避孕乳膏的制备及透皮吸收研究

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。

STUDY OF PREPARATION ON CONTRACEPTIVE CREAM AND ITS PERCUTANEOUS ABSORPTION

The preparation of cream containing contraceptives was observed. The accumulative release percentage from cream bases and their percutaneous absorption in mice were investigated by using ~3H-progesterone and ~3Hestradiol which are the analogues of norethisterone and ethylestrenol. Results of in vitro were that the rate of percutaneous release percentage varied with different cream bases and the formulation 3 and 7 released 52% and 41.6% within 8 hours, respectively. Results of in vivo showed that the rate of percutaneous absorption was faster than that of oral. The T_pof percutaneous absorption was at 1 h and that of oral absorption was at 2 h, but the extent of percutaneous absorption was lower than that of the oral absorption because of small absorption areas. No irritation was found after applying creams on the skin of the rabbit.