国产右旋布洛芬缓释胶囊在大鼠体内的药动学及生物利用度研究

摘要

目的 考察自制和市售右旋布洛芬缓释胶囊在大鼠体内的药动学性质与生物等效性.方法 建立反相高效液相色谱法,测定右旋布洛芬在血浆中的浓度,进行药动学和相对生物利用度研究.结果 自制和市售右旋布洛芬缓释胶囊的主要药动学参数Cmax分别为(1 173.87±281.68),(1 186.06±268.79) μg·mL-1;AUC(0-1)分别为(4 276.53±578.59),(4 489.83±645.73) mg·L-1·h;AUC(0-∞)分别为(5 095.58±683.82),(5 466.37±753.35)mg·L-1·h;tmax分别为(1.33±0.26),(1.58±0.49)h;各参数间比较差异无统计学意义(P＞0.05),以AUC(0-∞)计算自制右旋布洛芬缓释胶囊的相对生物利用度为(93.2±12.5)％.结论 自制右旋布洛芬缓释胶囊与市售制剂之间生物等效.%Objective To investigate the pharmacokinetics and bioavailability of self-prepared dexibuprofen sustained release capsules and reference formulation in rats. Methods An RP-HPLC method was established to determine the concentration of dexibuprofen in plasma. Dexibuprofen sustained release capsule was prepared, and its pharmacokinetic parameters and bioavailability in SD rats were studied after oral administration. Results The pharmacokinetics parameters of dexibuprofen showed that Cmax was (1173.87±281.68) and (1186.06±268.79) μg o mL-1, AUC(0-t)(4 276. 53±578.59) and (4 489.83±645.73) mg o L-1 o h, AUC(0-∞)(5 095.58±683. 82) and (5 466. 37±753. 35) mg o L-1 o h, tmax( 1. 33±O. 26) and ( 1. 58±0.49 ) h for self-prepared dexibuprofen sustained release capsules and reference formulation, respectively. There was no significant difference between the parameters of the two formulations ( P>0. 05). The relative bioavailability of self-prepared dexibuprofen sustained release capsules to reference formulation is (93.2±12.5)%. Conclusion The results of statistical analysis show that self-prepared dexibuprofen sustained release capsules and reference formulation are bioequivalent.