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前列腺素制剂的研究——Ⅱ.dl-15-甲基前列腺素F2α阴道海绵剂的研究

PREPARATIONS OF PROSTAGLANDINS Ⅱ. STUDY OF VAGINAL SPONGING-PREPARATION OF dl-15-METHYL PROSTAGLANDIN F2α

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【作者】 金昭英; 郑玲妹;

【Author】 JIN ZHAO-YING ZHENG LING-MEI(Department of pharmaceutics, Faculty of Pharmacy, Shanghai First Medical Collage, Shanghai)

【机构】 上海第一医学院药学系药剂学教研组; 上海第一医学院药学系药剂学教研组;

【摘要】 <正> 15-甲基PGF2α宫腔注入和肌内注射,在人工流产上虽然取得显著的疗效,但都有一定缺点。为了用药更加安全和简便,近年来国内外都很注意发展阴道给药。Green等研究了15-甲基PGF2α甲酯的药物代谢动力学,证明能在阴道吸收,奠定了阴道给药的理论基础。所用的剂型包括栓剂、长效栓剂和硅橡胶片。后者是一种较

【Abstract】 Prostaglandins formulated in a suppository or polysiloxane device had been reported from several clinics to be very successful in terminating the early pregnancy. A vaginal sponging-preparation with 4 mg of dl-15-methyl prostaglandin F2α per piece was hereby proposed for the same purpose.Drug releasing tests were performed with this sponging-preparation immersed in an elution medium at 37℃. Plotting the cumulative amount of the drug released against the time, the rate of drug releasing curve was well agreed with Pick’s law An empirical equation was derived, within an interval of 10 hours, a smooth drug releasing curve as a rule could be obtained.Following the vaginal insertion, the residual amount of dl-15-methyl prostaglandin F2αin the sponge was measured, it demonstrated that all of these sponges were quite definitely to be efficient for a period of 8 hours. For the termination of the firstand/or second trimester pregnancies, obstetricians were therefore advised to changethe vaginal sponges every 8 hours accordingly.This vaginal sponge of dl-15-methyl prostaglandin F2α were proved to be stable for one year under the room temperature.

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