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前列腺素制剂的研究——Ⅰ.长效dl-15-甲基前列腺素F2α注射剂的研究

PREPARATIONS OF PROSTAGLANDINS Ⅰ. STUDY OF LONG-ACTING INJECTION-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 Cottage, 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-甲基前列腺素F2α(简称15-甲基PGF2α)是一种人工合成的前列腺素同类物,作用强度是PGF2α的10~20倍,对于子宫的作用远超过胃肠道,是一种高效的人工流产药物。我国在1974年合成了dl-15-甲基PGF2α,并用于中期妊娠引产获得成功。15-甲基PGF2α的给药方法主要有三种:(1)官腔内和羊膜腔内注射,用药物的醇溶液加生理盐水稀释,或加高分子右旋醣酐或甲基羟乙基纤维素稀释,一次注射。(2)肌

【Abstract】 15-methyl prostaglandin F2α is known as an available prostaglandin analogue for terminating the first and second trimester pregnancies. To induce an abortion, multiple intramuscular injections however are required. A long-acting injection-preparation hereby was suggested with 2 mg of dl-15-methyl prostaglandin F2α disposed in 2 ml 15% polyvinylpyrrolidone.Drug releasing tests were performed with this injection solution sealed in Visking dialysis tube and then immersed in an elution medium at 37℃. The rate of releasing, expressed in an empirical equation, was studied with an ordinary non-sustained prepa-ration as control. It indicated that the amount of drug released from this long-acting preparation in 8 hours was just equal to those released from the ordinary preparation in 2.7 hours.Intramuscular injections of this long-acting preparation once every 8 hours, had been demonstrated in clinic in terminating the first and/or second trimester pregnancies with remarkable effectiveness.Under the room temperature, this long-acting preparation was quite stable for one year without loss its potency, while under 50℃ its full potency kept only 42 days.

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