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Effect of instillation method on the absorption of phenolsulphonphthalein as a model drug from the liver and small intestinal serosal surface in rats


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タイトル: Effect of instillation method on the absorption of phenolsulphonphthalein as a model drug from the liver and small intestinal serosal surface in rats
著者: Nishida, Koyo / Yoshida, Yayoi / Mukai, Takahiro / Kawakami, Shigeru / Sakaeda, Toshiyuki / Nakashima, Mikiro / Sasaki, Hitoshi / Nakamura, Junzo
発行日: 2001年10月
出版者: Pharmaceutical Press
引用: Journal of Pharmacy and Pharmacology, 53 (10), 1341-1346, 2001
抄録: The aim of this study is to examine the effect of the instillation method on absorption of a drug from the liver and small intestinal serosal surface in rats. We performed continuous microinstillation via an infusion pump and bolus instillation via a syringe. Phenol red as a model was absorbed after continuous microinstillation of 2.35 mg in 235 ?L for 5 min on the liver and small intestinal serosal surface in rats with a significantly higher AUC of the plasma concentration profile until 60 min, compared with that after bolus instillation. A similar trend was observed after continuous microinstillation of 2.35 mg in 117.5 ?L for 2.5 min. The calculated absorption rate constants Ka after continuous microinstillation of phenol red based on a two-compartment model with first-order absorption were higher than those after bolus instillation on the liver and small intestinal serosal surface at either instillation concentration. Moreover, Ka was increased after continuous microinstillation of 2.35 mg in 117.5 ?L on either instillation site. In the comparison between instillation sites, instillation of phenol red on the liver surface resulted in 1.2 to 2.3-fold higher Ka, compared to small intestinal serosal surface. This tendency was marked after continuous microinstillation of 2.35 mg in 117.5 ?L. In conclusion, absorption could be enhanced by instilling a small amount of drug solution on the liver surface gradually and continuously, suggesting a promising approach for instillation site-selective drug delivery in the peritoneal cavity.
URI: http://hdl.handle.net/10069/6675
ISSN: 00223573
PubMed ID: 11697541
資料タイプ: Journal Article
原稿種類: author
出現コレクション:050 学術雑誌論文

引用URI : http://hdl.handle.net/10069/6675

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