BIMAL=20 PHARMA PVT. LTD. MUMBAI , INDIA

THE = INTRODUCTION OF ASPARTAME

A) =20 INTRODUCTION :

B)=20 = THE PROPERTIES=20 :

C) = THE=20 SOLUBILITY AND STABILITY

D)=20 = THE=20 ADVANTAGES

E) THE = APPLICATIONS=20 :

A) =20 INTRODUCTION :

1. = ; =20 Aspartame=20 was an accidental discovery by Mr. James Schlatter, a chemist from the = company,=20

M/s. G.D. = Searle &=20 Company in the year 1965. =

2. = =20 G.D. Searle & Company first patented Aspartame in=20 1970.

3. In March = 1973, M/s.=20 G.D. Searle submitted its first petition to the FDA for Aspartame use &n= bsp; =20

=20 in Foods.

4. = =20 In 1974, FDA approved Aspartame use in Carbonated = Beverages=20 and in Dry Food=20 Products,

in = United States=20 .

5. = Marketing=20 Authorisation was granted for Solid Food in 1981 and, for Soft Drinks in = 1983.

=20 Aspartame was finally authorized as General Sweeteners in=20 1996.

6. Today, it is = an=20 everyday component of most Diet Beverages, Sugar-Free Desserts, and=20

=20 Chewing Gums in countries worldwide.

7. Aspartame has been renamed and is = now being=20 marketed as a Natural =20 Sweetener

=20 (M/s. Ajinomoto, the Maker of Aspartame )=20 (AminoSweet".)

=20 It is also Marketed as Canderel and NutraSweet.

8. =20 Aspartame=20 is used by more than 100 million people around the world and is found = in

=20 more than 6,000 products.

=20 This low-calorie sweetener has been extensively researched and = more than=20 200

=20 studies have been conducted. Aspartame is approved for use in = more than=20 100 countries.

9. It is = 180=20 to 200 times sweeter than Sucrose. (Normal = Sugar).

10. It is digested as a = protein. The=20 components are metabolized normally.

11.=20 = Aspartame=20 is classified as a =93General = Purpose=20 Sweetener=94 by FDA and is approved =

=20 for use in all Foods and Beverages.

B)=20 = THE PROPERTIES=20 :

1. Aspartame=20 is a nutritive sweetener made by joining two Amino Acids=20

=20 (Protein = components) , L- =20 Phenyl Alanine and L- Aspartic Acid, with a third component=20

=20 called a Methyl Ester group.

=20 Very little is needed for a sweet taste, making Aspartame = virtually=20 Non-Caloric.

2.=20 = Aspartame=20 is an odorless, low-calorie intensive sweetener. =

=20 It is chemically pure and contains no additives, preservatives, = or=20 colors.

3. =20 Aspartame=20 has a sugar-like taste.

It=20 enhances some flavors and is appropriate for many applications.=20

When=20 Aspartame is combined with other low-calorie sweeteners, they enhance = each other=20 so

that=20 the combinations are sweeter than the sum of the individual=20 sweeteners.

C) = THE=20 SOLUBILITY AND STABILITY =20

&nbs= p; =20 SOLUBILITY=20 :

=B7 = ; =20 The=20 solubility of Aspartame in Water is dependent on =

pH and =20 Temperature.

pH 2.2 : At this = pH, it=20 is maximum Soluble : 20 mg./ml. at 25=B0C=20

pH 5.2 : At this pH = , it is=20 minimum soluble : 13.5 = mg/ml at=20 25=B0C.

=20 STABILITY=20 :

=B7 =20 The=20 stability of Aspartame is dependent on =20

=20 Time; Temperature; pH=20 and Water activity.

=B7 =20 Aspartame=20 is very stable in the Dry state.

=B7 =20 At=20 105=B0C, a loss of approximately 5% (formation of = diketopiperazine)=20 is observed after &n= bsp; =20 100 hours of treatment.

=B7 =20 At=20 120=B0C, a 50% loss is obtained after 80 hours of treatment.=20

=B7 =20 In=20 solution, when stored at temperatures ranging from 30=B0C to 80=B0C, = Aspartame=20 is &n= bsp; =20 progressively degraded into Diketopiperazine=20 .

=B7 =20 It=20 is therefore not usable in Foods heated at higher temperature (cooking,=20 sterilisation, etc.).

=B7 =20 At=20 Room Temperature, its stability is good at pH values of between 3.4 and = 5.0 and=20 it is =20 maximum at pH 4.3. =

=B7 =20 At=20 pH below 3.4 , the Dipeptide is hydrolysed and at a pH greater than 5.0, = cyclisation occurs = with the=20 formation of Diketopiperazine.

=B7 =20 In=20 both cases, this transformation results in the loss of=20 sweetness.

=B7 =20 In=20 foods with a low or moderate water content (water activities between = 0.34 and=20 0.66), &n= bsp; =20 the maximum = stability is=20 observed at pH 5.0.

=B7 =20 Aspartame=20 has good stability in deep frozen products. =

=B7 =20 Its=20 main impurity (approximately 2%) is Diketopiperazine,=20 a degradation product of aspartame =20 which has no sweetening properties.

D)=20 = THE=20 ADVANTAGES

Aspartame=20 is a Low-Calorie sweetener which is approximately 200 times Sweeter than Sucrose =20 (Normal Sugar) .

