| 摘要 |
Solid sustained release diuretic and saliuretic compositions comprise an orally active diuretic and saliuretic 1,2,4 - benzothiadiazine - 1,1 - dioxide and a therapeutically acceptable K salt together with a fatty substance and alginic acid. Preferred 1,2,4 - benzothiadiazine - 1,1 - dioxides are 6 - chloro - or 6 - trifluoromethyl - 7 - sulphamoyl - 3,4 - dihydro - 1,2,4 - benzothiadiazine - 1,1 - dioxide and their 3 - n - butyl, 3 - iso - butyl, 3 - (2 - methylpropyl), 3 - (2 - ethyl-mercaptoethyl), 3 - benzylmercaptomethyl, 3 - dichloromethyl, 3 - benzyl, 3 - a - methyl benzyl, 3 - (2 - phenylethyl), 3 - cyclopentyl, 3 - cyclohexyl, 3 - (3 - cyclohexenyl), 3 - cyclopropyl, 3 - cyclobutyl, 3 - cyclopentylmethyl, 3 - cyclohexylmethyl, 3 - (2 - cyclopentylethyl), 3 - (1 - cyclopentylethyl), 3 - (5 - norbornen - 2 - yl), 3 - (9 - fluorenyl), 3 - thenyl, 2 - ethyl, 2 - allyl, 2 - n - propyl, 2 - benzyl, 2 - (2 - tetrahydropyranyl), 2 - methyl - 3 - chloromethyl, 2 - methyl - 3 - (2,2,2 - trifluoroethylmercaptomethyl), 2 - ethyl - 3 - dichloromethyl, 2 - benzyl - 3 - chloromethyl, or 2,7-bis - n - butylcarbamyl - 3 - chloromethyl derivatives. Preferred K salts include Kcl, K2HPO4, dipotassium tartrate and tri potassium citrate. Specified fatty substances include vegetable fats, fatty acids, and alkaline earth metal salts thereof, fatty alcohols, and esters thereof, fatty amides, waxes, both natural and synthetic, and resin-wax mixtures, e.g. polyethylene and cellulose ether-wax mixtures. The compositions may be prepared in the form of tablets by mixing the active ingredients and appropriate carriers, adding a granulating liquid to form a granulate, and compressing the latter into tablet form. The granulating liquid is preferably a solution of a film-forming agent which is capable of forming an acid-fast, alkali-soluble film, e.g. an acidic cellulose ester such as cellulose acetate phthalate, or a salt of carboxymethyl cellulose or alginic acid. The compositions may include dyestuffs, preserving, stabilising and wetting agents, and other therapeutically active substances, e.g. hypotensive agents such as Ranwolfia and related alkaloids, e.g. reserpine, deserpidine, rescinnamine, or syrosingopine, hydrazino - phthalazines, e.g. 1 - hydrazino- or 1,4-di-hydrazino phthalazine, guanidine compounds, e.g. guanethidine spirolactones, e.g. spironolactone, barbiturates, e.g. sodium 5-sec-butyl 5-ethyl barbiturate, purines, e.g. theobromine or the choline salt of theopylline, protoveratrines, e.g. protoveratrine A, veratrum viride tannate, or 2-methyl-2-propyl-1,3-propanediol dicarbamate. |
