In Vitro Transport of Sodium Diclofenac across Rat Abdominal Skin : Effect of Selection of Oleaginous Component and the Addition of Alcohols to the Vehicle
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概要
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The in vitro percutaneous transport of sodium diclofenac from various oil vehicles was examined using rat abdominal skin as a model skin membrane. The overall transport of diclofenac through the skin from the oleaginous vehicles was very poor because of a poor solubility of sodium diclofenac in nonpolar oils. To increase the solubility and the permeability of sodium diclofenac, ethanol and n-octanol were added to each oil (designated as the formulated vehicles). The addition of ethanol and n-octanol to the nonpolar vehicles resulted in an extreme increase in drug solubility in each vehicle, with a remarkable increase in the permeation of diclofenac. The effects of oil components in the formulated vehicle on the permeation of diclofenac across the skin were in the following order : squalane≧squalene>liquid paraffin>middle chain triglyceride>olive oil>castor oil.In order to clarify the reason for the differences in permeation of diclofenac from these formulated vehicles, the release of diclofenac and n-octanol from these vehicles in vitro was studied. The release rates of n-octanol from the formulated vehicles were in the following order : liquid paraffin>squalene≧squalane>middle chain triglyceride≧olive oil>castor oil. On the other hand, a linear correlation was observed between the initial release rate of diclofenac from the formulated vehicle and the in vitro permeation of diclofenac through the rat skin. Thus, the oil component in the formulated vehicle effects the release of the drug and the enhancer from the vehicle to the skin. The transport rate of diclofenac from the formulated vehicle of squalane at the steady state proportionally increased with an increase of drug concentration, and the lag times were not influenced by a change of the drug concentration in the formulated vehicles. Therefore, it may be suggested that the intrinsic permeation of diclofenac through the skin is not influenced by the concentration of sodium diclofenac in the vehicle. From these results, it is considered that the important factors in increasing the skin permeation of a drug from an oil vehicle are to select oils which have a low affinity for the drug and enhancer, and to increase the drug concentration in the oil.
- 社団法人日本薬学会の論文
- 1991-01-25
著者
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高橋 幸一
武庫川女子大学薬学部
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鎌田 皎
Faculty Of Pharmaceutical Sciences Osaka University
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水野 亘恭
Faculty of Pharmaceutical Sciences, Osaka University
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西畑 利明
カンサス大学
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吉富 博則
Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University
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西畑 利明
Pharmaceutical Chemistry Department, The University of Kansas
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吉富 博則
福山大学
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水野 亘恭
武庫川女子大学薬学部
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高橋 幸一
Faculty of Pharmaceutical Sciences, Mukogawa University
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西畑 利明
Pharmacy Research Upjohn Tsukuba Research Laboratories
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玉川 智子
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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Rytting J.
カンサス大学
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加多木 豊史
Faculty of Pharmaceutical Sciences, Mukogawa Women's University
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RYTTING J.
Pharmaceutical Chemistry Department, The University of Kansas
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鎌田 皎
大阪大学
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高橋 幸一
武庫川女子・薬
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高橋 幸一
武庫川女子大学薬学部薬剤学研究室
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加多木 豊之
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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Katagi T
School Of Pharmaceutical Sciences Mukogawa Women 's University
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加多木 豊史
Faculty Of Pharmaceutical Science Mukogawa University
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高橋 幸一
Faculty Of Pharmaceutical Sciences Mukogawa University
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水野 亘恭
武庫川女子大・薬
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水野 亘恭
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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玉川 智子
Faculty Of Pharmaceutical Sciences Mukogawa Women's University
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西畑 利明
Pharmaceutical Chemistry Department The University Of Kansas
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