Friday, July 23, 2021

Sweetening Agents Used In Oral Pharmaceutical Suspensions

by | October 3, 2020 0

Sweetening agents are excipients often added to pharmaceutical dosage forms to mask bitter taste of the partially dissolved drug and to improve palatability in general. Traditionally, oral formulations were sweetened using concentrated sucrose solution (syrup) or honey (contains fructose). However, these materials are inadequate for the formulation of many products because they simply are not able to adequately mask the unpleasant taste of many pharmaceutical materials, including Active Pharmaceutical Ingredients (APIs) and excipients. In addition, the large quantities of both sucrose and fructose required increased the dietary carbohydrate intake, particularly when consumed as soft drinks. There have been campaigns over the years to persuade people to eat and drink more healthily, and to cut down on carbohydrates.

Several alternative sweeteners have been developed over the years to better mask unpleasant tastes in both processed foods and pharmaceuticals. They are also used in low-calorie foods and soft drinks.

Several of the commonly used sweetening agents are ionic and have the potential to interact with other components of the suspension. Some sweetening agents are more stable than others in aqueous solution. These will be important factors in the final selection of the sweetening agent.

This article provides a comprehensive list of sweetening agents used in oral pharmaceutical suspensions. The regulatory position for the different sweetening agents varies with country and/or region.

The use of artificial sweetening agents in pediatric oral medicines is under active debate. However, the use of sucrose (“sugar”) is also under a cloud because of its cariogenic potential and potential interference with diabetic glucose control.

Sweetening agents used in oral pharmaceutical suspensions include:

1. Acesulfame K

Acesulfame potassium occurs as a colorless to white-colored, odorless, crystalline powder with an intensely sweet taste. The approximate sweetening power is 180 – 200 times that of sucrose, similar to aspartame, about one-third as sweet as sucralose, one-half as sweet as sodium saccharin, and about 4-5 times sweeter than sodium cyclamate.

Comments

  • Stable in acid pH.
  • Stable in solution at pH 3 – 3.5.
  • Included in the Inactive Ingredient Database, and permitted in certain foods in the US

2. Alitame

Alitame is an intense sweetening agent developed in the early 1980s. It is an odorless (or having a slight characteristic odor) white nonhygroscopic crystalline powder.

Alitame is approximately 2000 times sweeter than sucrose. It has an insignificant energy contribution of 6 kJ (1.4 kcal) per gram of alitame.

Comments

  • Not approved for use in pharmaceuticals in the US or Europe.
  • Unstable at low pH, more stable at higher pH.
  • Almost non-nutritive

3. Aspartame

Aspartame occurs as an off white, almost odorless crystalline powder with an intensely sweet taste. It enhances flavor systems and can be used to mask some bitter taste of partially dissolved drug substances.

Aspartame is approximately 180 – 200 times sweeter than sucrose. Unlike some other intense sweeteners, aspartame is metabolized in the body and consequently has some nutritive value: 1 g provides approximately 17 kJ (4 kcal).

In practice, the small quantity of aspartame consumed provides a minimal nutritive effect.

Comments

  • Unstable in the presence of moisture.
  • Optimal stability at pH 4.5; unstable to either acid or base.
  • GRAS (Generally Recognized as Safe) listed and recognized as a food additive in Europe.
  • Included in the Inactive Ingredient Database

4. Dextrose

Dextrose (BP: Glucose, JP: Glucose, PhEur: Glucose Monohydrate, USP: Dextrose) occurs as odorless, sweet-tasting, colorless crystals, or as a white crystalline or granular powder. It includes a range of very similar materials such as dextrates and high DE (dextrose equivalents) corn syrup.

Dextrose is approximately 0.5 times as sweet as sucrose.

Comments

  • Reducing sugar
  • Cariogenic
  • Included in the Inactive Ingredient Database

Read Also: Preservatives Used In Pharmaceutical Suspensions: Typical Use Levels and Comments

5. Fructose

Fructose occurs as odorless, colorless crystals, or a white crystalline powder with a very sweet taste. It is approximately 1.7 times sweeter than sucrose.

Comments

  • The sweetest tasting of the natural sugars.
  • Most stable at pH 3 – 4.
  • Included in the Inactive Ingredient Database.
  • Cariogenic

6. Galactose

Galactose sometimes abbreviated Gal, is a monosaccharide sugar that is similar to glucose in its structure, differing only in the position of one hydroxyl group. Galactose is about 0.3 – 0.5 times as sweet as sucrose.

Comments

  • Monographs in NF 25 and Ph.Eur 5.5

7. Inulin

Inulin occurs as an odorless white powder with a neutral to slightly sweet taste (about 0.1 times as sweet as sucrose).

Comments

  • GRAS listed.
  • Non-caloric.
  • Suitable for use by diabetic patients.
  • Natural material of plant origin.
  • Oligofructan

8. Isomalt

Isomalt is a sugar alcohol (polyol) that occurs as a white or almost white powder or granular or crystalline substance. It has a pleasant sugarlike taste with a mild sweetness approximately 50 – 60 % (0.5 – 0.6 times) of that of sucrose.

Comments

  • Sugar alcohol (polyol).
  • GRAS listed and recognized as a food additive in Europe.
  • Noncariogenic

9. Lactitol

Lactitol occurs as an odorless white orthorhombic crystal with a sweet taste that imparts a cooling sensation. It is available in powdered form and in a range of crystal sizes. The directly compressible form is a water-granulated product of microcrystalline aggregates.

Lactitol is used as a noncariogenic replacement for sucrose. It is about 0.3 times as sweet as sucrose.

Comments

  • GRAS listed and recognized as a food additive in Europe

10. Maltitol

Maltitol is a disaccharide consisting of one glucose unit linked with one sorbitol unit via an α-(1- 4) bond. It occurs as a white, odorless, sweet, anhydrous crystalline powder. The crystal structure is orthorhombic.

Maltitol is approximately as sweet as sucrose.

Comments

  • Noncariogenic sugar alcohol.
  • GRAS listed and recognized as a food additive in Europe.
  • Heat stable

11. Maltose

Maltose occurs as white crystals or as a crystalline powder. It is odorless and has a sweet taste approximately 30%  (0.3 times) that of sucrose.

Comments

  • .Recognized as a food in the US, and not subject to GRAS or Food Additive regulations

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