-1,6-dideoxy--D-fructofuranosyl-4-chloro-4-deoxy--
D-galactose.


2.   IDENTITY OF THE CHEMICAL

No claims for exempt information were made by the applicant.

                                    1,6-dichloro-1,6-dideoxy--D-fructofuranosyl-4-chloro-
Chemical Name:
                                    4-deoxy--D-galactose.

Chemical Abstracts Service
                                    56038-13-2
(CAS) Registry No.:

                                    Trichlorogalactosucrose;
Other Names:
                                    TGS;
                                    4,1',6'-trichlorogalactosucrose.

                                    SPLENDA Brand Sweetener; Sucralose
Marketing Name:

                                    C12H19Cl3O8
Molecular Formula:

Structural Formula:
                                    OH

                                                   OH            OH
                      Cl
                                    O

                                             Cl
                      HO                                 O
                                              O
                                                                   Cl
                               OH

                                    397.64
Molecular Weight:

                                                                        10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                               3/24

                                     Infrared spectrum
Method of Detection and
Determination:


3.    PHYSICAL AND CHEMICAL PROPERTIES

                                        Free-flowing, white crystalline powder.
Appearance at 20°C & 101.3 kPa:

                                        125.5°C
Melting Point:

                                        Not determined
Specific Gravity:

                                        Not determined ­ see comments below
Vapour Pressure:

                                        283 g/L at 20°C
Water Solubility:

Partition Co-efficient
                                        Log POW = -0.51±0.05
(n-octanol/water):

                                        See comments
Hydrolysis as a Function of pH:

                                        Not determined
Adsorption/Desorption:

                                        Not determined
Dissociation Constant:

                                        Not supplied
Particle size distribution:

                                        Not flammable
Flash Point:

                                        Negligible
Surface Tension:

                                        Not flammable (MSDS)
Flammability Limits:

                                        Not supplied
Autoignition Temperature:

                                        Not explosive unless in dust form (MSDS)
Explosive Properties:

                                        Stable under normal conditions
Reactivity/Stability:


3.1   Comments on Physico-Chemical Properties

The vapour pressure of the notified chemical was not determined for this notification.
However, the notifier indicates that its vapour pressure is expected to be negligible.

The notifier did not determine the melting point, water solubility, partition coefficient and
surface tension, but provided an article by Jenner and Smithson (1989) which dealt with these
parameters. The water solubility was determined using a thermostatically controlled Wheaton
                                                                         10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                4/24

jacketted glass vessel. The sucralose solutions were stirred for 22 hours then left to stand for 1
hour, after which samples were analysed by HPLC. The water solubility was determined to
be 283 g/L at 20oC.

The partition coefficient was determined by the shake flask method. Aliquots of saturated
sucralose solution were mixed with water/octanol solution in test tubes, stopped and shaken
100 times in 5 mins. The tubes were then centrifuged for 10 mins at 20oC. Samples from the
resultant layers were analysed by HPLC. The log P was determined to be ­0.51±0.05.

A Kruss model K8600 tensiometer, ring method, was used to determine the surface tension.
Initially the surface tension of double distilled water was determined followed by dilute
sucralose solutions prepared with the double distilled water. It was found that the surface
tension of the double distilled water was only negligibly lowered by the sucralose. Thus,
sucralose has negligible surface tension, ie is not surface active.

The degradation of the notified chemical was investigated at 62, 50, 40 and 30°C at pH 1, 1.5,
2 and 3 (Tate and Lyle Group Research and Development, 1983) to determine the stability of
sucralose in beverages. A quantity of the notified chemical was added to the each of the
buffered solutions and the resulting solutions were stored at the above temperatures. The
storage time and sampling times varied according to pH and temperature with sampling
starting on day 1 and the last sample taken on day 336 for pH 3 at 30 and 40oC. All samples
were analysed by HPLC. It was found that the notified chemical broke-down by simple
hydrolysis to 1,6-dichloro-1,6-dideoxy-D-fructosfuranose and 4-chloro-4-deoxy-D-
galactopyranose, the constituent monomers. The rate of hydrolysis increased with temperature
and decreasing pH, eg at pH 1 and 62oC 98.8% of sucralose is hydrolysed after 120 hours, at
pH 2 and 62oC only 30.4% is hydrolysed after 120 hours. While this study dealt with low
pHs, in the environmental pH range of 4 to 9, significant hydrolysis is unlikely to occur.

No adsorption/desorption tests were conducted for this notification. The notified chemical's
high water solubility, low partition coefficient and lack of surface tension indicate that it is a
hydrophilic compound likely to partition mainly into the aqueous phase.

Sucralose contains no acidic or basic groups.


4.    PURITY OF THE CHEMICAL

                                       98.0-102.0 % Calculated on the anhydrous basis
Degree of Purity:

Hazardous Impurities:

        Chemical name:                 Arsenic (as As)
        CAS N o.:                      7440-38-2
        Weight percentage:             Less than 3 mg/kg
                                       Toxic (T) by inhalation (R23) and if swallowed (R25)
        Toxic properties:

        Chemical name:                 Heavy metals (as Pb)

                                                                             10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                    5/24

       Weight percentage:            10 mg/kg or less
                                     Toxic (T), may cause harm to the unborn child (R61),
       Toxic properties:
                                     possible risk of impaired fertility (R62), harmful by
                                     inhalation (R20) and if swallowed (R22), danger of
                                     cumulative effects (R33).

       Chemical name:                Methanol
       Synonyms:                     Methyl alcohol
       CAS N o.:                     67-56-1
       Weight percentage:            0.1 % or less
                                     Toxic (T) by inhalation (R23) and if swallowed (R25)
       Toxic properties:


Non-hazardous Impurities
(> 1% by weight):

       Chemical name:                4-chloro-4-deoxygalactose
       Synonyms:                     4-CG
       Weight percentage:            Very low
       CAS N o.:

       Chemical name:                1,6-dichloro-1,6-dideoxyfructose
       Synonyms:                     1,6-DCF
       Weight percentage:            Very low

                                     None
Additives/Adjuvants:


5.   USE, VOLUME AND FORMULATION


The notified chemical is in use worldwide as a non-nutritive sweetener in food and beverages
and as an excipient in pharmaceutical products. In Australia these uses have been approved by
the Australia New Zealand Food Authority (ANZFA) and the Therapeutic Goods
Administration (TGA).

In this notification the notified use is as a sweetener at 0.06% in mouth wash products. The
usual concentration of sucralose in foods is 0.025-0.15 %.

The notified chemical will be imported as a 25% component of the product Splenda in sealed
4 and 20 kg plastic (HDPE) containers. Formulation of the mouth wash products will be
performed by FH Faulding at 1538 Main North Rd, Salisbury South, South Australia. During
formulation of the mouth wash products, Splenda will be added directly to a 6000 L stainless

                                                                         10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                6/24

steel manufacturing vessel and mixed with other materials. The formulated mouthwash will
be pumped directly from the mixing vessel via an in built connecting hose to into 250 and
500 mL PET bottles with polypropylene screw top caps for sale to consumers.

