依诺沙星胶囊在健康人体的相对生物利用度与生物等效性

Relative bioavailability and bioequivalence of enoxacin capsules in healthy volunteers

目的 建立测定血浆依诺沙星浓度的HPLC-UV法并研究依诺沙星胶囊的相对生物利用度及其生物等效性。方法 按两制剂双周期自身对照交叉试验设计, 20名男性健康志愿者分别单剂量口服2种国产依诺沙星胶囊(参比制剂)和(受试制剂),用HPLC法测定血药浓度,计算药代动力学参数,并评价2制剂的生物等效性。结果 口服依诺沙星胶囊参比制剂及受试制剂400mg后的主要药代动力学参数:Cmax分别为(2. 98±0. 65)和(2. 90±0. 63)mg·L-1;tmax分别为(1. 23±0. 47)和(1. 43±0. 47)h;AUC(0→24)分别为(18. 20±4. 60)和(19. 71±4. 31)mg·h·L-1;t1 /2Ke分别为(6. 08±1. 23)和(5. 88±0. 89)h。受试制剂对参比制剂平均相对生物利用度F0→24为( 112. 0±26. 7 )%,F0-inf为(112. 2±28. 1)%。结论 2种依诺沙星胶囊制剂生物等效。

Objective To determine enoxacin concentrations in human plasma and study the pharmacokinetics and relative bioavailability of enoxacin capsules. Methods A single dose 400 mg of reference and test enoxacin capsules was given to 20 healthy volunteers in a randomized 2-way cross-over study. The plasma enoxacin concentrations were determined by HPLC. The pharmacokinetics as well as relative bioavailability were measured. Results The main pharmacokinetic parameters of two formulations, reference and test drug were as follows: C max were (2.98±0.65) and (2.90± 0.63 ) mg·L -1 ,t max were(1.23±0.47) and (1.43±0.47)h, AUC (0→24) were (18.20±4.60) and (19.71±4.31) mg·h·L -1 ;t 1/2Ke were (6.08±1.23) and (5.88± 0.89 )h. The relative bioavailability of AUC (0→24) and AUC (0-inf) was (112.0±26.7)% and (112.2±28.1)%,respectively.Using 3P97 program, the results of variance and two one-sided t-test statistical analysis for LnC max , LnAUC (0→24) and LnAUC (0-inf) showed that two formulations were bioequivalent. Conclusion The reference and test enoxacin capsules were bioequivalent.