Pharmaceutical Approach to HIV Protease Inhibitor Atazanavir for Bioavailability Enhancement Based on Solid Dispersion System(Biopharmacy)

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概要

• 論文の詳細を見る

• Atazanavir (ATV) is a low oral bioavailability (BA) compound and, clinically, is generally coadministrated with ritonavir (RTV), which boosts the oral BA of ATV by inhibiting cytochrome P450 (CYP) 3A, and P-glyco-protein (Pgp) via the same metabolic pathway. However, depending on pharmacokinetic interaction, RTV-boosted ATV has great potential for other comedication. In this study we demonstrated the pharmaceutical approach to BA improvement of ATV without RTV in rats, based on the solid dispersion system using sodium lauryl sulfate (SLS) as a carrier and Gelucire^[○!R] 50/13 as an absorption enhancer. ATV solid dispersions in SLS were prepared by a conventional solvent method and, at ratios of ATV to SLS of 1:2 and 1:3, were demonstrated to form an amorphous state in powder X-ray diffraction (PXRD) analysis and exhibited 2.26- and 2.36-fold improvement in a dissolution test in comparison to bulk ATV, respectively. After oral administration to rats, ATV solid dispersion in SLS at a ratio of 1:2 showed a 3.5-fold increase in BA compared with bulk ATV. Moreover, the addition of Gelucire 50/13 to ATV solid dispersion, at a total ratio of Gelucire 50/13, ATV and SLS 1:1:2 gave 7.0- and 4.7-fold increase in C_<max> and BA compared with bulk ATV, respectively, when the relative BA to RTV-boosted ATV reached 93%. The results in this study proved that a pharmaceutical approach could improve the bioavailability of ATV without pharmacokinetic interaction with RTV.

• 公益社団法人日本薬学会の論文
• 2007-04-01

著者

• SUGIOKA Nobuyuki

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• HARAYA Kenta

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• FUKUSHIMA Keizo

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• TAKADA Kanji

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• Shibata Nobuhito

  Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Doshisha Womens College of Liber

• Wada Ayako

  Department Of Curriculum And Instruction Faculty Of Education And Regional Sciences Tottori Universi

• Takada Kanji

  Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.

• Takada K

  Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories

• Haraya Kenta

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• Sakurai Yuichi

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• Wada Ayako

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• TERASAKA Shuichi

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• KODERA Satoshi

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• SEKI Yuichiro

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• ITO Yukako

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• Kodera Satoshi

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• Takada Kanji

  Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories

• Terasaka Shuichi

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• Sugioka Nobuyuki

  Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.

• Seki Yuichiro

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• Takada K

  Kyoto Pharmaceutical Univ. Kyoto Jpn

• Fukumoto Kyoko

  Department Of Pharmacokinetics Kyoto Pharmaceutical University

• Kodera Satoshi

  Department Of Cardiology Asahi General Hospital

• Shibata Nobuhito

  Dep. Of Pharmacokinetics Kyoto Pharmaceutical Univ.

• Fukushima K

  大正製薬(株)開発研究所薬物動態研究室

• Inoue Yuji

  Department of Pharmacokinetics, Kyoto Pharmaceutical University

• Shibata Nobuhito

  Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Doshisha Women's College of Liberal Arts

• ITO Yukako

  Department of Dermatology and Plastic Surgery, Head & Neck Surgery

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