Kimball F A, Cornette J C, Bundy G L, Kirton K T
Prostaglandins. 1980 Sep;20(3):559-69. doi: 10.1016/0090-6980(80)90043-x.
A method is described for the estimation of 9-deoxo-16, 16-dimethyl-9-methylene-PGE2 by double antibody radioimmunoassay. Plasma samples obtained from animals treated with 9-methylene-16, 16-dimethyl-PGE2, 1-adamantanamic salt were extracted with diethyl ether to recover the prostaglandin. The validation of sample preparation and assay procedure are presented. Rhesus females were treated by several routes of administration and the samples assayed for drug content. Maximum blood levels were probably reached 30 minutes following subcutaneous injection and within 30 seconds of an intravenous injection. Results of the acute intravenous injection indicate an initial half-life of approximately one minute in peripheral circulation. Continuous intravenous infusion at 3 increasing doses of this compound resulted in a stepwise increase in plasma drug concentrations. Vaginal administration of 9-methylene-16, 16-dimethyl-PGE2, 1-adamantanamine salt in suppositories produced a dose dependent increase in plasma drug concentration. Higher plasma drug concentrations were produced when the prostaglandin was delivered in H-15 base suppositories than in E-76 base suppositories.
本文描述了一种通过双抗体放射免疫分析法来测定9-脱氧-16,16-二甲基-9-亚甲基-PGE2的方法。从用9-亚甲基-16,16-二甲基-PGE2的1-金刚烷胺盐处理过的动物身上获取血浆样本，用乙醚萃取以回收前列腺素。文中介绍了样本制备和测定方法的验证。对恒河猴雌性动物采用几种给药途径进行处理，并对样本进行药物含量测定。皮下注射后约30分钟以及静脉注射后30秒内可能达到最高血药浓度。急性静脉注射结果表明，在外周循环中初始半衰期约为1分钟。以3种递增剂量连续静脉输注该化合物导致血浆药物浓度逐步升高。阴道给药9-亚甲基-16,16-二甲基-PGE2的1-金刚烷胺盐栓剂会使血浆药物浓度呈剂量依赖性增加。当前列腺素以H-15基质栓剂给药时，产生的血浆药物浓度高于以E-76基质栓剂给药时的浓度。
