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评价两种环孢素软胶囊(受试制剂和参比制剂)在健康中国人体内的生物等效性。建立测定人全血中环孢素A的高效液相色谱-紫外(HPLC-UV)检测法,并进行方法学验证,采用随机双交叉自身对照试验设计,24名男性健康受试者分别口服受试制剂和参比制剂400mg后,测定环孢素A的血药浓度,计算药动学参数,评价两制剂的生物等效性。环孢素软胶囊(受试制剂)和环孢素软胶囊(参比制剂)中环孢素A主要的药动学参数如下:消除半衰期T1/2分别为(10.114±6.329)h和(9.717±4.076)h,达峰浓度Cmax分别为(2 021.235±298.581)ng.ml-1和(1 992.192±286.923)ng.ml-1,达峰时间Tmax分别为(1.729±0.361)h和(1.813±0.323)h;药时曲线下面积AUC0→t分别为(9 824.811±1 633.026)ng.h.ml-1和(10 316.514±1 395.955)ng.h.ml-1。以AUC0→t计算,环孢素软胶囊的相对生物利用度为(97.2±22.1)%。结果表明两制剂在健康中国人体内具有生物等效性。
To evaluate the bioequivalence of two cyclosporine soft capsules (test and reference preparations) in healthy Chinese. To establish a HPLC-UV method for the determination of ciclosporin A in human whole blood and verify the methodological validation. Twenty-four male healthy subjects were orally administered with a randomized double-crossover self-controlled trial The preparation and reference preparation after 400mg, determination of cyclosporin A plasma concentration, pharmacokinetic parameters were calculated to evaluate the bioequivalence of the two preparations. The main pharmacokinetic parameters of cyclosporin A in cyclosporin soft capsule (test preparation) and cyclosporin soft capsule (reference preparation) were as follows: elimination half-life T1 / 2 were (10.114 ± 6.329) h and (9.717 ± 4.076) h, respectively. The peak plasma Cmax values were (2 021.235 ± 298.581) ng.ml-1 and (1 992.192 ± 286.923) ng.ml-1, respectively. The time to peak Tmax were (1.729 ± 0.361) h and 0.323) h, and the AUC0 → t area under the curve was (9 824.811 ± 1633.026) ng.h.ml-1 and (10 316.514 ± 1 395.955) ng.h.ml-1, respectively. The relative bioavailability of cyclosporin soft capsule was (97.2 ± 22.1)%, calculated as AUC0 → t. The results show that both preparations are bioequivalent in healthy Chinese.