Pharmacokinetic Analysis of Phenytoin and Its Derivatives in Plasma and Brain in Rats
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概要
- 論文の詳細を見る
The derivatives of phenytoin (DPH) were synthesized by the reaction at 3 position of hydantoin ring with valproic acid and valeric acid, producing valproyl DPH (VPDPH) and valeroyl DPH (VADPH), respectively. These derivatives showed much higher lipid solubilities than that of DPH. Their distribution and elimination were compared to those of DPH. Additionally, the concentration profiles of the drugs in brain and plasma were analyzed with a modified 2-compartment model. DPH and its derivatives, without hydrolysis to DPH in blood, were found rapidly distributed into brain, although the distribution of derivatives was much less, probably due to the high protein binding capacities. The distribution of DPH and its derivatives into brain regions was similar to that into the cortex cerebri. VPDPH and VADPH were more rapidly eliminated from plasma and brain than DPH, giving smaller mean residence time (MRT) values (0.92 and 0.85 h) and much smaller cortex/plasma concentration ratio than those of DPH. The VPDPH and VADPH concentrations in the cerebrospinal fluid (CSF) were also much lower than that of DPH. The time course of plasma and brain concentrations of DPH and its derivatives after i.v. administration was successfully described by the modified 2-compartment models presented.
- 社団法人日本薬学会の論文
- 1993-10-15
著者
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岩城 正宏
近畿大学薬学部
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岩城 正宏
近畿大薬学部
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小木曽 太郎
Faculty of Pharmaceutical Sciences, Kinki University
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岩城 正宏
Faculty of Pharmaceutical Sciences, Kinki University
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谷野 公俊
近畿大薬学部
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田辺 元三
近畿大学薬学部
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谷野 公俊
Faculty of Pharmaceutical Sciences, Kinki University
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村岡 修
Faculty of Pharmaceutical Sciences, Kinki University
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田辺 元三
Faculty of Pharmaceutical Sciences, Kinki University
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村岡 修
Faculty Of Pharmaceutical Sciences Kinki University
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田邉 元三
近畿大薬
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小木曽 太郎
近畿大学 薬学部
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Tanino T
Kinki Univ. Osaka Jpn
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小木曽 太郎
近畿大 薬
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村岡 修
近畿大薬:近畿大薬総研
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