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敏乐啶属于外周血管扩张药,通常口服治疗重度高血压,外用可治疗男性型秃发。据报道,本品口服吸收迅速,48小时内经尿液排泄95%,其中约20%以原形排泄,其余为多个代谢物。本品局部给药吸收率很低,尿药回收量仅为给药剂量的3%不到。本文对敏乐啶局部给药的限速过程作了研究,其目的是为寻找释放度良好的外用制剂提供依据。试验采取随机、交叉方案,将22例患有男型秃发的成年男性健康志愿者按药物和表皮接触时间1、2、4和11.5小时分为4组,每隔12小时给予2%敏乐啶外用液(溶媒中乙醇:水:丙二醇体积比为6∶2∶2)1.0 ml,均匀
Minoxidil is a peripheral vasodilator, usually oral treatment of severe hypertension, topical treatment of male alopecia. It is reported that oral absorption of this product rapidly, within 48 hours by the urine excretion of 95%, of which about 20% of the prototype excretion, the rest of multiple metabolites. This product is very low absorption rate of local administration, urine drug recovery is only less than 3% of the dose. In this paper, the rate-limiting process of minoxidil topical administration was studied, the purpose of which is to provide a basis for finding a good topical formulation for release. Twenty-two adult male healthy volunteers with alopecia areata were randomly divided into four groups according to drug-epidermal exposure time of 1, 2, 4 and 11.5 hours, and 2% of them were given every 12 hours External use of liquid (solvent ethanol: water: propylene glycol volume ratio of 6: 2: 2) 1.0 ml, uniform