Duijkers I J, Beerens M C, Coelingh Bennink H J, Huisman J A, Rombout F, Vemer H M
Department of Obstetrics and Gynaecology, University Hospital, Nijmegen, The Netherlands.
Hum Reprod. 1995 Jun;10(6):1367-72. doi: 10.1093/humrep/10.6.1367.
A randomized study was performed in nine healthy women, to investigate pharmacokinetic parameters and bioequivalence of two human menopausal gonadotrophin preparations after i.v. administration. Endogenous gonadotrophin activity was suppressed by triptorelin administration. Humegon and Pergonal (225 IU of each) were injected i.v. in a cross-over way with an interval of 1 week. Blood samples were collected frequently and serum concentrations of follicle stimulating hormone (FSH), luteinizing hormone (LH), specific LH, and human chorionic gonadotrophin (HCG) were determined by fluoroimmunoassays assays. Serum LH bioactivity was measured by an in-vitro bioassay. The area under curve (AUC) and half-life of FSH were respectively 431.5 IU h/l and 22.20 h for Humegon, and 402.6 IU h/l and 21.33 h for Pergonal. For both preparations, the (total) LH immunoactivity and in-vitro bioactivity of serum LH were very similar, and appeared to be a composite of specific LH and HCG activity. The AUC data of specific LH were 17.50 IU h/l for Humegon and 21.79 IU h/l for Pergonal respectively. The AUC and half-life of HCG were 153.7 IU h/l and 14.80 h for Humegon, and 134.1 IU h/l and 12.11 h for Pergonal. The two preparations were bioequivalent with respect to FSH and HCG immunoreactivity. Bioequivalence could not be proven for LH activity because of the small number of subjects.
对9名健康女性进行了一项随机研究，以调查两种人绝经期促性腺激素制剂静脉注射后的药代动力学参数和生物等效性。通过注射曲普瑞林抑制内源性促性腺激素活性。以交叉方式静脉注射贺美奇和果纳芬（各225 IU），间隔1周。频繁采集血样，通过荧光免疫分析法测定血清中促卵泡激素（FSH）、促黄体生成素（LH）、特异性LH和人绒毛膜促性腺激素（HCG）的浓度。通过体外生物测定法测量血清LH生物活性。贺美奇的FSH曲线下面积（AUC）和半衰期分别为431.5 IU·h/l和22.20小时，果纳芬分别为402.6 IU·h/l和21.33小时。对于两种制剂，血清LH的（总）免疫活性和体外生物活性非常相似，似乎是特异性LH和HCG活性的复合物。特异性LH的AUC数据，贺美奇为17.50 IU·h/l，果纳芬为21.79 IU·h/l。HCG的AUC和半衰期，贺美奇分别为153.7 IU·h/l和14.80小时，果纳芬分别为134.1 IU·h/l和12.11小时。两种制剂在FSH和HCG免疫反应性方面具有生物等效性。由于受试者数量较少，无法证明LH活性的生物等效性。