For this use the notified chemical will be imported at 175 kg per year.


6.    OCCUPATIONAL EXPOSURE

Transport and Storage
Waterside, warehouse (4 workers, 20 minutes/day, 24 days/year) and transport (8 workers, 15
minutes/day, 24 days/year) workers are unlikely to be exposed to the notified polymer unless
the packaging is breached.

Formulation
Approximately 2 factory workers will have the potential for exposure to the notified chemical
during the formulation of the mouth wash products (maximum duration of exposure of 10
minutes/day, 12 days/year). Possible dermal and ocular exposure to spills and splashes
containing the notified chemical may occur during the addition of Splenda to the vessel,
during the mixing of the mouth wash products, and when connecting lines for filling into PET
bottles. Inhalation exposure to aerosols during mixing may also occur. The mixing process
occurs in a semi automated closed system in an area with an exhaust ventilation system.
Workers will wear overalls, dust masks, protective gloves and eye protection.

One QC sampling worker (duration of exposure of 5 minutes/day, 12 days/year) will take a 50
mL sample from the bulk liquid mouth wash formulations, which will be forwarded to a QC
laboratory for analysis by QC testing workers (2 workers, 20-60 minutes/day, 12 days/year).
QC sampling and testing worker may receive dermal and ocular exposure to drips and spills
containing the notified chemical during sampling and testing of mouth wash formulations.

Retail outlets
Retail outlet workers (approximately 500 workers, 1-10 minutes/day, 26-365 days/year) are
unlikely to be exposed to the notified polymer unless the packaging is breached.


7.    PUBLIC EXPOSURE

The public may be exposed to the notified chemical through transport accidents and
environmental contamination, although such events are unlikely. The notified chemical is an
ingredient of a mouth wash products intended for consumer use. Public exposure to the
notified chemical via the oral cavity can be expected to be widespread. If any contact with it
occurs by these means it is most likely to be dermal. Very small volumes of the mouth wash
may also be ingested. The notified chemical has negligible volatility and is unlikely to be
inhaled. The potential for public exposure to the notified chemical is therefore high.


8.    ENVIRONMENTAL EXPOSURE



                                                                          10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                 7/24

8.1   Release

The notifier estimates that during formulation of the mouthwash up to 0.1% per annum of
notified chemical will be released into the environment as a result of spills, equipment
cleaning and import container residue. This equates up to 0.175 kg per annum. It is possible
that the washwater generated by container or process equipment cleaning may be recycled
back into the process. Otherwise, it will be released to sewer.

It is expected that the plastic import drums containing residual polymer solution will be either
incinerated or cleaned and the plastic recycled. The mouthwash containers (250 or 500 mL
PET bottles), which will be sold to consumers, will be disposed of in domestic landfill. It is
estimated that less than 0.1% of the volume of the bottle will remain once it has been
`emptied', which equates to less than 175 g per annum of the notified chemical being
disposed of to landfill.

The notifier has estimated that approximately 10 mL of mouthwash will be used each time
someone rinses their mouth, with only 1 mL will remain in their mouth and 9 mL being spit
out down the drain. Thus, the majority (approximately 99%) of the notified chemical may
ultimately be released to the environment, on the understanding that any ingested will not be
absorbed but pass straight through the gut.


8.2   Fate

Wastes (0.1%) resulting from the cleaning process equipment and containers and spills may
be released into the sewer. The majority of the notified chemical will be released into the
sewer following mouth rinsing.

In landfill, the notified chemical contained in the disposed consumer PET bottles may leach
out but at very low levels and in a very diffuse manner.

The notifier has provided the results of a ready biodegradation test in an aerobic aqueous
media following a modified OECD TG 301E (1981) (Aquatox Ltd, 1984a). The
biodegradation was determined by the removal of dissolved organic carbon produced from a
mineral salt medium after it was inoculated with a mixed population of micro-organisms
(activated sludge) and stored in the dark at 22oC for 28 days. Sodium benzoate was used as
the reference substance. The results indicated that 5% of the notified chemical had degraded
over this time, while approximately 92% of the standard degraded in 28 days. The results
indicate that notified substance is not readily biodegradable.

The biodegradability of the notified chemical in a sediment/water system and water system
was investigated by Imperial Chemicals Industries PLC (1987). The biodegradation was
determined by the measurement of 14CO2 generated from the medium after it was inoculated
with either soil or micro-organisms population (activated sludge) and shaken at 20oC for 130
days. Sodium benzoate was used as the reference substance. For two of the soil inoculum, the
results indicated that approximately 56 days was required for microbial adaptation before
degradation began, thus resulting in 63 and 45.2% degradation by day 130. With the third soil
inoculum the adaptation period appeared to be 100 days, with 14.2% degradation by day 130.
No degradation was observed in the activated sludge inoculum. These results indicate that the

                                                                           10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                  8/24

notified chemical is inherently biodegradable but not readily degradable.

Due to its high water solubility and low log Pow, the notified chemical should not
bioaccumulate (Connell, 1990).


9.     EVALUATION OF TOXICOLOGICAL DATA

Because of its intended uses in food, beverages and pharmaceuticals, the notified chemical
has undergone much toxicological investigation including human volunteer studies. The
toxicological data have been extensively reviewed by government agencies and the chemical
approved for use in products for human ingestion by many national authorities.

9.1.    Pharmacokinetics and Metabolism

When administered orally, between 11-27% of the sucralose is absorbed from the
gastrointestinal tract in male humans. The remaining sucralose is excreted unchanged in
faeces (USFDA Department of Health and Human Services 1998).

Following gastrointestinal absorption, between 20-30% of the sucralose is broken down to
two metabolites in human. The remaining sucralose is excreted unchanged in urine (USFDA
Department of Health and Human Services 1998).

Studies in rats indicate that repeated dosing with sucralose does not induce microsomal
enzymes. Furthermore chronic dosing did not produce evidence of metabolic adaptation
(USFDA Department of Health and Human Services, 1998).

9.2     Acute toxicity

The acute oral toxicity of sucralose and its hydrolysis products, 4-chloro-4-deoxygalactose (4-
CG) and 1,6-dichloro-1,6-dideoxyfructose (1,6-DCF), have been assessed in mice and rats.
The results of these studies are summarised in table 9.2.1.

Table 9.2.1. Acute oral toxicity of sucralose and its hydrolysis products.

