Development of an Oral Formulation of Azetirelin, a New Thyrotropin-Releasing Hormone (TRH) Analogue, Using n-Lauryl-β-D-maltopyranoside as an Absorption Enhancer

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概要

• 論文の詳細を見る

• The effects of formulation factors on the enhancement of colonic absorption of azetirelin by n-lauryl-β-D-maltopyranoside (LM) were studied in rats. Coadministration of LM with a small volume of azetirelin solution to the proximal colon increased the AUC of the drug by 8.7-fold. There were on significant differences in the LM-in-duced absorption profiles of azetirelin between unligated and ligated colon. The addition of a viscous polymer to the drug solution, which delayed the in vitro release of both azetirelin and LM, reduced the promoting effects of LM. These results suggest that the action of LM is not affected by sample spreading in the colonic lumen, whereas a rapid release of both azetirelin and LM from the formulation is necessary to maximize the efficacy of LM. Utilizing the balloon sonde method, the effects of LM were also confirmed in the colonic loop of dogs. Based on these results, an enteric capsule formulation of azetirelin containing LM and citric acid (CA), a potential inhibitor of the bacterial degradation of azetirelin in the distal intestine, was prepared and its performance was evaluated in fasted dogs. The bioavailability of azetirelin after the oral administration of this enteric capsule with LM and CA was 43.5% compared with a bioavailability of 14.9% in capsule without LM and CA. Therefore, the delivery of azetirelin and LM to the lower intestine, together with a rapid release of capsule contents, are feasible for the improved peroral bioavailability of azetirelin.

• 公益社団法人日本薬学会の論文
• 1999-06-15

著者

• YAMAMOTO Akira

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• MURAKAMI Masahiro

  Department of Synthetic Chemistry and Biological Chemistry, Graduate School of Engineering, Kyoto Un

• MATSUMOTO Keiko

  Department of Geriatric Medicine, Osaka University Medical School

• 佐々木 功

  山之内製薬株式会社

• MURANISHI Shozo

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• FUJITA Takuya

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• Fujita T

  Division Of Oral Cytology And Cell Biology Department Of Developmental And Reconstructive Medicine N

• FUJITA Takuya

  Ritsumeikan University College of Information Science and Engeneering

• Yamamoto Akira

  Dep. Of Biopharmaceutics Kyoto Pharmaceutical Univ.

• ITO Yukiko

  Department of Gastroenterology, Japanese Red Cross Medical Center

• Fujita T

  Ritsumeikan University College Of Information Science And Engeneering

• Fujita Takuya

  Department Of Basic Pharmaceutics Faculty Of Pharmaceutical Sciences Kyoto University

• Fujita T

  Showa College Of Pharmaceutical Sciences

• Murakami Masahiro

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Ito Yukiko

  Department Of Gastroenterology Japanese Red Cross Medical Center

• Fukushima Tohru

  Department Of Pharmacology Faculty Of Pharmaceutical Sciences Setsunan University

• SAKAI Isao

  Novel Pharmaceutical Laboratories, Yamanouchi Pharmaceutical Co., Ltd.,

• TOZAKI Hideyuki

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• MATASUMOTO Keiko

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• Sakai Isao

  Novel Pharmaceutical Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• Tanaka Hideaki

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• 村西 昌三

  京都薬大

• Muranishi Shozo

  Department Of Biopharmaceutics Kyoto Pharmaceutical University:exploratory Development Laboratories

• Muranishi Shozo

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Ito Y

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Matasumoto Keiko

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Yamamoto Akira

  Department Of Biopharmaceutics Kyoto Pharmaceutical University

• Yamamoto Akira

  Department Of Anatomy School Of Medicine University Of Tokushuma

• Murakami Masahiro

  Department Of Aquatic Bioscience Graduate School Of Agricultural And Life Sciences The University Of

• Sasaki Isao

  Novel Pharmaceutical Laboratories, Yamanouchi Pharmaceutical Co., Ltd.,

• Yamamoto Akira

  Department Of Anatomy School Of Medicine University Of Tokushima

• ITO Yukiko

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• MURAKAMI MASAHIRO

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• Matsumoto Keiko

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• MURAKAMI Masahiro

  Department of Anatomy, Kurume University School of Medicine

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