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育龄妇女肌注复方甲地孕酮避孕针的药代动力学

PHARMACOKINETICS OF MEGESTROL ACETATE IN WOMEN RECEIVINGIM INJECTION OF ESTRADIOL-MEGESTROL LONG-ACTING INJECTABLE CONTRACEPTIVE

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【作者】 褚云鸿; 李全; 赵志芳;

【Author】 CHU Yun-Hong;LI Quan;ZHAO Zhi-Fong Department of pharmacolog, Shanghai Medical University, Shanghai

【机构】 上海医科大学药理教研室; 上海医科大学药理教研室 上海; 上海; 上海;

【摘要】 采用放射免疫、放射配体和平衡透析法研究肌注复方甲地孕酮避孕针后,健康育龄妇女血浆和唾液中醋酸甲地孕酮(MA)浓度,性激素结合球蛋白(SHBG)和MA与血浆蛋白结合率的变化,结果表明im复方甲地孕酮避孕针后血中AM浓度迅速升高,平均达峰时间为3天,以后下降,在下降阶段血浆MA浓度的对数与注射后大数成直线关系,消除相T1/2为14.35±9.1天,与注射前比较血浆SHBG含量于肌注后7和14天明显升高,21和29天明显降低、MA主要与血浆白蛋白结合,结合率达82.4%,MA与SHBG无特异结合,唾液中MA浓度与血浆浓度呈正相关。

【Abstract】 A radioimmunoassay(RIA), radiolignd assay and equilibriumdialysis for determination of plasma and salivary megestrol acetate(MA) concen-tration, sex hormone binding globulin(SHBG)capacity in plasma and percentagealbumin bound MA were studied in healthy women receiving single im injectionof estradiol-megestrol long-acting injectable contraceptive. The results showedthat after injection the concentration of plasma MA increased rapidly. The meantime of peak plasma MA level wsa 3th day, there was a linearr elationship betweenlog of plasma MA concentration and time(day)after administration in all subjects,Elimination phase half-life t 1/2β=14. 35±9. 1 days. The plasma SHBG capacitysignificantly increased at 7th, 14th day and decreased at 21th, 29th day afterinjection The percentage albumin bound MA was 82. 4%. There was no specificSHBG bound MA. There was a positive correlation between the MA concen-trations in saliva and those in plasma.

  • 【文献出处】 中国临床药理学杂志 ,The Chinese Journal of Clinical Pharmacology , 编辑部邮箱 ,1986年04期
  • 【被引频次】2
  • 【下载频次】20
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