Species                    Sex                  Route           LD50 (mg/kg bw)
Sucralose
Mouse                 Not specified              Oral               >16 000
Rat                       Male                   Oral               >10 000

Sucralose hydrolysis products
Mouse                Male & female               Oral                 3499
Rat                  Male & female               Oral                 1629
(TGA, unknown date)

9.3    Genotoxicity

The genotoxicity of sucralose and the two sucralose hydrolysis products, 4-CG and 1,6-DCF
have been assessed. The results of these studies are summarised in tables 9.3.1-4.
                                                                            10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                   9/24

Table 9.3.1. Sucralose mutagenicity studies.

Test system              Test object           Sucralose                   Result
                                             concentration
 S. typhimurium       TA98, TA100,             16-10 000                  Negative
                                                µg/plate
    (+ & - S9)       TA1535, TA1537,
                        TA1538.

 S. typhimurium        TA98, TA100.            16-10 000                  Negative
                                                µg/plate
    (+ & - S9)

     E. coli           W3110, P3478            0.5 -1 000                 Negative
                                                µg/plate
   (+ & - S9)

Mouse lymphoma             T K +/-           1 3 3 5 ­ 10 0 0 0   Positive at 7 500 & 10 000
                                                  µg/mL           µg/mL. Cell viability was
  (+ & - S9)
                                                                         less than 50%

                                             8 - 200 µg/mL                Negative
  Mammalian           Peripheral blood
  cytogenetics          lymphocytes
    (human)               (in vitro)

   Mammalian            Bone marrow          5 x 200 mg/kg                Negative
cytogenetics (rat)   (in vivo; oral route)         bw

     Mouse           In vivo; oral route     1 000 ­ 5 000                Negative
micronucleus test                            mg/kg bw, 24,
                                              48 and 72 h
(TGA, unknown date)

Table 9.3.2. 4-CG mutagenicity studies.

Test system              Test object             4-CG                      Result
                                             concentration
 S. typhimurium       TA98, TA100,             16-10 000                  Negative
                                                µg/plate
    (+ & - S9)       TA1535, TA1537,
                        TA1538.

Mouse lymphoma             T K + /-           1.3 ­ 10 000                Negative
                                                 µg/mL

  Mammalian           Peripheral blood         40 ­ 1 000                 Negative
                                                 µg/mL
  cytogenetics          lymphocytes
    (human)               (in vitro)

   Mammalian            Bone marrow          5 x 50, 150 &                Negative
cytogenetics (rat)   (in vivo; oral route)   150 mg/kg bw
(TGA, unknown date)

Table 9.3.3. 1,6-DCF genetic toxicity studies.


                                                                                    10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                         10/24

Test system              Test object            1,6-DCF                  Result
                                             concentration
 S. typhimurium       TA98, TA100,             16 -10 000               Negative
                                                µg/plate
    (+ & - S9)       TA1537, TA1538.

 S. typhimurium           TA1535.              16-10 000                Negative
                                                µg/plate

 S. typhimurium           TA1535.              250 - 5 000    Positive (2-3 fold increase in
                                                µg/plate           revertant colonies).

 S. typhimurium       TA98, TA100,             16 -10 000               Negative
                                                µg/plate
    (+ & - S9)       TA1535, TA1537,
                        TA1538

 S. typhimurium           TA1535.             2 000 - 5 000   Positive (2-3 fold increase in
                                                 µg/plate          revertant colonies).

 S. typhimurium       TA98, TA100,             16 -10 000               Negative
                                                µg/plate
    (+ & - S9)       TA1537, TA1538.

 S. typhimurium           TA1535.              60 - 6 000               Negative
                                                µg/plate

 S. typhimurium           TA1535.              60 - 3 000               Negative
                                                µg/plate
      (+ S9)

                                             6 000 µg/plate
 S. typhimurium           TA1535.                             Positive (2-3 fold increase in
                                                                   revertant colonies).

                                             13 - 42 µg/mL
Mouse lymphoma             T K +/-                                      Negative

                                             56 - 133 µg/mL
Mouse lymphoma             T K +/-                            Positive (increased mutation
                                                               frequency was associated
                                                                with decrease viability).

                                             13 - 169 µg/mL
Mouse lymphoma             T K +/-                                      Negative

                                             10 - 40 µg/mL
Mouse lymphoma             T K +/-                                      Negative

                                             53 - 127 µg/mL
Mouse lymphoma             T K +/ -                           Positive (increased mutation
    (+ S9)                                                     frequency was associated
                                                                with decrease viability).

                                             1.5 - 40 µg/mL
  Mammalian           Peripheral blood                                  Negative
  cytogenetics          lymphocytes
    (human)               (in vitro)
   (+ & - S9)

   Mammalian            Bone marrow          1 000 mg/kg bw             Negative
cytogenetics (rat)   (in vivo; oral route)

  Mammalian             Bone marrow           5 x 50, 150 &             Negative

                                                                                  10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                       11/24

cytogenetics (rat)     (in vivo; oral route)   500 mg/kg bw;
                                                24 h interval

   Sex-linked             Drosophila           0.2 ­ 2 mg/mL;      Negative
 recessive lethal       melanogaster ( i n         3 days.
                             vivo)

     Mouse              Bone marrow (in         415 ­ 1 660        Negative
micronucleus test       vivo; oral route)      mg/kg bw/day

     Mouse              Bone marrow (in        1 000 ­ 2 500       Negative
micronucleus test       vivo; oral route)        mg/kg bw

  Mouse sister          Bone marrow (in         200 ­ 2 000        Negative
   chromatid            vivo; oral route)        mg/kg bw
   exchange

  Covalent DNA            Liver, kidney,        21 mg/kg bw        Negative
      binding            small intestine,
(rat; oral; in vivo)    colon, stomach &
                          bone marrow
(TGA, unknown date)

Table 9.3.4. Sucralose hydrolysis products (sucralose-HP) mutagenicity studies.

Test system                Test object         Sucralose-HP         Result
                                               concentration
 Dominant lethal       In vivo; oral route     30 - 270 mg/kg      Negative
     assay                                         bw/day
   (mouse)
(TGA, unknown date)

9.4     Repeated dose toxicity

9.4.1    Bodyweight gain/food consumption

A number of studies have been conducted examining the acceptability and palatability of
sucralose when administered to rats in drinking water or diet. It was determined that sucralsoe
levels up to 3200 ppm were acceptable in drinking water and that levels above 800 ppm
resulted in reduced food consumption (USFDA Department of Health and Human Services
1998).

A pair feeding study was conducted to determine if any reduced weight gain associated with
sucralose intake was due to an effect of the test substance and not a reduction in food
consumption. Five groups of female Sprague-Dawley CD rats were used in the study. Group
1 was allowed unrestricted access to a diet containing 3% sucralose. Rats in group 2 were fed
a daily amount of basal diet equivalent to the mean group intake consumed on the previous
day by rats in group 1. Rats in group 3 were allowed unrestricted access to basal diet. Group 4
was administered by gavage an amount equivalent to group 1. Group 5 served as the control
for group 4 and received distilled water by gavage. A significant decrease in bodyweight gain


                                                                             10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                  12/24

and food consumption was detected in groups 1 and 2 relative to the group 3 control (USFDA
Department of Health and Human Services 1998).

