Ritter W, Patzschke K, Krause U, Stettendorf S
Chemotherapy. 1982;28 Suppl 1:37-42. doi: 10.1159/000238150.
Absorption of clotrimazole after vaginal application was estimated to be between 3 and 10%. In order to investigate the fate of clotrimazole reaching systemic circulation, pharmacokinetic studies following oral and intravenous administration were carried out. The concentrations of clotrimazole in vaginal fluid and in blood plasma after vaginal application of 200 and 500 mg were determined using a specific assay by quantitative thin-layer chromatography. Fungicidal concentrations of clotrimazole in vaginal fluid up to 3 days after application of one vaginal tablet containing 500 mg were found. In contrast, clotrimazole plasma levels were lower than 0.01 micrograms/ml, demonstrating that clotrimazole is rapidly metabolized.
阴道给药后克霉唑的吸收估计在3%至10%之间。为了研究进入体循环的克霉唑的转归，进行了口服和静脉给药后的药代动力学研究。采用定量薄层色谱法通过特定测定法测定了200毫克和500毫克阴道给药后阴道液和血浆中克霉唑的浓度。发现在应用一片含500毫克的阴道片后长达3天的时间里，阴道液中克霉唑的杀菌浓度存在。相比之下，克霉唑的血浆水平低于0.01微克/毫升，表明克霉唑迅速被代谢。
