亚叶酸钙分散片人体药动学与生物等效性研究

Pharmacokinetics and Bioequivalence of Calcium Folinate Dispersed Tablets

目的评价两种亚叶酸钙制剂在健康人体内的药动学和生物等效性。方法18例男性健康志愿者随机交叉单剂量口服两种亚叶酸钙分散片,采用高效液相色谱(HPLC)法测定血浆中药物浓度,通过方差分析和双向单侧t检验比较两种分散片药时曲线下面积AUC0～12。结果受试制剂和参比制剂的tmax均为(1.5±0.0)h,Cmax分别为(2295.51±368.93)和(2139.53±189.67)ng·mL-1,t1/2分别为(2.19±0.16)h和(2.23±0.17)h,药时曲线下面积AUC0～12分别为(6202.09±229.90)ng·mL-1·h和(6185.32±191.47)ng·mL-1·h,AUC0-∞分别为(6478.43±250.69)ng·mL-1·h和(6478.63±248.10)ng·mL-1·h。结论两种亚叶酸钙分散片生物等效,相对生物利用度为(100.13±5.39)%。

Objective To evaluate the bioavailability and pharmacokinetics of two preparations of calcium folinate in healthy volunteers. Methods The randomized, crossed-over study was conducted in 18 healthy volunteers. After a single dose of administration （ containing 90 mg calcium folinate dispersed tablets）, the plasma levels of medicines were determined by HPLC. The AUC0-12 of both forms were compared by variance analysis and two-way one-sided t test. Results The main pharmacokinetics parameters of test and reference preparation were as followed ： tmax were （ 1.5 ± 0.0） h and （ 1.5 ± 0.0） h, Camx were （2295.51 ± 368.93） ng·mL^-1 and （2 139.53±189.67） ng·mL^-1, t1/2 were （2.19±0.16） h and （2.23 ± 0.17） h, AUC0-12 were （6 202.09 ±229.90） ng·mL^-1·h and （6 185.32 ±191.47 ） ng·mL^-1·h, and AUC0-∞ were （6 478.43 ± 250.69 ） ng·mL^-1·h and （ 6 478.63 ± 248. 10 ） ng·mL^-1·h, respectively. Conclusion The results showed that the two formulations were bioequivalent. The relative bioavailability of calcium folinate dispersed tablets was （100.13 ±5.39）%.