SIBUTRAMINE COMPOSITION OF THE POWDERS AND GRANULES TYPE HAVING IMPROVED SOLUBILITY, ITS PHARMACEUTICAL PREPARATION AND METHOD

摘要

A powder and granule type composition comprising sibutramine having improved solubility is provided to improve formulation efficiency of sibutramine by overcoming sibutramine problems of pH dependency, water-insolubility and oil state through formulation into powder and granule. And a preparation method thereof is provided to simplify the production process and reduce the production costs by eliminating a process for preparing acid addition salts of sibutramine from sibutramine. A powder and granule type composition having improved solubility comprises 1 part by weight of sibutramine, 0.1-2 parts by weight of hydroxypropylmethyl cellulose, 0.1-2 parts by weight of water-soluble sugars and 0.1-2 parts by weight of organic acid, wherein the water-soluble sugars include lactose, sucrose, glucose, mannitol, xylitol, sorbitol and fructose, and the organic acid is citric acid, stannic acid, ascorbic acid, lactic acid, succinic acid, malic acid or tartaric acid. The method for preparing the powder and granule type composition having improved solubility comprises the steps of: (a) solubilizing 1 part by weight of sibutramine and 0.1-2 parts by weight of hydroxypropylmethyl cellulose in organic solvent; (b) dissolving 0.1-2 parts by weight of water-soluble sugars and 0.1-2 parts by weight of organic acid in water, and mixing with the solution of step (a); and (c) granulating the mixture solution of step (b) with solvent evaporation or fluidized bed granulation. The pharmaceutical preparation comprises the powder and granule type composition comprising the sibutramine, and pharmaceutically acceptable excipients or supplements and has a formulation of capsule or tablet.