Micro:granules contg. beta-histine - for controlled release and less side effects useful in treating Menieres syndrome

摘要

Microgranules for pharmaceutical use contain (1) a neutral inert core made from =2 of sucrose, starch, talc, dessicating silica, lactose and stearic acid; (2) a first layer contg. betahistine of formula (I) or its deriv. esp. the hydrochloride or methane sulphonate; and (3) a microporous coating contg. =1 natural or synthetic polymer selected from gum lac, gum arabic, gelatine, ethyl cellulose, cellulose acetophthalate, cellulose triacetate, polyxyethylene glycol, methacrylates, styrene-acrylonitrile copolymer and PVP. (I) is useful in treating disorders of intra-labyrinthine, cochlear, or vestibular pressure or microcirculation, esp. Meniere's syndrome. The microcapsules give a controlled release of (I) free from side-effects such as nausea. They may be formulated into capsules, tablets, suppositories, syrups, granules or powder, which is not always possible with (I) alone, due to its hygroscopic nature.