米非司酮胶囊的相对生物利用度

Study on relative bioavailability of mifepristone capsules

目的:评价米非司酮胶囊的相对生物利用度。方法:采用高效液相色谱法(HPLC)检测。18 名健康女性志愿者采用两制剂双周期交叉试验方法,分别口服两种制剂后不同间隔时间的血药浓度。并依此计算药动学参数评价胶囊的生物利用度。结果:受试者口服75 mg米非司酮胶囊或片剂的Cmax分别为(1.3±0.4)mg·L-1,(1.3±0.4) mg·L-1;Tpeak是(0.9±0.3)h,(0.9±0.5)h;T1/2Ke为(36.2±21.0)h,(33.4±12.3)h;AUC(0-t)分别是(19.7±6.4)mg·L-1·h,(19.6±9.9)mg·L-1·h。胶囊的相对生物利用度为(109.4±34.8)%。结论:两种制剂的主要药动参数,经对数转换后进行交叉试验的方差分析与双单侧 t检验表明,两种制剂的AUC及有关的药动学参数具有生物等效性。

OBJECTIVE To evaluate the bioequivalence of two dosageforms of mifeipristone METHODS Single oral dose of mifeipristone capsule and tablet were given to 18 volunteers in an open randomized cross over way to study the relative bioavailability. Mifepristone concentriations in plasma were determined by HPLC. RESULTS The. pharmacokinetic parameters of capsule and tablet formulations were as follows ： Tpeak （0. 9 ± 0. 3 ） h and （0. 9 ± 0. 5 ） h; Cmax （ 1. 3 ± 0. 4） mg·L^-1 and （ 1.3 -± 0. 40）mg·L^-1; T1/ 2Ke （36. 2 ± 21.0）h and （33. 4 ± 12. 3） h; AUC（0-t） （ 19. 7 ± 6. 4）mg·L^-1 ·h, （ 19. 6 ± 9. 9）mg·L^-1 , h. The relative bioavailability of cap- sule was （109. 4 ± 34. 8）%. The statistical analysis result of above parameters showed that there was no significant difference between two formulations. CONCLUSION The two formulations are bioequivalent.