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为了避免口服避孕对胃肠道刺激性,本文设计制备了避孕乳膏,试图使药物经皮吸收进入体内发挥其避孕作用。通过物理稳定性试验筛选了避孕乳膏基质。用同位素示踪技术和体外流通扩散室研究了炔雌醇和十八甲基炔诺酮的化学结构类似物~3H-雌二醇和~3H-孕酮从避孕乳膏中释药透皮百分率及小鼠体内透皮吸收过程。体外试验结果表明:不同乳膏处方内标记药物的释药透皮百分率不同,水包油型基质释药透皮速度较有规律。处方3,7在8h内分别可释药52%和41.6%。体内试验结果表明:避孕乳膏中药物透皮吸收速度比口服快,透皮吸收峰时为1h,口服吸收峰时为2h。由于小鼠给药时涂布面积较小,透皮吸收程度较差。避孕乳膏对动物皮肤无刺激性。
In order to avoid oral contraceptive gastrointestinal irritation, this article designed and prepared a contraceptive cream, trying to make the drug transdermal absorption into the body to play its role in contraception. Contraceptive cream bases were screened by physical stability test. The chemical structure of ethinylestradiol and eighteen norgestrel ~ 3H-estradiol and ~ 3H-progesterone were studied for the percentage of transdermal drug release from the contraceptive cream and isotope tracer Transdermal absorption in mice. The results of in vitro tests showed that the percentages of transdermal drug delivery in different cream prescriptions were different, and the transdermal delivery rate of oil-in-water matrix was regular. Prescription 3,7 were released in 52h and 41.6% respectively within 8h. In vivo test results showed that the transdermal absorption rate of the contraceptive cream was faster than that of oral administration, 1 h when the transdermal absorption peak and 2 h when the oral absorption peak was obtained. Due to the smaller area of administration when administered to mice, the degree of transdermal absorption was poor. Contraceptive cream is non-irritating to animal skin.