Enhanced Rectal Absorption of Amphotericin B Lyophilized with Glycyrrhizinate in Rabbits

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概要

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• The influence of bases and additives in the formulation for rectal absorption of amphotericin B (AMB) lyophilized with dipotassium glycyrrhizinate (GLYK) ws investigated using rabbits in relation to an in vitro release test. The release of AMB from the fatty base of Witepsol or a medium chain triglyceride (MCT) was markedly faster than that from the hydrophilic base of macrogol. The addition of polyoxyethylene (2) lauryl ether (POE(2)LE) into the fatty bases led to a marked increase in the release rate, wherease POE(9)LE or sodium lauryl sulfate resulted in a significantly lower release rate. Animals received rectally each of seven AMB formulatins of Witepsol H-15,macrogol, MCT with surfactants and aqueous solution. The absorption of the AMB lyophilized mixture with GLYK at a 1 : 9 molar ratio from a MCT base was significantly superior to that from macrogol. The addition of POE(2)LE into the MCT base resulted in a marked increase in bioavailability, showing the highest bioavailability of 4.9%. High serum levels of over 100 ng/ml of serum were maintained for 24 h following administration. The lowest bioavailability was 0.32% for the macrogol suppository. There was a good correlation between the release rate of AMB from the formulations and bioavailability. These results suggest that an AMB rectal formulation may provide a promising therapeutic alternative to infusion, taking into account the serum level of AMB exceeding the minimal inhibitory concentration of the infecting organism.

• 公益社団法人日本薬学会の論文
• 1998-08-15

著者

• Takahashi N

  Faculty Of Pharmaceutical Sciences Okayama University

• Tanaka M

  Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn

• YOTSUYANAGI Toshihisa

  Faculty of Pharmaceutical Sciences, Nagoya City University

• Koyama Osamu

  Kanagawa Laboratories Bristol-myers Squibb K.k.

• TANAKA Makoto

  Kanagawa Laboratories, Bristol-Myers Squibb K.K.,

• KUWAHARA Etsuhisa

  Kanagawa Laboratories, Bristol-Myers Squibb K.K.,

• TAKAHASHI Norimitsu

  Kanagawa Laboratories, Bristol-Myers Squibb K.K.,

• TAKAHASHI Masahiro

  Kanagawa Laboratories, Bristol-Myers Squibb K.K.

• Kuwahara E

  Kanagawa Laboratories Bristol-myers Squibb K.k.

• Tanaka M

  Kanagawa Laboratories Bristol-myers Squibb K.k.

• Yotsuyanagi Toshihisa

  Faculty Of Pharmaceutical Science Nagoya City University

• Takahashi M

  Kanagawa Laboratories Bristol-myers Squibb K.k.

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