The=20 rapid rise in Aspartame's popularity can be attributed to the many = Benefits=20 (Advantages ) that Aspartame provides to Calorie-Conscious consumers,=20 including:

=B7 =20 Aspartame=20 Tastes Like Sugar

=B7 =20 Aspartame=20 Enhances and Extends Flavors

=B7 =20 Aspartame=20 Does Not Promote Tooth Decay

=B7 =20 Aspartame=20 is Helpful for Individuals with Diabetes

=B7 =20 Scientific=20 Studies Show Aspartame is Beneficial in Weight=20 Control

=B7 =20 Aspartame=20 Can Be Part of a Healthful Diet. =B7 =20 More=20 benefits : =20

Low-calorie=20 sweeteners provide consumers with many benefits, both psychological and = physiological.=20

Health=20 professionals and consumers believe low-calorie sweeteners are effective = for the=20 following purposes: Weight maintenance, Weight reduction, Management of=20 diabetes, Reduction of dental =20 caries, and Reduction in the risks associated with=20 obesity.

E) THE = APPLICATIONS=20 :

1. =20 Aspartame=20 has established itself as an important component in many Low- calorie, Sugar-free =20 Foods and Beverages and is primarily responsible for the growth = over the=20 last two decades in the = Sugar-Free=20 Market.

2.=20 = Currently,=20 aspartame is consumed by over 200 million people around the world and is found in = more than 6,000 = products=20 including carbonated soft drinks, powdered soft drinks, chewing gum,=20 confections, gelatins, dessert mixes, puddings and fillings, frozen = desserts,=20 yogurt, tabletop sweeteners, and some pharmaceuticals such as vitamins = and=20 sugar-free cough drops.

3.=20 = The safety=20 of aspartame has been affirmed by the U.S. FDA, 26 times in the = past 23=20 years.

4. = Aspartame is used in the manufacture of = many=20 Sugar-free, low calorie and dietary products, &n= bsp; =20 such as:

=B7 =20 Beverages:=20 Carbonated and still Soft Drinks, Fruit-Juices and Fruit Syrups.=20

=B7 =20 Table-top:=20 Compressed=20 Sweeteners, Powdered Sweeteners (spoon-for-spoon), &n= bsp; =20 Sweetener Sachets and Liquid table-top Sweeteners.=20

=B7 =20 Dry=20 mixes: Hot=20 and Cold Chocolate and Beverage Mixes and Instant Desserts.=20

=B7 =20 Dairy:=20 Yoghurt,=20 Frozen Novelties and Desserts.

=B7 =20 Confectionery:=20 Chewing=20 Gum, Boiled Sweets, Pastilles, Mints, Chocolate, Gums and Jellies.=20

=B7 =20 Pharmaceutical:=20 Tablets,=20 Sugar-Free Syrups, Powdered Mixes and Effervescent=20 Tablets.

5. =20 The=20 Following Reduced Calorie Products Have Aspartame-Sweetened=20 Choices

=B7 =20 Breath=20 Mints

=B7 =20 Carbonated=20 Soft Drinks

=B7 =20 Cereals=20

=B7 =20 Chewing=20 Gum

=B7 =20 Flavored=20 Syrups for Coffee

=B7 =20 Flavored=20 Water Products

=B7 =20 Frozen=20 Ice

=B7 =20 Frozen=20 Ice Cream Novelties

=B7 =20 Fruit=20 Spreads

=B7 =20 Gelatin,=20 Sugar Free

=B7 =20 Hard=20 Candies

=B7 =20 Ice=20 cream Toppings

=B7 =20 Ice=20 Creams, No Sugar Added or Sugar Free

=B7 =20 Iced=20 Tea, Powder

=B7 =20 Iced=20 Tea, Ready to Drink

=B7 =20 Instant=20 Cocoa Mix

=B7 =20 Jams=20 & Jellies

=B7 =20 Juice=20 Blends

=B7 =20 Juice=20 Drinks

=B7 =20 Maple=20 Syrups

=B7 =20 Meal=20 Replacements

=B7 =20 Mousse=20

=B7 =20 No=20 Sugar Added Pies

=B7 =20 Non-Carbonated=20 Diet Soft drinks

=B7 =20 Nutritional=20 Bars

=B7 =20 Powdered=20 Soft Drinks

=B7 =20 Protein=20 Nutritional Drinks

=B7 =20 Pudding=20

=B7 =20 Soft=20 Candy Chews

=B7 =20 Sugar=20 Free Chocolate Syrup

=B7 =20 Sugar=20 Free Cookies

=B7 =20 Sugar=20 Free Ketchup

=B7 =20 Table=20 Top Sweeteners

=B7 =20 Vegetable=20 Drinks

=B7 =20 Yogurt,=20 Drinkable

=B7 =20 Yogurt,=20 Fat Free

=B7 =20 Yogurt,=20 Sugar Free

6. = Recently,=20 researchers have found possible Medical uses for Aspartame. In 1998, researchers=20 =20 at the Oklahoma Medical Research Foundation found that Aspartame = could be=20 used as a Pain- Reliever, Anticoagulant, and Fever-Reducer much like a=20 Non-Steroidal Anti-Inflammatory drug such as=20 Aspirin.