In a separate study, groups of Sprague-Dawley rats (10/sex/group) were dosed by gavage with
2000 mg/kg bw/day for 13 weeks, 3000 mg/kg bw/day for 9 weeks or 4000 mg/kg bw/day for
4 weeks. No treatment related changes were detected. Food consumption and bodyweight
gain were slightly increased (103-109%) when compared to controls (USFDA Department of
Health and Human Services 1998).

A study has been conducted examining if decrease food consumption and bodyweight gain
associated with dietary sucralose intake is due to increased spillage of the sucralose
containing diet. In this study 3 groups of Sprague-Dawley rats (15/sex/group) were fed either
a basal diet or a basal diet containing 3 or 5% sucralose. A 5-8% decrease in food
consumption, associated with a 10-15% reduction in bodyweight gain, was observed in
treated rats. During the first two weeks rats fed a diet containing sucralose showed
significantly higher spillage when compared to controls (USFDA Department of Health and
Human Services 1998).

A diet restriction study was also conducted to examine decreased food consumption and
bodyweight gain associated with dietary sucralose intake. Results from this study indicate that
3% dietary sucralose resulted in a significant decrease in weight gain in Sprague-Dawley CD
rats that was attributable to the test substance. 1% dietary sucralose (equivalent to 500 mg/kg
bw/day) had no effect on bodyweight gain and was considered the NOEL for this toxic
endpoint (USFDA Department of Health and Human Services 1998).

Sucralose related bodyweight gain effects were also investigated in groups of Sprague-
Dawley rats (20/sex/group) dosed by gavage with 0-3000 mg/kg bw/day for 26 weeks. Food
intake for males dosed with 3000 mg/kg bw/day was 3.9% greater than controls. Interestingly,
the adjusted mean body weight gain of males dosed with 3000 mg/kg bw/day was
significantly decreased (4.6%; p = 0.035) compared to controls. The NOEL for the
bodyweight gain effect observed in this study was determined to be 1500 mg/kg bw/day
(USFDA Department of Health and Human Services 1998).

9.4.2   Chronic toxicity/carcinogenicity studies

The toxicity of sucralose has been examined in a combined chronic toxicity/carcinogenicity
study consisting of a breeding phase, a carcinogenicity phase and a chronic toxicity phase. In
the breeding phase 140 (70 /sex) Sprague-Dawley CD rats were fed diets containing 0, 0.3, 1
or 3% sucralose for a 4 week period prior to mating and during gestation. Two weaning pups
(1/sex) from each of 50 litters were allocated to the carcinogenicity phase of the study while
60 additional rats (30/sex) were selected for the chronic toxicity phase. Rats were sacrificed
after 52, 78 and 104 weeks of sucralose treatment. The reproductive performance and fertility
of parental rats during the breeding phase were normal. The survival of rats in the chronic and
carcinogenicity phases of the study were unaffected by sucralose. There was no evidence of
treatment related neoplasm in any rat during the carcinogenicity phase. A minimal increase in
the incidence of renal pelvic mineralisation and epithelial hyperplasia lesions were detected in
rats, primarily females treated with 3% sucralose, in the chronic and carcinogenicity phases.
During the chronic and carcinogenicity phases of the study all sucralose treated rats showed
decreased bodyweight gain. At the end of the chronic toxicity phase the reduction in

                                                                           10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                13/24

bodyweight gain was 12-25% while food intake was reduced by 5-10% compared to controls.
A NOEL could not be determined from this study (USFDA Department of Health and Human
Services 1998).

The carcinogenicity of sucralose has also been tested in a study where groups of Charles
River CD-1 mice (52/sex/group) were fed 0, 0.3, 1 and 3% sucralose in the diet for 104
weeks. During the treatment period the mean body weight gain of mice dosed with 3%
sucralose was significantly reduced compared to controls, even though food consumption was
normal. A significant decrease in erythrocyte count was also detected in females dosed with
3% sucralose. No evidence of treatment related neoplasia was detected. The dietary NOEL
was determined to be 1% sucralose (equivalent to 1500 mg/kg bw/day) (USFDA Department
of Health and Human Services 1998).

The chronic toxicity of sucralose has been tested in a study where groups of beagle dogs
(4/sex/group) were dose with 0, 0.3, 1 and 3% sucralose in the diet for 52 weeks. An increase
in body weight gain, accompanied by a general increase in food consumption, was observed
at all dose levels. The dietary NOEL was determined to be 3% sucralose (equivalent to 750
mg/kg bw/day) (USFDA Department of Health and Human Services 1998).

The chronic toxicity of sucralose hydrolysis products has been tested in a study where groups
of Sprague-Dawley CD rats (50/sex/group) were dose with an equimolar mixture of 4-CG and
1,6-DCF at 0, 200, 600 and 2000 ppm in the diet for 104 weeks. No evidence of treatment
related neoplasia was detected. A small increase in the incidence of hepatocellular clear cell
foci was observed in treated rats. The mean bodyweight gain of females treated with 2000
ppm was reduced by 24%, which was accompanied by a 14% reduction in food intake. The
dietary NOEL was determined to be 600 ppm of sucralose hydrolysis products (equivalent to
30 mg/kg bw/day) (USFDA Department of Health and Human Services 1998).

9.4.3    Immunotoxicity

The immunotoxicity of sucralose was assessed in groups of Sprague-Dawley rats
(13/sex/group) dosed by gavage with 0-3000 mg/kg bw/day for 28 days. A significant
decrease in mean thymus weight was noted in males dosed with 3000 mg/kg bw/day. Due to
difficulties in interpreting the large variation in data at observed at 1500 mg/kg bw/day, the
NOEL for immunological endpoints was determined to be 750 mg/kg bw/day (USFDA
Department of Health and Human Services 1998).

9.4.4    Neurotoxicity

Mice and monkeys that received sucralose or an equimolar mixture of sucralose hydrolysis
products at doses up to 1500 mg/kg bw/day did not exhibit any clinical signs of neurotoxicity
or morphological changes in central nervous system tissues (USFDA Department of Health
and Human Services 1998).

9.5     Reproductive/Developmental Toxicity

In a two generation reproductive toxicity study, groups of 60 Sprague-Dawley CD rats
(30/sex) were dosed with 0, 0.3, 1 and 3% sucralose in the diet for 10 weeks prior to breeding
and throughout two successive generations. Reproductive endpoints (estrous cycles, mating

                                                                          10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                               14/24

performance, fertility index, gestation length and gestation index), litter size and offspring
viability were considered normal in either generation. A decrease in body weight gain was
observed during the premating periods of the first (11-25%) and second (2-12%) generations.
A slight decrease in food intake was also observed during the premating periods of the first
(5-9%) and second (3-5%) generations. A significant decrease in thymic weight was detected
in both generations at the 3% dose level. The findings of this study indicate that sucralose
does not causes reproductive effects in rats up to 3% in the diet (USFDA Department of
Health and Human Services 1998).

