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Sweetening Agents Used In Oral Pharmaceutical Suspensions

by | October 3, 2020 0

12. Mannitol

Mannitol (D-mannitol) is a hexahydric alcohol related to mannose and is isomeric with sorbitol. It occurs as a white, odorless, crystalline powder, or free-flowing granules.

Mannitol has a sweet taste, approximately as sweet as glucose and half as sweet as sucrose, and imparts a cooling sensation in the mouth.

Comments

  • GRAS listed and recognized as a food additive in Europe.
  • Included in the Inactive Ingredient Database.
  • Negative heat of solution

13. Neohesperidin dihydrochalcone

Neohesperidin dihydrochalcone occurs as a white or yellowish-white powder with an intensely sweet taste. It is a synthetic intense sweetening agent approximately 1500 – 1800 times sweeter than sucrose and 20 times sweeter than saccharin.

Structurally it is an analog of neohesperidin, a flavanone that occurs naturally in Seville oranges (Citrus aurantium).

Comments

  • GRAS listed and recognized as a food additive in Europe.
  • Limited solution stability; optimum pH 2 – 6.

14. Saccharin

Saccharin occurs as odorless white crystals or a white crystalline powder. It has an intensely sweet taste, with a metallic or bitter aftertaste that at normal levels of use can be detected by approximately 25% of users. The aftertaste can be masked by blending saccharin with other sweeteners.

The sweetening power of saccharin is approximately 300 – 600 times that of sucrose.

Comments

  • Commonly used as the sodium salt
  • Recognized as a food additive in Europe.
  • Included in the Inactive Ingredient Database.

15. Sodium cyclamate

Sodium cyclamate occurs as white, odorless or almost odorless crystals, or as a crystalline powder with an intensely sweet taste. In dilute solution, up to about 0.17% w/v, the sweetening power is approximately 30 times that of sucrose.

However, at higher concentrations, this is reduced and at a concentration of 0.5% w/v a bitter taste becomes noticeable.

Comments

  • Recognized as a food additive in Europe.
  • Included in the Inactive Ingredient Database.
  • Formerly under suspicion as a carcinogen, but study design questionable and results not confirmed

16. Sorbitol

Sorbitol (D-glucitol) is a hexahydric alcohol related to mannose and is isomeric with mannitol. It occurs as an odorless, white or almost colorless, crystalline, hygroscopic powder. Sorbitol has approximately 50 – 60% (0.5 – 0.6 times) of the sweetness of sucrose.

Comments

  • Hydrogenated sugar; non-cariogenic.
  • GRAS listed and recognized as a food additive in Europe.
  • Included in the Inactive Ingredient Database.
  • Reacts with iron oxide leading to discoloration

17. Sucralose

Sucralose is a white to off-white colored, free-flowing, crystalline powder. It has a sweetening power approximately 300 – 1000 times that of sucrose and has no aftertaste.

Sucralose has no nutritional value, is non-cariogenic, does not promote dental caries, and produces no glycemic response.

Comments

  • GRAS listed and approved for food use in the UK.
  • Included in the Inactive Ingredient Database.
  • Stable above pH 3; optimally pH 5–6.

Read Also: Surface Active Agents (Surfactants) Used in Pharmaceutical Suspensions

18. Sucrose

Sucrose is a sugar obtained from sugar cane (Saccharum officinarum Linne´ (Fam. Gramineae)), sugar beet (Beta vulgaris Linne´ (Fam. Chenopodiaceae)), and other sources. It occurs as colorless crystals, as crystalline masses or blocks, or as a white crystalline powder. It is odorless and has a sweet taste.

Sucrose is the standard sweetener to which all other sweeteners are compared. For this purpose, the relative sweetness of sucrose is set to 1.

Comments

  • Cariogenic
  • Will show the reactions of a reducing sugar due to traces of “invert sugar”

19. Tagatose

Tagatose is a white, anhydrous crystalline solid. It is a carbohydrate, a ketohexose, an epimer of D-fructose inverted at C – 4. It can exist in several tautomeric forms.

A 10% solution of tagatose is about 92% (0.9 times) as sweet as a 10% sucrose solution. It is a low-calorie sugar with approximately 38% of the calories of sucrose per gram.

Comments

  • Prepared from d-galactose by isomerization under alkaline conditions

20. Thaumatin

Thaumatin occurs as a pale-brown colored, odorless, hygroscopic powder with an intensely sweet taste. It is a naturally occurring intense sweetening agent approximately 2000 – 3000 times as sweet as sucrose.

Thaumatin has a delayed-onset taste profile and long (up to one hour) licorice-like aftertaste.

Comments

  • A structure of five related proteins stabilized by disulfide cross-link.
  • Disulfide link cleavage destroys sweetness.
  • Synergies with other sweetening agents.
  • Used in foods and pharmaceutical products.
  • GRAS listed and accepted as a food additive in Europe

21. Trehalose

Trehalose occurs as virtually odorless, white, or almost white crystals with a sweet taste approximately 45% (0.45 times) of the sweetness of sucrose.

Comments

  • GRAS listed.
  • May be used in some food applications in the UK.
  • Mainly used as a lyoprotectant in the formulation of therapeutic proteins.
  • Also used in topical products and cosmetics

22. Xylitol

Xylitol occurs as a white, granular solid, comprising crystalline, equidimensional particles having a mean diameter of about 0.4 – 0.6 mm. It is odorless, with a sweet taste that imparts a cooling sensation. Xylitol is also commercially available in powdered form, and several granular, directly compressible forms.

Xylitol has equal sweetness intensity to sucrose, combined with a distinct cooling effect upon dissolution of the crystal.

 Comments

  • Hydrogenated sugar; non-cariogenic.
  • GRAS listed and recognized as a food additive in Europe.
  • Included in the Inactive Ingredient Database.
  • negative heat of solution

References

  • Kulshreshtha A., Singh O. and Wall M. (2010). Pharmaceutical Suspensions: From Formulation Development to Manufacturing.London, New York, Dordrecht Heidelberg: Springer.
  • Rowa R., Sheskey P. and Quinn M. (2009). Handbook of Pharmaceutical Excipients. USA: Pharmaceutical Press and American Pharmacists Association.

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