el-Raghy I, Back D J, Makeram M, Salem H, Osman F, Fathalla M, Orme M L
Contraception. 1986 Apr;33(4):379-84. doi: 10.1016/0010-7824(86)90100-9.
Plasma concentration profiles and pharmacokinetic parameters have been obtained following single dose administration of three commonly used oral contraceptive steroid preparations, Ovral, Nordette and Norminest to Egyptian women. The constituents of the preparations are as follows: Ovral (50 micrograms ethinyloestradiol, EE2 and 500 micrograms levonorgestrel, LNG); Nordette (30 micrograms EE2 and 150 micrograms LNG); and Norminest (35 micrograms EE2 and 500 micrograms norethisterone, NOR). Peak plasma concentrations of EE2 ranged between 116-160 pg ml-1 for Ovral, 55-78 pg ml-1 for Norminest and 30-70 pg ml-1 for Nordette. There was no significant difference in half-life (t1/2), oral clearance (CL) or apparent volume of distribution (Vd). The relative values of the area under the plasma concentration-time curve (AUC) reflected well the different amounts of oestrogen in each preparation. There was no significant difference in t1/2, CL or Vd for LNG in the 2 preparations containing this progestogen. The mean AUC following Nordette (150 micrograms LNG) was 40% of that following Ovral (500 micrograms LNG; p less than 0.001). Comparing pharmacokinetic parameters for the same dose of LNG (Ovral) and NOR (Norminest) showed the AUC to be decreased and CL and Vd increased in the latter group. The study indicates that the kinetic profile of the OCS in healthy Egyptian women are similar to other ethnic populations.
对埃及女性单剂量服用三种常用口服避孕甾体制剂(复方炔诺孕酮片、复方左炔诺孕酮片和复方炔诺酮片)后,获得了血浆浓度曲线和药代动力学参数。制剂的成分如下:复方炔诺孕酮片(50微克炔雌醇,EE2和500微克左炔诺孕酮,LNG);复方左炔诺孕酮片(30微克EE2和150微克LNG);复方炔诺酮片(35微克EE2和500微克炔诺酮,NOR)。复方炔诺孕酮片中EE2的血浆峰值浓度在116 - 160 pg/ml之间,复方炔诺酮片中为55 - 78 pg/ml,复方左炔诺孕酮片中为30 - 70 pg/ml。半衰期(t1/2)、口服清除率(CL)或表观分布容积(Vd)无显著差异。血浆浓度 - 时间曲线下面积(AUC)的相对值很好地反映了每种制剂中雌激素的不同含量。在含有这种孕激素的两种制剂中,LNG的t1/2、CL或Vd无显著差异。复方左炔诺孕酮片(150微克LNG)后的平均AUC是复方炔诺孕酮片(500微克LNG)后的40%(p小于0.001)。比较相同剂量LNG(复方炔诺孕酮片)和NOR(复方炔诺酮片)的药代动力学参数显示,后一组的AUC降低,CL和Vd增加。该研究表明,健康埃及女性中口服避孕药的动力学特征与其他种族人群相似。