INTESTINAL ABSORPTION MECHANISMS OF γ-BUTYROLACTONE-γ-CARBONYL-L-HISTIDYL-L-PROLINAMIDE CITRATE (DN-1417) AND THYROTROPIN-RELEASING HORMONE (TRH)

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概要

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• The absorption mechanisms of γ-butyrolactone-γ-carbonyl-L-histidyl-L-prolinamide citrate (DN-1417) and thyrotropin-releasing hormone (TRH) were studied in the rat. In situ absorption experiments were carried out by radioimmunoassay, and experiments using everted sacs of small intestine were by radioactivity measurements with ^<14>C-labeled DN-1417 or ^3H-labeled TRH in the low concentration range of drug and by a high pressure liquid chromatography in the rather high concentration range of drug. The site specificity of absorption in the small intestine of rats could not be found with DN-1417 whereas TRH-T was absorbed from only the upper part of small intestine. Dose-proportional absorption of of DN-1417 was observed in experiments of in situ as well as in vitro. Dose-proportional transfer of DN-1417 through the everted small intestine was also found within the concentration range from 120 ng/ml to 27 mg/ml, whereas the transfer ratio of TRH decreased with increase in the concentration of TRH. DN-1417 transfer from mucosal to serosal fluid was not inhibited by the replacement of medium Na ions by K ions, pretreatment of intestinal mucosa with HgCl_2,the existence of an oligopeptide, or the existence of β-lactam antibiotics which had been reported to be absorbed by active transport or carrier-mediated transport systems. While, TRH transfer was inhibited by the replacement of medium Na ions by K ions, pretreatment of intestinal mucosa with HgCl_2,the existence of an oligopeptide, and the existence of β-lactam antibiotics. From these results, it was concluded that DN-1417 transfer through the small intestine was mainly due to the simple diffusion, and the contribution of the carrier-mediated transport to TRH transfer through the small intestine was not disregarded

• 公益社団法人日本薬学会の論文

著者

• Shimamoto Tsugio

  Central Research Division Takeda Chemical Industries Ltd.

• Kitamori Nobuyuki

  Central Research Division Takeda Chemical Industries Ltd.

• YOKOHAMA SHIGEHARU

  Central Research Division, Takeda Chemical Industries, Ltd.

• Yoshioka Toshio

  Central Research Division Takeda Chemical Industries Ltd.

• Shimamoto T

  Central Research Division Takeda Chemical Industries Ltd.

• KAMAD AKIRA

  Faculty of Pharmaceutical Science, Osaka University

• Kamad Akira

  Faculty Of Pharmaceutical Science Osaka University

• Yokohama Shigeharu

  Central Research Division Takeda Chemical Industries Ltd.

関連論文

• DESENSITIZATION OF GONADOTROPIN-RELEASING RESPONSE FOLLOWING VAGINAL CONSECUTIVE ADMINISTRATION OF LEUPROLIDE IN RATS
• ABSORPTION OF THYROTROPIN-RELEASING HORMONE AFTER ORAL ADMINISTRATION OF TRH TARTRATE MONOHYDRATE IN THE RAT, DOG AND HUMAN
• RADIOIMMUNOASSAY OF THYROTROPIN-RELEASING HORMONE (TRH) IN RAT, DOG, AND HUMAN BLOOD
• INTESTINAL ABSORPTION MECHANISMS OF THYROTROPINRELEASING HORMONE
• INTESTINAL ABSORPTION MECHANISMS OF γ-BUTYROLACTONE-γ-CARBONYL-L-HISTIDYL-L-PROLINAMIDE CITRATE (DN-1417) AND THYROTROPIN-RELEASING HORMONE (TRH)
• ABSORPTION OF γ-BUTYROLACTONE-γ-CARBONYL-L-HISTIDYL-L-PROLINAMIDE CITRATE (DN-1417), AN ANALOG OF THY-ROTROPIN-RELEASING HORMONE, IN RATS AND DOGS
• BLOOD LEVEL AND BRAIN DISTRIBUTION OF THYROTROPIN-RELEASING HORMONE (TRH) DETERMINED BY RADIOIMMUNOASSAY AFTER INTRAVENOUS ADMINISTRATION IN RATS

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