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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”。
Six healthy women received transdermal controlled release system (TCDS) combined with transdermal delivery of LNG through the upper arm, buttocks and abdomen respectively. The serum concentrations of LNG were measured by radioimmunoassay and the main pharmacokinetic parameters were calculated. The results showed that the C (max), T (max) and AUC (0 ~ 168h) of the three sites were close to each other and there was no significant difference between the two sites during the TCDS treatment (P> 0.05) (168 ~ 204h) and elimination phase half-life (T (1/2) (Ke)) were the largest in the abdomen, the second in the hips, the smallest in the upper arm and the other in the abdomen and upper arm (P <0.05). The above results are attributable to the “storage effect” of TCDS on controlled release of LNG and human subcutaneous fat.