氟康唑胶囊的人体药动学及其生物等效性研究

Study on pharmacokinetics and bioequivalence of fluconazole capsule in human

目的：研究氟康唑胶囊受试制剂与参比制剂在健康志愿者体内的药代动力学和生物等效性。方法：18名健康男性受试者随机双周期交叉单剂量口服氟康唑胶囊受试制剂和参比制剂200mg，用HPLC法测定氟康唑的血药浓度，求得有关药动学参数。结果：氟康唑胶囊受试制剂和参比制剂的AUCm，狲分别为（224．977±39．361）和（211．212±36．221）mg／a·L^-1，Cmax分别为（5．811±1．202）和（5．705±1．092）mg／L，Tmax分别为（1．056±0．466）和（1．375±0．884）h，t1／2分别为（32．559±5．072）和（30．162±7．257）h。受试制剂相对于参比制剂的生物利用度（F）为（107．41±14．79）％。氟康唑AUC0-120h和Cmax经对数转换后双单侧t检验均P〉0．05，受试制剂AUC0-120h 90％可信限度在参比制剂100．7%-112．6％内，Cmax90％可信限度在参比制剂92．8％～111．1％区间内。结论：氟康唑胶囊的受试制剂与参比制剂具有生物等效性。

Objective： To study the pharmacokinetics and bioequivalence of fluconazole capsule in human. Methods： Fluconazole capsule tested preparation and reference preparation were taken orally with double cycle and cross single dose 200 mg randomly by 18 healthy male volunteers, the concentration of fluconazole in blood plasma was determined using HPLC, and some of the pharmacokinetic parameters were acquired. Results： Of fluconazole capsule tested preparation and reference preparation, the AUC0 - 120 h were （224. 977 ± 39. 361 ） and （211.212 ± 36.221） mg/h·L^-1, Cmax were （5.811± 1.202） and （5.705 ± 1.092） mg/L, Tmax were （1.056 ± 0.466） and （1.375 ± 0.884） h, t1/2 were （32.559 ± 5.072） and （30.162 ±7.257） h,respeetively. Preparations for the test phase reference preparation of The bioavailability （F） of tested preparation to referenee preparation was（ 107.41 ± 14.79） %. Double and unilateral t - test for the AUC0 - 120h and Cmax of Fluconazole were all P 〉 0.05 after log conversion. The 90% credible interval of AUC0 -120 h was equivalent to 100. 7% - 112.6% range that in reference preparation; 90% credible interval of Cmax was equivalent to 92.8% -111.1% range that in reference preparation. Conclusion： The tested preparation and reference preparation of fluconazole capsules are bioequivalent.