The ability of sucralose to cause reproductive/developmental toxicity was examined in a
teratology study. Sucralose was dose orally (gavage) at 0, 500, 1000 and 2000 mg/kg bw/day
to groups of 20 Sprague-Dawley CD rats from day 5 through day 15 of gestation. Bodyweight
gain, food consumption, number of live young, and foetal and placental weight were
unaffected by the treatment. The number of implantation sites, pre-implantation loses, and
post-implantation losses were normal. The findings of this study indicate that sucralose does
not causes maternal toxicity, embryo toxicity, foetal toxicity of induce teratology in rats at
oral doses up to 2000 mg/kg bw/day (USFDA Department of Health and Human Services
1998).

The ability of sucralose to induce teratology was examined in groups of 16-18 pregnant
rabbits dosed orally (gavage) with 0, 175, 350, and 700 mg/kg bw/day during days 6-19 of
gestation. Eleven treatment unrelated deaths were recorded during the study. 2/18 treatment
related deaths were noted in the 700 mg/kg bw/day group. Prior to death, both rabbits showed
weight loss and reduced food intake. 3/18 rabbits in the 700 mg/kg bw/day group failed to
become pregnant. Of the 9 pregnant rabbits in the 700 mg/kg bw/day, only 5 carried to term
and produced viable young. At 700 mg/kg bw/day a decrease in the mean number of viable
young per litter and an increase in post-implantation losses were observed. Gastrointestinal
tract disturbances were also noted in the high dose group. Although maternal and foetal
toxicity was observed at 700 mg/kg bw/day, no evidence of teratology was detected (USFDA
Department of Health and Human Services 1998).

The ability of sucralose hydrolysis products to cause reproductive/developmental toxicity was
examined in a two generation reproductive toxicity study. Groups of 60 Sprague-Dawley CD
rats (30/sex) were dosed with an equimolar mixture of 4-CG and 1,6-DCF at 0, 200, 600 and
2000 ppm in the diet for 10 weeks prior to breeding and through two successive generations.
In both generations estrus cycles, mating performance, fertility, gestation length, litter size
and offspring viability were normal. Body weight gain of females at all doses and males at
2000 ppm was significantly reduced in the premating period for both generations. A reduction
in weight gain was observed in females during pregnancy and in offspring from birth to
weaning in both generations. 4-CG and 1,6-DCF at levels up to 2000 ppm in the diet caused
no alterations in the reproductive performance of rats over two generations (USFDA
Department of Health and Human Services 1998).

The ability of sucralose hydrolysis products to induce teratology was examined in groups of
20 pregnant Sprague-Dawley CD rats dosed orally (gavage) with an equimolar mixture of 4-
CG and 1,6-DCF at 0, 30, 90 and 270 mg/kg bw/day during day 6-15 of gestation. No dose
related increase in teratology was detected. Placental weight and bodyweight gain of dams in
the 270 mg/kg bw/day group were significantly reduced (USFDA Department of Health and
Human Services 1998).

                                                                           10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                15/24

9.6     Studies in humans

9.6.1    Diabetic studies

In a single dose crossover study the level of plasma glucose and serum c-peptide in the serum
of insulin-dependant (type I diabetics) and non insulin-dependant (type II diabetics) diabetic
patients was unaffected by a single dose of sucralose (1000 mg) (USFDA Department of
Health and Human Services 1998).

In a separate study sucralose was administered orally at 667 mg/day for 6 months to patients
with type II diabetes. A small yet statistically significant increase in haemoglobin
glycosylation was observed from 1-6 months in the treatment group. This increase was
determined not to be a direct effect of sucralose (USFDA Department of Health and Human
Services 1998).

In a follow up study, human red blood cell preparations from diabetic and non-diabetic
patients were treated with 100 mg/L sucralose. Sucralose was not found to increase
haemoglobin glycosylation in this study (USFDA Department of Health and Human Services
1998).

In a second study where sucralose was administered orally at 667 mg/day no effect on
haemoglobin glycosylation was observed in the treatment group. It was concluded that 667
mg/day sucralose had no effect on long term glucose homeostasis (as measured by
haemoglobin glycosylation) in type II diabetics (USFDA Department of Health and Human
Services 1998).

9.6.2    Clinical trials

The effect of sucralose on healthy humans was assessed in 8 subjects (4 per sex). Sucralose
was administered orally at 0, 1, 2.5, 5 and 10 mg/kg bw at 24 hour intervals. This was
followed by administration of sucralose at 2 mg/kg bw/day for 3 days then 5 mg/kg bw/day
for 4 days. No adverse reactions or complaints were noted throughout the study. All
haematological and biochemical markers examined were normal, as were ECG parameters,
urine volume and blood insulin levels (TGA, unknown date).

In a separate study the effect of sucralose in healthy human volunteers was compared to that
of fructose. In this study sucralose was administered to 79 human volunteers at 125 mg/day
for weeks 1-3, 250 mg/day on weeks 4-7 and 500 mg/day on weeks 8-13. Fructose was
administered to 31 human volunteers at 100 g/day. All ECG parameters and haematological,
urinalysis and biochemical markers examined were normal (TGA, unknown date).

In a double blind cross over study eight healthy human volunteers were administered
sucralose alone (10 mg/kg bw), sucrose alone (100 g) and a mixture of sucralose (10 mg/kg
bw) and sucrose (100 g) at 24 hour intervals in random order. The serum concentration of
glucose and fructose was similar in patients that received sucrose and sucralose when
compared to those that received sucrose alone. Sucralose had no effect on insulin levels when
administered alone and did not alter insulin responses to sucrose (TGA, unknown date).


                                                                          10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                               16/24

9.7   Overall Assessment of Toxicological Data

Sucralose was poorly absorbed after oral administration in humans.

The notified chemical was of very low acute oral toxicity in rats (LD50 > 16 000 mg/kg bw)
and mice (LD50 > 10 000 mg/kg bw). The sucralose hydrolysis products, 4-CG and 1,6-DCF,
when tested as an equimolar mixture were of low and very low acute oral toxicity in rats
(LD50 = 1629 mg/kg bw) and mice (LD50 = 3499 mg/kg bw) respectively.

