曲尼司特缓释胶囊剂及其药物动力学研究

Studies on Tranilast Surstained-Release Capsules and Their Pharmacokinetics in Healthy Volunteers

研制了曲尼司特缓释胶囊剂,建立了高效液相色谱测定血药浓度的方法。以市售胶囊剂为对照品,研究了自制缓释胶囊剂在6名健康志愿受试者体内药物动力学。结果表明曲尼司特缓释胶囊剂和市售胶囊剂在人体内的药动学参数分别为C_(max)∶29.1μg/ml,T_(max)∶5.5h,MRT∶14.352h,AUC∶462.315h·μg/ml和C_(max)∶34.2μg/ml,T_(max)∶3.5h,MRT∶10.236h,AUMC∶4293.582h^2·μg/ml,419.46h·μg/ml。本品的相对生物利用度为110.22%。

Tranilast custained-release capsules were developed by the one-step spheronization and pan coating technique. The results indicated that the TSRC were able to produce a sustained release of the drug for 12h. The pharmcokinetie parameters C_(max), T_(max), MRT, AUMC and AUC of TSRC were 29. 1μg/ml, 5.5h, 14.352h, 6635.145h^2·μg/ml,462.315h·μag/ml, respectively.