Preparation of Liposome-Encapsulated Anti-tumor Drugs ; Relationship between Lipophilicity of Drugs and in Vitro Drug Release
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概要
- 論文の詳細を見る
Liposomal encapsulation of drugs by a reverse-phase evaporation vesicle (REV) method was carried out, and the relation between the in vitro release rates and the lipophilicity of drugs was investigated. Anti-tumor drugs such as carboquone (CQ), nimustine (ACNU), nimustine hydrochloride (ACNU-HCl), cytosine arabinoside (Ara-C), 5-fluorouracil (5-FU) and related compounds were used as model drugs. Encapsulation of the drugs in liposomes was concluded to have no relation with the partition coefficients of the drugs, whereas the in vitro release rate was highly correlated to the partition coefficient and it was evident that the drug was released more slowly when the partition coefficient was lower. Therefore, to achieve sustained release of a drug by means of liposomal encapsulation, it would be necessary to decrease the partition coefficient of the drug by converting it into the hydrochloride form, as in the case of ACNU, or by forming the sodium salt of the drug, if the drug has a carboxylic acid group.
- 公益社団法人日本薬学会の論文
- 1984-05-25
著者
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岡田 隆三
Product Development Laboratories Sankyo Company Ltd.
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上田 省吾
Product Development Laboratories Sankyo Co. Ltd.
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上田 省吾
Product Development Laboratories Sankyo Company Ltd.
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塚田 和弘
Product Development Laboratories, Sankyo Company, Ltd.
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塚田 和弘
Product Development Laboratories Sankyo Company Ltd.
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