method for the preparation of peroraal should active preparations prolonged therapeutic effect, and the resulting shaped preparations.

摘要

Prolonged acting pharmaceutical preparations are prepared by a process which comprises embedding a solid pharmacologically active material having a selected, substantially uniform particle size in a cohesive matrix by intimately mixing said active material with (a) a substance which is inert and insoluble in gastro-intestinal fluids, e.g. CaSO4. 1/2 H2O, Ca3(PO4)2 or Florite, (b) a substance selected from the group consisting of fats and waxes which are solid at body temperature and non-hydrophilic salts of alkaline earth metals and aluminium, and (c) a binding and/or swelling agent, all of which said ingredients (a) to (c) are solids and have the same substantially uniform particle size as the said active material, then adding a granulating agent and, if the ingredients (a) to (c) are not inherently cohesive, an adhesive agent, granulating and, if desired, compressing to form tablets. Before being embedded in the matrix, the active material may first be admixed with a solid material which is soluble in gastrointestinal fluids, for example, NaCl, Na2HPO4 or a sugar, e.g. glucose. Suitable matrix ingredients (b) are the stearates and palmitates of calcium, magnesium and aluminium. The binding or swelling agent may be selected from methyl and ethyl cellulose, polyvinyl acetate, polyvinyl pyrrolidone, cellulose acetate and p prolamines such as zein, kafirin, hordein and gliadin. Water may be used as granulating agent and, where an adhesive agent is also employed, this may be added as a solution in a liquid granulating agent, e.g. solutions of colophonium in alcohol, polyvinyl pyrrolidone or polyethylene glycol. Examples describe preparations containing as active ingredient (a) orphenadrine, (b) orphenadrine citrate, (c) physostigmine salicylate and (d) ephedrine hydrochloride.