盐酸丙哌维林散在健康人体内的生物等效性研究

Bioequivalence of Two Oral Formulations of Propiverine Hydrochloridein Healthy Volunteer

目的评价盐酸丙哌维林在健康人体内的相对生物利用度及生物等效性。方法受试者随机、自身双交叉、单剂量口服受试制剂和参比制剂20mg,采用液相-质谱(LC-MS)法测定血浆中药物浓度,药代动力学参数通过DAS软件处理获得。结果两种制剂的峰浓度(Cmax)分别为(63.47±25.46)ng/mL和(61.51±22.31)ng/mL,达峰时间(Tmax)分别为(1.7±0.7)h和(1.7±0.7)h,半衰期(t1/2)分别为(12.68±4.11)h和(12.35±3.09)h,0-tn药时曲线下面积AUC0-tn为(827.62±370.02)ng/(mL·h)和(804.76±380.73)ng/(mL·h),0-∞药时曲线下面积AUC0-∞分别为(881.77±412.22)和(848.63±409.22)ng/(mL·h);受试制剂的相对生物利用度为(111.22±37.21)%。结论石家庄市华新制药厂研制的盐酸丙哌维林散与其生产的盐酸丙哌维林片具有生物等效性。

Objective To study the bioavailability and bioequivalence of the tested and reference propiverine hydrochloride, two oral formulations of tablets and powders, in healthy male volunteers. Methods According to the crossover design, each volunteer was orally given 20 mg propiverine hydrochloride. The plasma concentrations were determined by LC/MS. The pharmacokinetic parameters were obtained using DAS program. Results Cmax were（63.47±25.46）ng/mL and（61.51 ±22.31）ng/mL, Tmax were（1.7±0.7）h and （1.7±0.7）h, T1/2 were （12.68± 4.11）h and （12.35±3.09）h, AUC0-tn were （827. 62 ±370. 02）ng/（mL · h） and （804. 76 ±380. 73）ng/（mL · h）, AUC0-∞ were （881.77± 412.22） and （848.63±409.22）ng/（mL · h） respectively. The relative bioavailability was （111.22 ±37.21）%. The data of the reference and tested drugs were up to the standard of bioequivalence as shown by F test. Conclusion The two dosage formulations of propiverine hydrochloride are bioequivalent.