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卡托普利是一种血管紧张素转化酶抑制剂,常用于口服降血压,疗效良好。但有两个缺点,一是单剂量口服作用持续约6～8小时,因而临床每天需服3次,二是与食物同用,生物利用度显著降低,研究表明在高pH值中迅速降解是其主要原因。本文设计二种新制剂,一是尽可能延长保留在胃肠道近端的漂浮胶囊,二是生物粘附片。各设计了7种处方,前者用不同配比的羟丙基甲基纤维素(Methocel K4M及K15M)、乳糖、微晶纤维素及少量硬脂酸镁,过筛混匀,装入胶囊而成。后者用缓释型丙烯酸树脂Eudrgit RS 100或乙基纤维素作阻滞剂,以聚羟乙烯Carbopol 9349或丙烯酸与丙烯
Captopril is an angiotensin converting enzyme inhibitor, commonly used in oral antihypertensive, good effect. However, there are two disadvantages. First, oral administration of a single dose lasts for about 6 to 8 hours. Therefore, it is required to take 3 times a day in clinical practice. Second, with food, the bioavailability is significantly reduced. Studies have shown that rapid degradation in high pH is The main reason. This article designs two kinds of new preparations, one is to extend as far as possible to retain the floating capsule in the proximal gastrointestinal tract, the second is the bioadhesive sheet. The design of the seven kinds of prescriptions, the former with different proportions of hydroxypropyl methyl cellulose (Methocel K4M and K15M), lactose, microcrystalline cellulose and a small amount of magnesium stearate, sifted through the screen, into the capsule . The latter with a sustained-release acrylic resin Eudrgit RS 100 or ethyl cellulose as a retarder to polyethylene glycol Carbopol 9349 or acrylic acid and propylene