Bolaji O O, Onyeji C O, Ogundaini A O, Olugbade T A, Ogunbona F A
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife, Nigeria.
Eur J Drug Metab Pharmacokinet. 1996 Jul-Sep;21(3):217-21. doi: 10.1007/BF03189716.
The pharmacokinetics and bioavailability of drotaverine was studied in 10 healthy volunteers after administration of single 80 mg oral and intravenous doses of the HCl salt of the drug, in a crossover fashion. Plasma and urine samples were analyzed for the unchanged drug by HPLC. The pharmacokinetic parameters, such as elimination half-life, plasma clearance, renal clearance and apparent volume of distribution, were not influenced by the route of drug administration. The drug was mainly eliminated by non-renal routes since renal clearance accounted for only 0.31 +/- 0.13% of the total plasma clearance. The absolute bioavailability was variable and ranged from 24.5-91% with a mean of 58.2 +/- 18.2% (mean +/- SD). It is suggested that the high variation in the bioavailability of drotaverine HCl after oral administration may result in significant interindividual differences in therapeutic response.
采用交叉试验设计，对10名健康志愿者单次口服和静脉注射80mg盐酸屈他维林后的药代动力学和生物利用度进行了研究。通过高效液相色谱法（HPLC）分析血浆和尿液样本中的原形药物。消除半衰期、血浆清除率、肾清除率和表观分布容积等药代动力学参数不受给药途径的影响。由于肾清除率仅占总血浆清除率的0.31±0.13%，药物主要通过非肾途径消除。绝对生物利用度存在差异，范围为24.5-91%，平均值为58.2±18.2%（平均值±标准差）。提示口服盐酸屈他维林后生物利用度的高度差异可能导致治疗反应的显著个体间差异。
