Retarded release forms of indomethacin and niomethacin - allow oral administration once daily and avoid sec. stomach effects, as antiinflammatories for rheumatism, arthritis etc.

摘要

Prepn. of retarded release indomethacin or niomethacin prepn. by intimately mixing the powdered octive cpd. with (a) one or more physiologically harmless substances which, in aqueous medium at pH 1-9 and at 37 deg. C, have a solubility of at least 1g/10 ml, e.g. lactose, saccharose, fructose, sorbitol, mannitol and xylitol (component A) and b) one or more physiologically harmless substances which, in aqueous medium at pH 1-9 and at 37 deg. C, have a solubility of at least 1g/100 ml, such as methylcellulose, hydroxypropyl-methyl-cellulose, hydroxyethylcellulose, hydroxy-methylcellulose, methyl-hydroxy-ethyl-cellulose and ethythydroxyethylcellulose (component B) and c) addition to the above mixture of a solution of one or more physiologically harmless substances (which in aqueous medium 1-) at pH 1-9 and at 37 deg. C, have a solubility of less than 1g/1000 mol, such as ethylcellulose carnauba wax and E-pharma hard wax (Hoschst) or 2) at pH 1 and at 37 deg. C, have a solubility of less than 1g/1000 ml, such as cellulose acetyl-phthalate, cellulose phthalate, cellulose acetyl-succinate on carboxymethylcellulose (component C)) in an organic solvent (opt.-contg. water) to form a workable paste, which is subjected to a pressure of at least 2 bar, and is granulated, opt. during the pressure treatment; the granules are dired and converted to known dosage forms (tablets, dragees, capsules etc.), opt. with addition of known adjuvants.