HMG和FSH一次性注射青年黄牛的药代动力学比较研究

目的]人绝经期促性腺激素(HMG)是一种具有促卵泡素(FSH)和促黄体素(LH)活性的蛋白质激素,为了比较HMG和FSH一次性注射青年母牛的药代动力学差异和参数。方法]本研究选择处于发情间期健康状况良好的青年母黄牛20头,随机分成两组,每头牛按4IU/kg体重肌肉注射HMG或FSH,于激素注射后不同时间段采集血样,分离血清后用放射免疫法测定血液中FSH和LH浓度。结果]表明注射HMG或FSH后血液中FSH与LH水平呈现先升高后下降的趋势,注射HMG后血液中FSH和LH激素水平达峰时间为6h,然后呈缓慢下降趋势,药代半衰期为18h;注射FSH后血液中FSH和LH激素水平在注射后激素血药达峰时间为0.5h,之后呈下降趋势,药代半衰期为6h。单次注射HMG后,0至144h监测期血液中FSH和LH的血药曲线下面积分别为971.21±342.06和176.28±81.80mIU*hr/mL(P0.05),均显著高于单次注射FSH后同期内血液中FSH和LH的血药曲线下面积(分别为39.81±18.01和32.00±20.92mIU*hr/mL,P0.05)。结论]在青年黄牛体内HMG比FSH的代谢稳定,其活性成分FSH和LH起作用的时间也较长。

Pharmacokinetics of HMG Compared with FSH in a Single Injection on the Heifer

Objective] HMG（human menopausal gonadotrophin）, a protein hormone, has the similar biological activity with FSH （follicle stimulating hormone） and LH （luteinizing hormone）. Thus, the objective of the present study is to compare the pharmacokinetics of HMG and FSH following intramuscular administration in heifers. Method]Diestrum heifers （n= 20） were equally divided into two groups. Animal in each group was injected by an intramuscular injection （4 IU/kg b. w） of HMG or FSH, respectively. Blood samples were collected at different time intervals after injections. After separating the sera, levels of FSH and LH were measured by radioimmunoassay （RIA）. Result]Both groups exhibited a sudden increase in FSH and LH after injections, while the peak was observed after 6 h and 0.5 h in HGM and FSH groups, respectively. Similarly, the half life of HMG was significantly prolonged （18 h） in comparison to that of FSH （6 h）. Between the groups, the area under curve from 0-144 h after injection, HMG significantly confined higher FSH and LH level （971. 21±342. 0 and 176. 28 ±81. 80 mIU ＊ hr/ml, P 〈0.05） in subject to FSH （39. 81± 18. 0 and 32. 00±20. 92 mIU ＊ hr/ml, P〈0. 05） administration. Conclusion]In short, HMG had more stable and prolonged metabolism than FSH. Thus it could be considered as long-acting FSH and LH analogue.