普瑞巴林缓释片在中国健康男性受试者的人体相对生物利用度及生物等效性研究

发布时间：2018-08-27 08:13

【摘要】：目的研究中国健康男性受试者餐后口服两种不同规格的普瑞巴林缓释片与空腹服用普瑞巴林胶囊(乐瑞卡溲)后的相对生物利用度及生物等效性。方法 24例健康男性受试者按单中心、随机、开放、3周期交叉设计,分别餐后单次给予受试药品T1普瑞巴林缓释片330 mg、餐后单次给予受试药品T2普瑞巴林缓释片330 mg或者空腹2次给予参比药品R普瑞巴林胶囊300 mg,用液质联用法(LC-MS/MS)测定给药后普瑞巴林的血浆浓度,计算主要药代动力学参数,评价两种受试药品相对于参比药品的相对生物利用度及生物等效性。结果服用受试药品T1、T2和参比药品R后,普瑞巴林的主要药代动力学参数为:C_(max)为(4137.92±802.13),(3761.67±516.79),(5792.92±828.34)ng·m L~(-1);tmax为(9.83±2.04),(9.75±2.15),(12.81±0.24)h;AUC_(last)为(64467.78±11266.17),(61434.44±9684.92),(61730.01±6750.94)ng·h·m L~(-1);AUC_(inf)为(65049.66±11405.80),(62019.33±9858.38),(62292.49±6903.74)ng·h·m L~(-1);t1/2为(6.03±0.59),(6.16±0.49),(5.85±0.55)h。受试药品T1与参比药品R的平均相对生物利用度F(AUC_(last))为(104.32±13.05)%,F(AUC_(inf))为(104.31±12.95)%;受试药品T2与参比药品的平均相对生物利用度F(AUC_(last))为(99.58±11.17)%,F(AUC_(inf))为(99.61±11.14)%。受试药品T1、T2与参比药品R的C_(max)和AUC比值的90%置信区间均在80.00%~125.00%。结论餐后口服两种不同规格的普瑞巴林缓释片330 mg和空腹服用普瑞巴林胶囊300 mg后,普瑞巴林的体内暴露量等效,受试药品发挥了很好的缓释特性。
[Abstract]:OBJECTIVE To study the relative bioavailability and bioequivalence of pregabalin sustained-release tablets and pregabalin capsules in Chinese healthy male volunteers. T1 pregabalin sustained-release tablets 330 mg, T2 pregabalin sustained-release tablets 330 mg after meals or R pregabalin capsules 300 mg twice on an empty stomach. Plasma concentrations of pregabalin after administration were determined by liquid chromatography-mass spectrometry (LC-MS/MS), main pharmacokinetic parameters were calculated, and the relative pharmacokinetics of the two drugs were evaluated. Relative bioavailability and bioequivalence. Results After taking T1, T2 and R, the main pharmacokinetic parameters of pregabalin were as follows: C_ (max) was (4137.92 (+ 802.13)), (3761.67 (+ 516.79)), (5792.92 (+ 828.34) ng (- 1); Tmax was (9.83 (+ 2.04)), (9.75 (+ 2.15)), (12.81 (+ 0.24) h; AUC (+ last) was (64467.78 (+ 11266.17)), and (5792.92 (+ 828.34) ng (- 1). (61434.44 [9684.92 [(61434.44 [9684.92], (61730.01 [(67730.01 [6750.94) ng (~ (-1), (61730.01 [6750.94) ng (-1)], (AUC (inf) was (650409.69.66 [11405.80), (62 019.33 [9858.38), (62 2929 29.33 [(62 292 292.49 [6.49 [(690.49.49 [6903.74.74.74) ng [h (-1), (6.03 [(6.03 [(6.16 The last value was (104.32 13.05)% and the F (AUC_ (inf)) value was (104.32 13.05)%. The average relative bioavailability F (AUC_ (last)) and F (AUC_ (inf)) of T2 and reference drugs were (99.58 11.17)% and (99.61 (11.14)%. The confidence intervals of C_ (max) and AUC ratio of T1, T2 and reference drug R were 80.00% ~ 125.00%. Conclusion Two different specifications of sustained-release tablets of pregabalin were administered orally after meal. After taking pregabalin capsule 300 mg on an empty stomach, the dose of pregabalin was equivalent to that of pregabalin in vivo. The drug exhibited good sustained-release characteristics.
【作者单位】：中南大学湘雅三医院临床药理中心;中南大学湘雅三医院药学部;
【基金】：国家国际科技合作专项基金资助项目(2014DFA30900) 国家自然科学基金青年基金资助项目(81302851)
【分类号】：R969

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