Abstract

This study was to compare the pharmacokinetic characteristics of domestic altrenogest oral solution (DAOS) or imported altrenogest oral solution (IAOS) in healthy sows. A single administration (1 mg/kg body weight) of DAOS or IAOS was performed in sixteen healthy sows according to a two-period crossover design. Plasma concentrations of altrenogest (AT) were measured by high performance liquid chromatography coupled to a tandem mass spectrometer (HPLC-MS/MS) and the concentration-time data of AT was analyzed by WINNONLIN 5.2. It was suggested that the main pharmacokinetic parameters of DAOS and IAOS were as follows: C_max was 227.59 ± 83.35 ng/mL and 152.83 ± 80.34 ng/mL, T_max was 1.16 ± 0.52 h and 1.58 ± 0.85 h, t_1/2 was 3.63 ± 0.72 h and 3.45 ± 0.63 h, MRT was 5.02 ± 0.79 h and 5.21 ± 0.87 h, AUC_0–t was 1050.23 ± 409.80 h·ng/mL and 778.22 ± 397.84 h·ng/mL, and AUC_0–∞ was 1060 h·ng/mL and 786 h·ng/mL, respectively. The relative bioavailability of DAOS was 134.9%. Above results indicated that oral DAOS was better absorbed than IAOS, C_max of DAOS was higher than that of IAOS (p < 0.05). However, there was no significant difference in the main pharmacokinetic parameters between oral DAOS and IAOS (p > 0.05). Our data confirmed that the absorption, fast elimination and bioavailability of DAOS in sows were better than those of IAOS.

摘要

本研究旨在比较国产altrenogest口服溶液（DAOS）和进口altrenogest口服溶液（IAOS）在健康母猪体内的药代动力学特征。根据两期交叉设计，在 16 头健康母猪中进行 DAOS 或 IAOS 的单次给药（1 毫克/千克体重）。altrenogest (AT) 的血浆浓度通过高效液相色谱与串联质谱仪 (HPLC-MS/MS) 联用进行测量，AT 的浓度-时间数据通过 WINNONLIN 5.2 进行分析。提出DAOS和IAOS的主要药代动力学参数如下：C _max为227.59±83.35 ng/mL和152.83±80.34 ng/mL，T _max为1.16±0.52 h和1.58±0.85 h，t _1/2为3.63±0.72小时，3.45±0.63小时，MRT为5.02±0.79小时，5.21±0.87小时，AUC _0-吨为1050.23±409.80·H·ng / mL和778.22±397.84·H·毫微克/毫升，和AUC _{0- ∞ 分别}为 1060 h·ng/mL 和 786 h·ng/mL。DAOS 的相对生物利用度为 134.9%。以上结果表明口服DAOS比IAOS吸收更好，DAOS的C _max高于IAOS（p  < 0.05）。然而，口服DAOS和IAOS的主要药代动力学参数没有显着差异（p  >0.05）。我们的数据证实，母猪中DAOS的吸收、快速消除和生物利用度优于IAOS。