十八甲基炔诺酮透皮控释传递系统在人体不同部位皮肤的药物动力学

Pharmacokinetics of Levonorgestrel Transdermal Controlled Delivery System in Body Different Parts of Healthy Women

6名健康妇女分别于上臂、臀部和腹部三部位经皮给予合LNG的透皮控释传递系统（TCDS）后，用放射免疫法测定LNG血清浓度，计算其主要药物动力学参数。结果表明：在TCDS用药期间，三部位的C（max）、T（max）及AUC（0～168h）基本接近，部位间无显著性差异（P＞0．05）；TCDS揭除后，AUC（168～204h）及消除相半衰期T（1／2）（Ke）均以腹部最大，臀部次之，上臂最小，在腹部与上臂间有显著性差异（P＜0．05）。上述结果可归因于TCDS对LNG的控释和人体皮下脂肪的“贮库效应”。

The serum concentration - time profiles and pharmacokinetics of LNG were characterized after application of LNG/E2 TCDS to the following parts of body of 6 healthy women on: upper arm, haunch and lower abdomen. The serum concentration of LNG was measured by radioimmunoassay method. The pharmacokinetic parameters of C(max),T(max) and AUC (0~168 h) of the three application sites during the wearing period were found to have no significant difference (P> 0. 05). However, after removal of LNG/E2 TCDS, the parameter values of AUC (168~204 h) and T1/2(Ke) of abdomen were great compared with those of arm and haunch. There were statistically significant differences between abdomen and arm (P<0. 05). These results may be attributed to the TCDS - controlled release of LNG and'reservoir effect' of the drug on human boby.