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:
Contents
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.
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.
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.
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.
Read Also: Preservatives Used In Pharmaceutical Suspensions: Typical Use Levels and Comments
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.
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.
Inulin occurs as an odorless white powder with a neutral to slightly sweet taste (about 0.1 times as sweet as sucrose).
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.
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.
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.
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.
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