Water-Soluble Prodrug of Vitamin E for Parenteral Use and Its Effect on Endotoxin-Induced Liver Toxicity

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概要

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• The acid salts of aminoalkanecarboxylic acid esters of d-α-tocopherol were in a previous in vitro study identified as prodrug candidates for a parenteral form of d-α-tocopherol. The disposition of d-α-tocopheryl N, N-dimethylaminoacetate hydrochloride (TDMA), the most potential candidate for the prodrug, after a single intravenous administration was investigated and compared with that of the d-α-tocopheryl acetate (TA) and dl-α-tocopherol, solubilized with HCO-60,in order to establish the utility as a prodrug for i.v. administration. The preventive effect of the prodrug against endotoxin (lipopolysaccharide (LPS))-induced liver lipid peroxidation was also investigated in mice. The plasma and liver levels of α-tocopherol (Toc) were increased rapidly after i.v. administration of the prodrug. The distribution of Toc and TDMA in the plasma and the liver at 1 h was as follows; 2.1±0.2 (plasma, Toc), 2.0±0.2 (plasma, TDMA), 32.8±2.9 (liver, Toc), and 35.3±6.5% of dose (liver, TDMA). The rapid and liver-selective uptake and liver-esterase specific regeneration characteristics of the prodrug enhance the delivery of Toc to liver. The liver availability of Toc after i.v. administration of TDMA, TA and Toc were 116,50 and 100%, respectively. The elevation of liver lipid peroxide induced with LPS was significantly suppressed to a normal range by a single i.v. postadministration of TDMA (over 10 mg/kg equivalent for Toc). These results indicated that the water-soluble and liver-esterase hydrolyzable derivative of Toc was a potential candidate for a parenteral prodrug which can thus achieve the systemic liver-specific delivery of Toc. Such effective and selective delivery of Toc into the liver can therefore lead to enhanced pharmacological efficacy against liver oxidative injury associated with free radicals.

• 公益社団法人日本薬学会の論文
• 1997-02-15

著者

• Takata Jiro

  Laboratory Of Drug Design And Drug Delivery Faculty Of Pharmaceutical Sciences Fukuoka University

• ITO Shigeru

  Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University

• TAKATA Jiro

  Faculty of Pharmaceutical Sciences, Fukuoka University

• KARUBE Yoshiharu

  Faculty of Pharmaceutical Sciences, Fukuoka University

• MATSUSHIMA Yoshikazu

  Kyoritsu College of Pharmacy

• NAGATA Yoshiko

  Kyoritsu College of Pharmacy

• Karube Yoshiharu

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Ito S

  Institute For Medical And Dental Engineering Tokyo Medical And Dental University

• YOSHIDA Keisuke

  Faculty of Pharmaceutical Sciences, Fukuoka University

• Takata Jiro

  Faculty Of Pharmaceutical Sciences Fukuoka University

• Matsuoka Yuji

  School Of Medicine Fukuoka University

• Nagata Y

  Kyoritsu College Of Pharmacy

• ITO Sanae

  Faculty of Pharmaceutical Sciences, Fukuoka University

• Matsushima Y

  Kyoritsu College Of Pharmacy

• Tanaka Jiro

  Faculty Of Marine Science Tokyo University Of Marine Science And Technology

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