目的 以异福片中两种利福平晶型为研究对象,比较这两种晶型在体内外是否等效。方法 分别测定参比制剂和受试制剂在不同介质中的溶出曲线,比较溶出曲线的相似度;选29例男性健康志愿者随机交叉口服参比制剂和受试制剂1粒(含利福平300 mg),用HPLC-MS分析血液中利福平含量,经SAS软件统计,进行相对生物利用度和生物等效性分析。结果 参比制剂和受试制剂的溶出曲线相似度因子f₂值大于50;参比制剂和受试制剂的AUC分别为(28 476±8 050)和(28 120±6 916) ng·mL·h^-1,达峰浓度分别为(5 552±1 554)和(5 911±1 700)ng·mL^-1,达峰时间分别为(2.0±1.0)和(1.8±1.0)h,半衰期分别为(2.8±0.5)和(2.8±0.5)h。受试制剂的AUC和ρ_max的90%置信区间分别为96.2%~106.4%和98.6%~115.3%,均落在参比制剂的80%~125%内;受试制剂和参比制剂的t_max没有显著性差异(P>0.05)。结论 异福片中两种晶型的利福平生物等效。

OBJECTIVE To evaluate the pharmacokinetic properties and bioequivalence of two crystal forms of rifampicin. METHODS Drawing the dissolution curves of reference and test medicines in different solutions,and calculated the value of f₂. Twenty-nine healthy male volunteers were randomly administered in a crossover single 300 mg dose of reference and test medicines. Determining the concentration of rifampicin in plasma by HPLC-MS,and analyzed the relative bioavailability and bioequivalence of tablets using SAS program. RESULTS The values of f₂ were more than 50. The pharmacokinetic properties of reference and test tablets were as followsAUC_0→t:(28 476±8 050) vs (28 120±6 916) ng·mL·h^-1,ρ_max:(5 552±1 554) vs (5 911±1 700)ng·mL^-1,t_max:(2.0±1.0) vs (1.8±1.0)h,t_1/2:(2.8±0.5)vs(2.8±0.5)h. 90% CI of AUC and ρ_max of test medicine were 96.2%-106.4% and 98.6%-115.3%,respectively. And there were no significant difference of the t_max of rifampicin between the two medicines(P>0.05). CONCLUSION The results indicate that the two medicines made from rifampicin two crystal forms are bioequivalent completely.