罗红霉素胶囊人体相对生物利用度研究

Study on the relative bioavailability of roxithromycin capsule

目的估算试验罗红霉素胶囊(T)的药代动力学参数及相对生物利用度,并以相同规格的罗红霉素胶囊作为参比制剂(R),判断两种胶囊是否具有生物等效性。方法22名健康志愿者单剂量口服罗红霉素胶囊(150mg)后48h内多点采集血样,微生物法测定人血清中罗红霉素的浓度。双周期两制剂交叉试验设计。血药浓度-时间数据经DAS软件处理后得药代动力学数据,并进行等效性检验。结果两种罗红霉素胶囊的血药浓度经时变化和药代动力学参数相近,AUC0～tT为(50.448±11.964)mg·h/L,AUC0～tR为(48.990±9.113)mg·h/L;AUC0～∞T为(50.538±12.806)mg·h/L,AUC0～∞R为(50.099±8.917)mg·h/L;CmaxT为(11.098±0.869)mg/L,CmaxR为(11.133±1.269)mg/L;TmaxT为(1.500±0.154)h,TmaxR(1.280±0.271)h;T1/2βT为(3.637±1.362)h,T1/2βR”为(3.522±0.575)h。以参比药作对照,计算罗红霉素的相对生物利用度,F为103.56%±19.67%,F′为100.91%±19.03%,均符合生物等效性要求。结论两种罗红霉素胶囊的口服生物利用度具有生物等效性。

Objective To measure the pharmacokinetics and relative bioavailability of test roxithromycin capsule (T) and to compare them with those of reference roxithromycin capsule (R). Methods Serum concentrations of roxithromycin within 48 h were measured by microbiology method following single oral dose of roxithromycin capsule (150mg) given to 22 healthy volunteers in a randomized 2-way crossover study. Data were processed by DA S software. Results The serum concentration-time curves and pharmacokinetics of the two products were similar. AUC_(0～t), AUC_(0 ～∞),C_(max), T_(max) and T_(1/2β) of T and R were (50.448±11 .964) mg/(L·h) and (48.990±9.113) mg /(L·h), (50.538±12.806) mg/(L·h) and (50.099±8.917) mg/(L·h), (11.098 ±0.869) mg/L and (11.133±1.269) mg/L, (1.500±0.154) h and(1.280±0.271 ) h, (3.637±1.362) h and(3.522±0.575) h pectively. The relative bioavailab ilities of T were (103.56±19.67%)(F) and (100.91±19.03%)(F′) compared with R. Conclusion Test roxithromycin capsules and reference roxithromycin capsules were bioequivalent.