Sucralose was non mutagenic in three Ames tests and non clastogenic in human lymphocytes
and rat bone marrow cells. Sucralose was weakly mutagenic in a mouse lymphoma mutation
assay. 4-CG was non mutagenic in an Ames test and a mouse lymphoma assay. 4-CG was
non clastogenic as determined by a human lymphocyte assay and a rat bone marrow test.
Although 1,6-DCF was found to be weakly mutagenic in 3/9 Ames tests and 2/5 mouse
lymphoma assays, it was non clastogenic as determined by two rat bone marrow
chromosomal aberration assay and a human lymphocyte test. 1,6-DCF did not induce sister
chromatid exchanges or micronuclei in mouse bone marrow cells. A sex linked recessive
lethal assay in Drosophilia melanogaster and a covalent DNA binding potential study in rats
were negative. The sucralose hydrolysis products 4-CG and 1,6-DCF were not genotoxic as
determined by a dominant lethal test in the mouse when tested as an equimolar mixture.

There was no evidence of treatment related neoplasm in rats fed a diet containing up to 3%
sucralose (equivalent to 3000 mg/kg bw/day) during the carcinogenicity phase of a combined
chronic toxicity/carcinogenicity study and during a 104 week carcinogenicity study. No
evidence of treatment related neoplasia was detected in rats dosed with an equimolar mixture
of the sucralose hydrolysis products, 4-CG and 1,6-DCF, at up to 2000 ppm in the diet for
104 weeks.

Decreased bodyweight gain was observed in rats and mice fed diets containing 3% sucralose
for 104 weeks. This effect was not observed in beagle dogs dosed with 3% sucralose
(equivalent to 750 mg/kg bw/day) in the diet for 52 weeks. A minimal increase in the
incidence of renal pelvic mineralisation and epithelial hyperplasia lesions were detected in
rats, primarily females treated with 3% sucralose. A significant decrease in erythrocyte count
was detected in female mice dosed with 3% sucralose. Decreased bodyweight gain and a
small increase in the incidence of hepatocellular clear cell foci was observed in female rats
treated dose with an equimolar mixture of 4-CG and 1,6-DCF at 2000 ppm in the diet for 104
weeks. A number of studies have been conducted examining the acceptability and palatability
of sucralose as a cause of reduced bodyweight gain when administered in drinking water or
diet. It was determined that reduced bodyweight resulted from reduced palatability of diets
containing sucralose. The dietary NOEL for mice and rats was determined to be 30 000 ppm
(equivalent to 1500 mg/kg bw/day). The dietary NOEL for the sucralose hydrolysis products
was determined to be 600 ppm (equivalent to 30 mg/kg bw/day).

The notified chemical was not teratogenic in rats and rabbits, was not neurotoxic in mice and
monkeys, and had no effect on male and female reproduction in rats, or insulin secretion and
carbohydrate metabolism in normal and diabetic human volunteers. Sucralose was found to
induce a reduction in thymus weight in rats dosed orally with 3000 mg/kg bw/day. The NOEL
for immunological endpoints was 750 mg/kg bw/day.


                                                                          10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                               17/24

The sucralose hydrolysis products, 4-CG and 1,6-DCF, when test as an equimolar mixture
was not teratogenic, not neurotoxic, and had no effect on male and female reproduction.

The notified chemical is not determined to be a hazardous substance according to the NOHSC
Approved Criteria for Classifying Hazardous Substances (NOHSC, 1999).


10.   ASSESSMENT OF ENVIRONMENTAL EFFECTS

The following ecotoxicity studies have been supplied by the notifier and were carried out
according to OECD Principles of Good Laboratory Practice and Test Methods, or accepted
equivalent.

           Test                           Species                         Results
                                                             LC50 >3200 mg/L
96 h Acute toxicity         Bluegill sunfish
US EPA                      (Lepomis macrochirus)
96 h Acute toxicity         Rainbow trout                    LC50 =1800 mg/L
                                                             LC50 >2400 mg/L
OECD TG 203
48 h Acute toxicity         Daphnia magna                    EC50 >1800 mg/L
OECD TG 202
                                                             NOEC =1800 mg/L
21 d C hronic t ox icity    Daphnia magna
OECD guidelines
                            Green Algae
96h Acute toxicity                                           NOEC =1800 mg/L
                            (Selenastrum capricornutum)
OECD TG 201                                                  EbC50 >1800 mg/L
                                                             ErC50 >1800 mg/L
3 h respiratory toxicity Activated            sludge   micro- NOEC = 100 mg/L
                         organisms
OECD        TG      209-
respirometric
technique
* NOEC - no observable effect concentration

Imperial Chemicals Industries PLC (1985a) studied the toxicity of the notified chemical on
Bluegill sunfish using the US EPA Office of Toxic Substances Guidelines for Testing
Chemicals (EG-9). The fish were exposed to the notified chemical at the nominal
concentrations of 0, 320, 560, 1000, 1800 and 3200 mg/L under static conditions at 22oC for
96 hours. Mortalities were observed in 1800 and 3200 mg/L were attributed to stress due to
decreased dissolved oxygen. These were the only mortalities observed during the 96 hours
except for 1 in the control. Therefore, the LC50 is greater than 3200 mg/L.

Aquatox Ltd (1984b) investigated the acute fish toxicity of the notified chemical using
Rainbow trout and following OECD TG 203. Two definitive tests were conducted under
static conditions at a temperature of 14oC. In the first the nominal concentrations used were 0,
560, 1000 and 1800 mg/L. In this study, 50% mortality was observed at 1800 mg/L. The

                                                                           10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                18/24

estimated LC50 of 1800 mg/L was calculated by the moving averages method. In the second
study the nominal concentrations used were 0, 560, 1000, 1800 and 2400 mg/L. Only 20%
mortality observed in the highest concentration (2400 mg/L) with none in any other
concentrations. Therefore, the LC50 is greater than 2400 mg/L with the NOEC being 1800
mg/L.

The acute toxicity of the notified chemical was studied by Aquatox Ltd (1984c) following the
OECD TG 202. Daphnia were observed for 48 hours under static conditions at the nominal
concentrations of 0, 180, 560, 1000 and 1800 mg/L. At 1800 mg/L no immobilisation was
observed, while at 180 and 1000 mg/L 5% immobilisation was observed. Therefore from the
study results it can only be said that the EC50 is greater than the maximum concentration
studied (ie >1800 mg/L).

Imperial Chemicals Industries PLC (1986a) studied the chronic toxicity of the notified
chemical to Daphnia magna following the OECD guidelines. Daphnia, older than 24 hours of
age, were exposed to the notified chemical under semi-static conditions at 20oC for 21 days.
The nominal concentrations used were 0, 180, 320, 560, 1000 and 1800 mg/L. During the
study mortality and number of offspring were observed. No effects were observed over the
full 21 days, therefore, the LC50 is greater than 1800 mg/L and the NOEC is 1800 mg/L.

Imperial Chemicals Industries PLC (1986b) investigated the toxicity of the notified chemical
on green algae following the OECD TG 201, with an extended test duration of 96 hours. The
nominal concentrations studied were 0, 180, 320, 560, 1000 and 1800 mg/L. For the 96 hours
the test vessels were maintained at 24oC. Based on area under the growth curve, and
logarithm growth rate, the EbC50 and ErC50 were found to be greater than 1800 mg/L, while
the NOEC was 1800 mg/L.

