论文部分内容阅读
目的评价左旋去甲基苯环壬酯在比格犬体内生物利用度。方法 LC-MS/MS法测定比格犬口服和静脉给药后体内的血药浓度,计算药代动力学参数和绝对生物利用度。结果比格犬口服给药2 mg/kg后5 min即可测得血中药物含量,口服给药后1 h左旋去甲基苯环壬酯在比格犬体内血药浓度达峰,给药后36 h血中药物浓度均已降至LLOQ以下。比格犬口服和静脉注射2 mg/kg左旋去甲基苯环壬酯的t1/2分别为(5.36±0.82)h和(6.73±2.00)h,Cmax分别为(141.88±51.03)和(591.84±144.61)μg/L;AUC(0-36 h)分别为(962.42±220.96)和(1572.06±365.80)μg.L-1.h;用AUC(0-36 h)计算比格犬口服单剂量左旋去甲基苯环壬酯的绝对生物利用度为(61.22±10.78)%。结论左旋去甲基苯环壬酯口服给药吸收迅速,绝对生物利用度较高,具有良好的开发前景。
Objective To evaluate the bioavailability of L-nor -benzylcynonate in Beagle dogs. Methods LC-MS / MS method was used to determine the pharmacokinetic parameters and absolute bioavailability of Beagle dogs after oral administration and intravenous administration. Results Beagle dogs oral administration of 2 mg / kg after 5 min to measure the blood drug levels, 1 h after oral administration of L-nor -benzyl nonyl ester in Beagle dogs blood concentration peak, the administration After 36 h blood drug concentrations have dropped below LLOQ. The t1 / 2 of oral and intravenous injection of 2 mg / kg levonorgestrel were (5.36 ± 0.82) h and (6.73 ± 2.00) h, respectively, with Cmax of (141.88 ± 51.03) and (591.84 ± 96.61) μg / L; AUC (0-36 h) were (962.42 ± 220.96) and (1572.06 ± 365.80) μg.L-1.h respectively; AUC (0-36 h) The absolute bioavailability of L-nor -benzylcynonate was (61.22 ± 10.78)%. Conclusions L-nor -benzylcyclononane is absorbed orally rapidly and has high absolute bioavailability, which has a good prospect of development.