米非司酮片在健康人体的生物等效性研究

目的：建立测定人血浆中米非司酮浓度的HPLC法，以评价2种制剂在健康人体内的生物等效性。方法：18名健康女性受试者双周期随机交叉单剂量口服2种米非司酮片剂（受试制剂和参比制剂）25 mg，采用HPLC法测定米非司酮的血药浓度，计算两者药代动力学参数及相对生物利用度。结果：受试制剂与参比制剂的主要药动学参数： T_max分别为(0.81±0.23)和(0.81±0.23)h；C_max分别为(849.91±257.77)和(852.01±258.26)ng·mL^-1；t_1/2分别为(29.72±11.06)和（27.96±13.35）h；AUC_0~120分别为(7259.49±2256.93)和(7802.63±4049.20)ng·h·mL^-1；AUC_0~∞分别为(8635.35±2696.45)和(9354.08±4469.31)ng·h·mL^-1。受试制剂相对生物利用度为(104.91±36.45)%。结论：该方法选择性好，灵敏度高，适于米非司酮的体内过程研究；2种片剂具有生物等效性。

Objective:To establish an HPLC method for determination of pharmacokinetic of mifepristone in human plasma and to evaluate the bioequivalence of two mifepristone tablets in healthy volunteers.Method:In a randomized,crossover and self-control study,18 healthy female volunteers were orally administrated with mifepristone tablets(test sample and reference sample)25 mg.The plasma concentration of mifepristone was determined by HPLC detection.The pharmacokinetic parameters and relative bioavailability were calculated.Results:The main pharmacokinetic parameters of test and reference preparation were as follows: T_max(0.81± 0.23)and(0.81± 0.23)h; C_max(849.91± 257.77)and(852.01± 258.26)ng·mL^-1; t_1/2(29.72± 11.06)and(27.96± 13.35)h;AUC_0-120(7259.49± 2256.93)and(7802.63± 4049.20)ng·h·mL^-1;AUC_0-∞(8635.35±2696.45)and(9354.08±4469.31)μg·h·mL^-1,respectively.The relative bioavailability of the test formulation was(104.91± 36.45)%.Conclusion:The method is selective,sensitive and rapid for mifepristone determination.The results showed that the two formulations were bioequivalent.