两种苦参素软胶囊的人体生物等效性研究

Research of Bioequivalence of Two Kinds of Oxymatrine Soft Capsules in Healthy Volunteers

目的研究两种苦参素软胶囊的人体生物等效性。方法18例健康男性志愿者随机分为两组,分别口服受试制剂苦参素软胶囊和参比制剂苦参素软胶囊900mg,7d后交叉服用参比制剂和受试制剂。采用高效液相色谱法测定两组受试者体内苦参碱的经时血药浓度,计算其药动学参数和相对生物利用度,评价两种制剂的生物等效性。结果单次口服受试制剂与参比制剂900mg后,两组受试者的主要药动学参数Cmax分别为(3.48±1.01)和(3.40±0.57)mg·L1,tmax分别为(11.44±2.97)和(12.11±1.45)h,t1/2分别为(7.94±2.86)和(8.55±3.49)h,AUC0→36分别为(57.66±14.10)和(59.04±10.57)mg·h·L1,AUC0→∞分别为(64.56±18.70)和(67.06±14.75)mg·h·L1。经检验,两组药动学参数均差异无显著性(均P>0.05)。受试制剂的相对生物利用度为(98.5±21.3)%(F0→36)和(97.4±23.0)%(F0→∞)。结论受试制剂与参比制剂苦参素软胶囊具有生物等效性。

Objective To study the bioequivalence of two kinds of oxymatrine soft capsules in healthy volunteers. Method A single oral dose of 900 mg matrine of test product or of reference product was given to 18 healthy male volunteers randomized into two groups. Seven days later the two products were administrated again by exchange of the oxymatrine products. Oxymatrine concentrations in plasma were determined by HPLC method. The pharmacokinetic parameters and relative bioavailability were calculated by 3P97 program to evaluate the bioequivalence of two preparations. Results The main pharmacokinetic parameters of the test and the reference were: C max were(3. 48±1. 01) mg·L -1 and(3. 40±0. 57) mg·L - 1 ; t max were (11.44±2. 97) h and(12.11±1.45) h; t 1/2 were (7.94±2.86) h and (8.55±3.49) h; AUC 0→36 were (57.66±14.10) mg·h·L -1 and(59.04±10.57) mg·h·L -1 ; AUC 0→∞ were (64.56±18.70) mg·h·L -1 and (67.06±14.75) mg·h·L -1,respectively. The relative bioavailability of the test to the reference were(98.5±21.3)%( F 0→36 )and(97.4±23.0)% ( F 0→∞).Conclusion The results demonstrated that the two oxymatrine products had bioequivalent.