These studies indicate that the notified chemical is practically non-toxic to aquatic organisms
(fish, Daphnia and algae).

The toxicity of the notified chemical to aerobic micro-organisms was studied by Imperial
Chemicals Industries PLC (1985b) following the OECD TG 209 (Respirometric technique).
The nominal concentrations of the notified chemical were 0, 10, 32, 100, 180 and 320 mg/L.
3,5-Dichlorophenol was used as the control substance. Each test beaker included 200 mL of
activated sludge. The beakers were kept at 22oC and aerated continuously for 3 hours. After 3
hours a respirometric cell was used to determine the oxygen uptake rate. The results indicated
that at 180 and 320 mg/L of notified chemical there had been a slight inhibition of respiration,
with no impact at other concentrations. The NOEC therefore, is 100 mg/L and the LC50 is
greater than 320 mg/L. These results indicate that the notified chemical is very slightly toxic
to sewage sludge micro-organisms (Mensink, 1995).


11.   ASSESSMENT OF ENVIRONMENTAL HAZARD

The intended use pattern of the notified chemical is expected to result in the majority of the
chemical being eventually released to the environment. However, this will be in a dilute
manner, as the notified chemical contained within a mouthwash will be released from
domestic use at low concentrations. The ecotoxicity data indicates the notified substance is

                                                                           10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                19/24

practically non-toxic to fish, daphnia and algae and very slightly toxic to sewage micro-
organism based on measured concentrations.

In a worst case based on maximum annual imports of 175 kg per annum, all of which is
released to sewer and assuming no removal during sewage treatment processes, a national
population of 19,000,000 and an average personal contribution of 150 L/day to overall
sewage flows, the predicted concentration in sewage effluent on a nationwide basis is
estimated as 0.17 µg/L.

        Amount of sucralose entering sewer annually             175 kg
        Population of Australia                                 19 million
        Amount of water used per person per day                 150 L
        Number of days in a year                                365
                                                                0.17 µg/L (0.17 ppb)
        Estimated PEC

When released to receiving waters the concentration is reduced by a further factor of at least
10, so the Predicted Environmental Concentration (PEC) is around 0.017 µg/L.

The nationwide PEC estimate indicates that after discharge to receiving waters the
environmental concentration of the notified chemical will be at least 6 orders of magnitude
less than the demonstrated toxicity to micro-organisms (LC50 >320 mg/L).

Wastes containing the notified chemical including residues from imported drums and from
repackaging will also be disposed of in landfill where it may leachout at very low
concentrations.

Therefore, the environmental exposure and overall environmental hazard from the notified
chemical is expected to be acceptable.


12.   ASSESSMENT OF PUBLIC AND OCCUPATIONAL HEALTH AND SAFETY
       EFFECTS

Hazard Assessment

Based on the toxicological data provided, the notified chemical would not be acutely toxic via
the oral routes. It is not likely to be genotoxic or clastogenic.

Decreased bodyweight gain, a minimal increase in the incidence of renal pelvic mineralisation
and epithelial hyperplasia lesions and a decrease in erythrocyte count have been observed
upon repeated exposure to 3% sucralose. The dietary NOEL for mice and rats was determined
to be 30 000 ppm (equivalent to 1500 mg/kg bw/day).

The notified chemical was not teratogenic or neurotoxic and had no effect on reproduction,
insulin secretion and carbohydrate metabolism. Sucralose was found to induce a reduction in
thymus weight in rats dosed orally with 3000 mg/kg bw/day. The NOEL for immunological
endpoints was 750 mg/kg bw/day.

The notified chemical would not be classified as a hazardous substance according to NOHSC
                                                                          10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                               20/24

Approved Criteria for Classifying Hazardous Substances (NOHSC, 1999) in terms of the
toxicological data provided.

Occupational Health and Safety

Factory workers will have the potential for exposure to the notified chemical during the
formulation of the mouth wash products containing 0.06 % notified chemical. Possible
dermal and ocular exposure to spills and splashes containing the notified chemical may occur
during the addition of Splenda (25 % notified chemical) to the mixing vessel, during the
mixing of the mouth wash products, and when connecting lines for filling into PET bottles.
Dermal and ocular exposure will be controlled by the use of overalls, protective gloves and
eye protection. Inhalation exposure to any aerosols generated during the mixing of the mouth
wash is expected to be negligible, as the mixing process occurs in a semi automated closed
system in an area with an exhaust ventilation system.

QC sampling and testing workers may receive dermal and ocular exposure to drips and spills
containing the notified chemical during sampling and testing of mouth wash formulations.
Although not indicated by the notifier, QC sampling and testing workers should wear
laboratory coats, protective gloves and eye protection when handling solutions containing the
notified chemical to control exposure.

Retail outlet workers are unlikely to be exposed to the notified polymer unless the packaging
is breached. Waterside, warehouse and transport workers are unlikely to be exposed to the
notified polymer unless the packaging is breached.

Given the non-hazardous nature of the notified chemical and the low potential for exposure,
the health risk to workers handling the notified chemical is negligible.

Public Health

The notified chemical is approved for use in foods and therapeutic goods for oral ingestion.
The transient nature of the contact with the oral cavity, the very low concentration of the
notified chemical in the mouth wash, the low enteric absorption rate and the low toxicity of
the notified chemical and its metabolites, suggest that the notified chemical will not pose a
significant hazard to public health when used as proposed.


13.       RECOMMENDATIONS

Control Measures

Occupational Health and Safety

      ·   A copy of the MSDS should be easily accessible to employees.

      ·   If products and mixtures containing the notified chemical are classified as hazardous
          to health in accordance with the NOHSC Approved Criteria for Classifying
          Hazardous Substances, workplace practices and control procedures consistent with


                                                                           10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                21/24

       provisions of State and Territory hazardous substances legislation must be in
       operation.


Secondary notification

The Director of Chemicals Notification and Assessment must be notified in writing within 28
days by the notifier, other importer or manufacturer:

       Under Subsection 64(2) of the Act:
       - if any of the circumstances listed in the subsection arise.

The Director will then decide whether secondary notification is required.

No additional secondary notification conditions are stipulated.


14.   MATERIAL SAFETY DATA SHEET

The MSDS for the notified chemical was provided in a format consistent with the National
Code of Practice for the Preparation of Material Safety Data Sheets (NOHSC 1994).

This MSDS was provided by the applicant as part of the notification statement. It is
reproduced here as a matter of public record. The accuracy of this information remains the
responsibility of the applicant.


15.   REFERENCES

Aquatox Ltd (1984a). Determination of Biodegradability of 1,6-dichloro-1,6-dideoxy--D-
fructosfuranosyl-4-chloro-4-deoxy--D-galactopyranoside (TGS) by a screening test with as
inoculum of activated sludge: Aquatox Report no. ABD/83/073. Aquatox Ltd, Suffolk, IP23
7PX.

