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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f_2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·m L·h~(-1),达峰浓度分别为(5 552±1 554)和(5 911±1 700)ng·m L~(-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 study the two polymorphs of rifampicin in the tablets of Fufang, and to compare whether the two polymorphs are equivalent in vitro and in vivo. Methods The dissolution profiles of reference preparations and test preparations in different media were determined respectively, and the similarity of dissolution curves was compared. A randomized crossover oral reference preparation and a test preparation of 29 male healthy volunteers (including rifampicin 300 mg). The content of rifampicin in blood was analyzed by HPLC-MS. The relative bioavailability and bioequivalence were analyzed by SAS software. Results The f2 value of the dissolution profile of the reference preparation and the test preparation was greater than 50; the AUC of the reference preparation and the test preparation were (28 476 ± 8 050) and (28 120 ± 6 916) ng · m L · The peak time was (5 552 ± 1 554) and (5 911 ± 1 700) ng · m L -1, peak time was (2.0 ± 1.0) and (1.8 ± 1.0) h, and the half-lives were (2.8 ± 0.5) and (2.8 ± 0.5) h, respectively. The 90% confidence intervals of the AUC and ρ max of the test preparations were 96.2% -106.4% and 98.6% -115.3% respectively, which all fell within the range of 80% -125% of the reference preparations. The test preparations and the reference preparations There was no significant difference in t max (P> 0.05). Conclusion The two forms of rifampicin in Yifu tablets are bioequivalent.