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大鼠腹膜透析与肠道透析过程中茶碱和苯巴比妥的药代动力学比较

Pharmacokinetics of theophylline and phenobarbital during peritoneal dialysis compared with intestinal dialysis in rats.

作者信息

Arimori K, Hashimoto Y, Nakano M

机构信息

Department of Pharmacy, Kumamoto University Hospital, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1990 Nov;38(11):3177-9. doi: 10.1248/cpb.38.3177.

Abstract

The transfer rates of theophylline and phenobarbital from blood into the peritoneal cavity were investigated after their intravenous administrations at a dose of 10 mg/kg each in rats. Appreciable amounts of both drugs were transported into the dialysate with their transfer rates decreasing as the serum concentrations declined. The average amount of theophylline transferred into the dialysate was 17% and 24% of dose in 2 and 4 h, respectively, while that of phenobarbital was 13% and 45% of dose in 2 and 8 h, respectively. The amounts appeared to be greater than those transported into the intestinal lumen which was previously reported by the authors. Peritoneal dialysis decreased the serum half-life and the area under the serum concentration-time curve (AUC) value of theophylline from 2.1 to 1.5 h and from 38 to 26 micrograms.h/ml, respectively and increased the total body clearance by 47% as compared with the control. The dialysis also decreased the serum half-life and the AUC value of phenobarbital from 8.3 to 5.3 h and from 116 to 83 micrograms.h/ml, respectively and increased the total body clearance by 112% as compared with the control. Overall, the effectiveness of peritoneal dialysis in removing theophylline and phenobarbital appears to be not very different from that of intestinal dialysis with oral activated charcoal which has been previously reported by the authors in spite of the difference in transport into the intestinal lumen and peritoneum.

摘要

在大鼠静脉注射剂量均为10mg/kg的茶碱和苯巴比妥后,研究了它们从血液到腹腔的转运速率。两种药物均有相当数量转运至透析液中,其转运速率随血清浓度下降而降低。茶碱转运至透析液中的平均量在2小时和4小时分别为剂量的17%和24%,而苯巴比妥在2小时和8小时分别为剂量的13%和45%。这些量似乎大于作者先前报道的转运至肠腔的量。与对照组相比,腹膜透析使茶碱的血清半衰期从2.1小时降至1.5小时,血清浓度-时间曲线下面积(AUC)值从38μg·h/ml降至26μg·h/ml,总体清除率增加47%。透析还使苯巴比妥的血清半衰期从8.3小时降至5.3小时,AUC值从116μg·h/ml降至83μg·h/ml,总体清除率与对照组相比增加112%。总体而言,尽管茶碱和苯巴比妥转运至肠腔和腹膜的量存在差异,但腹膜透析清除这两种药物的效果似乎与作者先前报道的口服活性炭进行肠道透析的效果没有太大不同。

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