The Upjohn Co.

Pharmacia & Upjohn Company

Dae Y Cha

Verlan H Van Rheenen

The present invention provides for an improvement in the emulsion copolymerization process for the preparation of fine-beaded colestipol hydrochloride (FBCH) wherein the improvement comprises: 1) utilizing a weight ratio of water to polyethylenepolyamine in the process of 1.8 to 3.6 grams per gram, and 2) utilizing a weight ratio of surface active agent or surfactant to polyethylenepolyamine in the process of 1.0 to 3.0 grams per kilogram. The colestipol hydrochloride product thus produced is a novel fine-beaded form of a known pharmaceutical composition, yielding pharmaceutically elegant dosage forms exhibiting increased potency, including non-gritty oral powders and oral tablets. Conventional colestipol hydrochloride was heretofore available in large spherical granules which produced less elegant (gritty) oral suspensions.

Fine-beaded colestipol hydrochloride and pharmaceutically elegant dosage

Oxymercuration reaction products (I) and/or mercury contaminated steroids (I) are purified by dissolving the compound in a suitable solvent and contacting with a metal dust selected from zinc, copper or iron and a suitable acid.

Mercury removal process

The process of the present invention uses an amine to prepare monolithium acetylide which is sufficiently stable at up to 0.degree. and yet is sufficiently reactive to react with 16-substituted-17-keto steroids producing the useful 17.alpha.-ethynyl-17.beta.-hydroxy-16-substituted steroids.

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Kalamazoo, MI, United States of America

Dae Y Cha