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吡喹酮凝胶剂的研制 被引量:10

PREPARATION OF PRAZIQUANTEL HYDROGEL
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摘要 绘制了吡喹酮在丙二醇-乙醇-水系统中的相图,通过均匀设计确定了1%吡喹酮凝胶剂中各溶媒所占的最佳比例为:40%(w/w)丙二醇,45%(w/w)乙醇,5%(w/w)水。以卡波普940为基质制备了吡喹酮凝胶剂,考察了其体外经皮渗透性、月桂氮酮的促渗作用以及其体外释放。结果表明吡喹酮凝胶剂的体外经皮渗透为零级过程,皮肤为其经皮渗透的限速屏障,月桂氮酮能有效促进其体外经皮渗透,其体外释放符合Higuchi方程。 The solution phase diagram of praziquantel (1) was made using tricomponent solvent system, and the optimum percentage of each solvent in the 1% 1 hydrogel formulation was determined by uniform design:40% w/w of propylene glycol, 45% w/w of alcohol and 5% w/w of water. Hydrogel formulations were prepared by gelling the optimum solvent mixture with Carbopol 940. The percutaneous penetration of 1 hydrogel through excised mouse skin, the enhancement of laurocapram and release of it through cellophane were observed. It was found that percutaneous penetration of 1 hydrogel in vitro followed zeroorder kinetics, skin was the main barrier, laurocapram could effectively enhance the permeability, and release of 1 through cellophane was well described by the Higuchi's model.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 1998年第4期161-164,共4页 Chinese Journal of Pharmaceuticals
关键词 吡喹酮 凝胶剂 月桂氮ZHUO酮 抗蠕虫药 solution phase diagram, praziquantel, hydrogel, laurocapram
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