Aquatox Ltd (1984b). The Acute toxicity of 1,6-dichloro-1,6-dideoxy--D-fructosfuranosyl-
4-chloro-4-deoxy--D-galactopyranoside (TGS) to Rainbow Trout: Aquatox Report no.
AFT/83/051. Aquatox Ltd, Suffolk, IP23 7PX.

Aquatox Ltd (1984c). Acute toxicity of 1,6-dichloro-1,6-dideoxy--D-fructosfuranosyl-4-
chloro-4-deoxy--deoxy-galactopyranoside (TGS) to Daphnia magna. Aquatox Report no.
AFT/83/050. Aquatox Ltd, Suffolk, IP23 7PX.

Connell, D.W. (1990). General Characteristics of Organic Compounds Which Exhibit
Bioaccumulation. In: Bioaccumulation of Xenobiotic Compounds. CRC Press, Boca Raton,
USA, pp. 47-57.

Imperial Chemicals Industries PLC (1985a). BL/B/2686 ­ Trichlorogalactosucrose (TGS):
Acute Toxicity to bluegill sunfish (Lepomis macrochirus). Brixham Study no N197/B.
Imperial Chemicals Industries PLC

                                                                            10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                                 22/24

Imperial Chemicals Industries PLC (1985b). BL/B/2546 ­ Trichlorogalactosucrose (TGS):
Toxicity to aerobic micro-organisms in sewage treatment. Brixham Study no M321/B.
Imperial Chemicals Industries PLC

Imperial Chemicals Industries PLC (1986a). BL/B/2915 - Sucralose: Determination of effects
on the survival and reproduction of Daphnia magna. Brixham Study no P205/C. Imperial
Chemicals Industries PLC

Imperial Chemicals Industries PLC (1986b). BL/B/2897 ­ Sucralose: Determination of
toxicity to green algae Selenastrum capricornutum. Brixham Study no P205/B. Imperial
Chemicals Industries PLC

Imperial Chemicals Industries PLC (1987). BL/B/3015 ­ Sucralose: Determination of
microbial metabolism in water. Brixham Study nos P162/A and P162/C. Imperial Chemicals
Industries PLC

Jenner MR and Smithson A (1989). Physicochemical Properties of the Sweetener Sucralose.
Journal of Food Science, vol 54(6):1646-1649.

Mensink, B. J. W. G. et al. (1995) Manual for summarising and evaluating the environmental
aspects of pesticides, National Institute of Public Health and Environmental Protection,
Bilthoven, The Netherlands. Report no. 679101022.

Nabholz, J. V., Miller, P. and Zeeman, M. (1993). Environmental Risk Assessment of New
Chemicals Under the Toxic Substances Control Act (TSCA) Section Five, in Environmental
Toxicology and Risk Assessment, ASTM STP 1179, Wayne G. Landis, Jane S. Hughes, and
Michael A. Lewis (Eds.), American Society for Testing and Materials, Philadelphia, , pp. 48.

NOHSC (1999) Approved Criteria for Classifying Hazardous                         Substances
[NOHSC:1008(1999)]. Canberra, Australian Government Publishing Service.

NOHSC (1994) National Code of Practice for the Preparation of Material Safety Data Sheets
[NOHSC:2011(1994)]. Canberra, Australian Government Publishing Service.

Tate and Lyle Group Rearch and Development (1983). Effects of pH and Temperature on
                     1,6-dichloro-1,6-dideoxy--D-fructosfuranosyl-4-chloro-4-deoxy--D-
stability     of
galactopyranoside (TGS) in aqueous solution. Tate & Lyle Report No: OFD 26.

TGA (unknown date) Preclinical evaluation of an excipient ­ Sucralose.

USFDA Department of Health and Human Services (1998) Final rule sucralose. 21 CFR Part
172. Volume 63, 16417-16433.




                                                                         10 December, 2001
FULL PUBLIC REPORT
NA/944                                                                              23/24

                                                        Attachment 1

The Draize Scale (Draize, 1959) for evaluation of skin reactions is as follows:

Erythema Formation                             Rating                    Oedema Formation                                  Rating
No erythema                                   0                          No oedema                                      0
Very slight erythema (barely perceptible)     1                          Very slight oedema (barely perceptible)        1
Well-defined erythema                         2                          Slight oedema (edges of area well-defined      2
                                                                         by definite raising
Moderate to severe erythema                   3                          Moderate oedema (raised approx. 1 mm)          3
Severe erythema (beet redness)                4                          Severe oedema (raised more than 1 mm           4
                                                                         and extending beyond area of exposure)


The Draize scale (Draize et al., 1944) for evaluation of eye reactions is as follows:

CORNEA
Opacity                                      Rating                      Area of Cornea involved                       Rating
No opacity                                   0 none                      25% or less (not zero)                        1
Diffuse area, details of iris clearly        1 slight                    25% to 50%                                    2
visible
Easily visible translucent areas, details    2 mild                      50% to 75%                                    3
of iris slightly obscure
Opalescent areas, no details of iris         3                           Greater than 75%                              4
visible, size of pupil barely discernible    moderate
Opaque, iris invisible                       4 severe


CONJUNCTIVAE
Redness                        Rating         Chemosis                     Rating           Discharge                      Rating
Vessels normal                 0 none         No swelling                  0 none           No discharge                   0 none
Vessels definitely                 1          Any swelling above           1 slight         Any amount different           1 slight
injected above normal          slight         normal                                        from normal
More diffuse, deeper           2 mod.         Obvious swelling with        2 mild           Discharge with                 2 mod.
crimson red with                              partial eversion of lids                      moistening of lids and
individual vessels not                                                                      adjacent hairs
                                              Swelling with lids half-
easily discernible                            closed                       3 mod.           Discharge with                 3 severe
Diffuse beefy red              3 severe                                                     moistening of lids and
                                              Swelling with lids half-
                                                                                            hairs and considerable
                                              closed to completely         4 severe
                                                                                            area around eye
                                              closed


IRIS
Values                                                                                                               Rating
Normal                                                                                                               0 none
Folds above normal, congestion, swelling, circumcorneal injection, iris reacts to light                              1 slight
No reaction to light, haemorrhage, gross destruction                                                                 2 severe

Draize, J. H., Woodward, G., Calvery, H. O. (1944) Methods for the Study of Irritation and Toxicity of Substances Applied
Topically to the Skin and Mucous Membranes, J. Pharmacol. Exp. Ther. 82 : 377-390.


Draize J. H. (1959) Appraisal of the Safety of Chemicals in Foods, Drugs and Cosmetics. Association of Food and Drug
Officials of the US, 49 : 2-56.




                                                                                                           Day Month Year
FULL PUBLIC REPORT
NA/944                                                                                                              24/24