Tsujiyama T, Suzuki N, Kuriki T, Kawata M, Goto S
Pharma Research Laboratories, Hoechst Japan Limited, Saitama.
J Pharmacobiodyn. 1990 Jan;13(1):1-9. doi: 10.1248/bpb1978.13.1.
Hydroxypropylcellulose (HPC)-ethylcellulose (EC) microcapsules containing piretanide prepared by a solvent evaporation technique, were evaluated on pharmacokinetic, pharmacodynamic and pharmacological parameters in spontaneously hypertensive rats (SHR). HPC-EC10 (5:3) microcapsules showed sustained plasma piretanide levels and almost the same AUC (area under the curve) as compared with piretanide solution. Effect of treatment with the microcapsules (single oral administration per day in doses of 10 and 30 mg/kg) and the solution (double oral administration per day in doses of 5 and 15 mg/kg) was examined for 4 weeks on urine volume and urinary electrolytes excretion and blood pressure. The microcapsules and solution induced dose-dependent diuresis throughout the experimental period and a reduction in blood pressure from 2 weeks of the treatment. HPC-EC10 (5:3) microcapsules containing piretanide were satisfactory as a sustained-release preparation in the light of the anti hypertensive effect even at a half frequency of daily dosing of the solution.
采用溶剂蒸发技术制备了含吡咯他尼的羟丙基纤维素（HPC）-乙基纤维素（EC）微胶囊，并在自发性高血压大鼠（SHR）上对其药代动力学、药效学和药理学参数进行了评估。与吡咯他尼溶液相比，HPC-EC10（5:3）微胶囊显示出持续的血浆吡咯他尼水平，且曲线下面积（AUC）几乎相同。研究了微胶囊（每天单次口服给药，剂量为10和30mg/kg）和溶液（每天两次口服给药，剂量为5和15mg/kg）治疗4周对尿量、尿电解质排泄和血压的影响。在整个实验期间，微胶囊和溶液均引起剂量依赖性利尿作用，且从治疗2周起血压开始降低。含吡咯他尼的HPC-EC10（5:3）微胶囊作为一种缓释制剂，即使每日给药频率为溶液的一半，其降压效果也令人满意。
