Preparation of aqueous clear solution dosage forms with bile acids

Abstract

Compositions for pharmaceutical and other uses comprising clear aqueous solutions of bile acids which do not form any detectable precipitates over selected ranges of pH values of the aqueous solution and methods of making such solutions. The compositions of the invention comprise water; a bile acid in the form of a bile acid, bile acid salt, or a bile acid conjugated with an amine by an amide linkage; and either or both an aqueous soluble starch conversion product and a aqueous soluble non-starch polysaccharide. The composition remains in solution without forming a precipitate over a range of pH values and, according to one embodiment, remains in solution for all pH values obtainable in an aqueous system. The composition, according to some embodiments, may further contain a pharmaceutical compound in a pharmaceutically effective amount. Non-limiting examples of pharmaceutical compounds include insulin, heparin, bismuth compounds, amantadine and rimantadine.

Description

Background of the invention [0001] Bile salts are organic acids derived from cholesterol, which are natural ionic detergents and play key roles in the absorption, transport and secretion of lipids. In bile acid chemistry, the steroid nucleus of bile salts has a hydrocyclopentaphenanthrene nucleus common to all perhydrosteroid compounds. Distinguishing features of bile acids include a saturated 19-carbon steroid nucleus, a beta hydrogen at the 5-position, a saturated branched 5-carbon side chain terminating in a carboxylic acid, and an alpha hydroxyl at the 3-position. The only substituent present in most natural bile acids is the hydroxyl group. In most mammals, the hydroxyl group is at the 3, 6, 7 or 12 position. [0002] General bile acids differ mainly in the number of hydroxyl groups on the sterol ring and the nuclear orientation. The term primary bile acids refers to bile acids de novo synthesized by the liver. In humans, primary bile acids include cholic acid (3α, 7α...

AI Technical Summary

Problems solved by technology

[0032] Drug delivery systems involving bile acids can provide liver-specific drug targeting, an important direction for drug development, as standard pharmacological approaches to treating liver disease have suffered from insufficient delivery of active agents into liver cells , and nonspecific toxicity to other organs

Unfortunately, bismuth concentrations in mucus are often lower than the average inhibitory effect of H. concentration

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