利福平的剂型与生物利用度的研究STUDIES ON DOSAGE FORMS OF RIFAMPICIN AND THEIR BIOAVAILABILITY
蔡玉珉;杨乐荫;王喜进;童寅生;孙鑑堂;李暮春;林东海;林学勤;刘志彬;
Cai Yumin et al Department of Pharmacy
摘要(Abstract):
本文研究了利福平不同剂型的生物利用度。用狗,家兔和健康人做了对比实验,发现利福平的脂肪性基质口服制剂的生物利用度较胶囊剂、片剂、栓剂都高,且对肝脏的毒性也较小。用非模型矩量分析法求出的AUC(0→∞)和MRT可知:450mg的脂肪性基质口服制剂可以获得与600mg胶囊剂相似的血药水平。因而可以推测利福平的脂肪性基质口服制剂的剂量较胶囊剂可降低1/4—1/3。
The bioavailability of different dosage forms of rifampicin were studied in dogs,rabbits and healthy human volunteers using comparative experimental designs.It was found that the bioavailability of aliphatic base preparation of the drug was greater than that of its commonly-used preparations in the dosage form of capsules,tablets and suppositories,and that the toxic effect on liver was low.AUC(0→∞)和MRT可知:450mg的脂肪性基质口服制剂可以获得与600mg胶囊剂相似的血药水平。因而可以推测利福平的脂肪性基质口服制剂的剂量较胶囊剂可降低1/4—1/3。
The bioavailability of different dosage forms of rifampicin were studied in dogs,rabbits and healthy human volunteers using comparative experimental designs.It was found that the bioavailability of aliphatic base preparation of the drug was greater than that of its commonly-used preparations in the dosage form of capsules,tablets and suppositories,and that the toxic effect on liver was low.AUC(0→) and MRT(Mean Residence Time)were calculated using the model-independent moment analysis method.The aliphatic base preparation containig 450mg of rifampicin could give the same drug level in plasma as the capsule with 600mg.It was,herefore,inferred that the amount of rifampicin administered in aliphatic base reparation can be decreased by 1/4—1/3 compared with that in capsule.
关键词(KeyWords):
利福平;生物利用度;非模型矩量分析法;曲线下面积;平均滞留时间
Rifampicin; Bioavailability; Model-independent moment analysis method; AUC; MRT
基金项目(Foundation):
作者(Authors):
蔡玉珉;杨乐荫;王喜进;童寅生;孙鑑堂;李暮春;林东海;林学勤;刘志彬;
Cai Yumin et al Department of Pharmacy
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