甲砜霉素胶囊人体生物等效性研究

Investigation of bioequivalence of thiamphenicol capsules in healthy volunteers

目的:进行试验制剂甲砜霉素胶囊与参比制剂市售甲砜霉素胶囊生物等效性研究。方法:男性健康志愿者20名,随机分为2组,分别交叉单剂服用试验制剂或参比制剂甲砜霉素胶囊500mg,采用高效液相色谱法测定甲砜霉素经时血药浓度,计算药动学参数,评价2制剂的生物等效性。结果:试验制剂和参比制剂主要药动学参数t1/2为(3.7±s0.5)h和(3.1±0.6)h,tmax为(2.0±0.3)h和(2.0±0.3)h,cmax为(2.3±0.6)mg·L-1和(2.3±0.5)mg·L-1,AUC0～12为(9.0±1.4)mg·h·L-1和(9.0±1.6)mg·h·L-1,AUC0～∞为(9.8±1.8)mg·h·L-1和(9.8±1.6)mg·h·L-1。试验制剂甲砜霉素胶囊相对生物利用度(F)为(101±6)%。结论:甲砜霉素胶囊试验制剂和参比制剂为生物等效制剂。

AIM:To study the bioequivalence of thiamphenicol capsules in healthy volunteers . METHODS:Twenty volunteers were randomly divided into 2 groups,ten f or each and undertaken two crossover designs. Blood samples were collected at 0, 0.5,1,1.5,2,3,4,6,8,12,24,36,48,72 h after a single oral dose of 500 mg thiamphenicol capsules of test or reference respectively. The time-concentr a tions of thiamphenicol were determined by HPLC and pharmarcokinetic parameters calculating with DAS practical pharmacokinetic programme. RESULTS: The pharmarcokinetic pa rameters of thiamphenicol capsules of test and reference were as follows: t _(1/2)(3.7±s 0.5) h and ((3.1±)0.6) h ,t_(max) (2.0±( 0. 3) h) and ( 2.0±0.3) h,c_(max) (2.3±0.6) mg·L^(-1) and (2.3±0.5) mg·L^(-1),AUC_(0-12)(9.0±1.4) mg· h·L^(-1) and (9.0±(1.6) mg·h·L^(-1),)AUC_(0-∞) (9.8±1 .8) mg·h·L^(-1) and (9.8±1.6) mg·h·L^(-1), respectively. The relativ e bioavailability of thiamphenicol capsules was (101±6) %. CONCLUSION: The statistical analysis showes that thiamphenicol capsules of the test and ref er ence are bioquivalent.