国产与进口司他夫定胶囊的人体生物等效性

Bioequivalence of domestic and imported stavudine in human plasma

目的评价国产与进口司他夫定胶囊的人体生物等效性。方法20名健康受试者随机分组、自身交叉口服单剂量司他夫定试验制剂和参比制剂。血浆样品采用固相萃取处理,HPLC内标法测定。结果试验制剂与参比制剂的AUC0→10分别为(2.36±0.65)、(2.40±0.69)h·mg·L-1;AUC0→∞为(2.41±0.67)、(2.46±0.72)h·mg·L-1;cmax为(1.15±0.36)、(1.10±0.32)mg·L-1;tmax为(0.95±0.13)、(0.94±0.14)h;T1/2为(1.90±0.34)、(1.90±0.26)h。试验制剂相对参比制剂的人体生物利用度是(99.69±14.28)%(n=20,以AUC0→10计)。2种司他夫定胶囊的主要药动学参数经交叉试验方差分析示差异无显著性(P>0.05)。2制剂的AUC0→10、AUC0→∞、cmax经双单侧t检验示90%置信区间位于有效区间80%～125%范围内。结论司他夫定胶囊的国产制剂与进口制剂具有生物等效性。

AIM To evaluate the bioequivalence of domestic and imported stavudine capsules. METHODS Twenty healthy volunteers were divided randomly into 2 groups , and a cross-over, single oral dose of stavudine at the dose of 40 mg of test capsule and reference one were given,respectively.Plasma sample was extracted by solid-phase ,and determined by HPLC. RESULTS AUC 0→10,AUC 0→∞,c max,t max,T 1/2 of test capsule and reference one were (2.36±0.65) h·mg·L -1,(2.41±0.67) h·mg·L -1,(1.15±0.36) mg·L -1,(0.95±0.13) h,(1.90±0.34) h,and (2.40±0.69) h·mg·L -1,(2.46±0.72) h·mg·L -1,(1.10±0.32) mg·L -1,(0.94±0.14)h,(1.90±0.26) h,respectively.The bioavailability of test capsule versus reference one was (99.69±14.28)% (n=20).There were no statistical differences of main phamacokinetic parameters between test capsule and reference one (P>0.05). CONCLUSION The results suggest that the two preparations are bioequivalent.