Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide

Masateru Miyake, Takanori Minami, Yoshikazu Oka, Naoki Kamada, Hiroyuki Yamazaki, Yusuke Kato, Tadashi Mukai, Hajime Toguchi, Masaaki Odomi, Ken Ichi Ogawara, Kazutaka Higaki, Toshikiro Kimura

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

We previously reported that the fatty base suppository containing sodium laurate (C12) and taurine (Tau)(C12-Tau suppository) could enhance the colonic absorption of rebamipide, a poorly water-soluble and poorly absorbable drug, without any serious mucosal damages in rats. In the preset study, in order to make C12-Tau suppositories available for practical use, the scaling-up studies of animal and formulation size were performed, compared with the suppositories containing sodium caprate (C10) (C10 suppository) at the same amounts as those contained in the commercial products. Twenty-mg C12 improved the dissolution of rebamipide from suppository remarkably and the addition of 30-mg Tau only slightly decreased the dissolution rate. The absorption of rebamipide from rabbit rectum was more markedly improved by suppositories containing C12 than C10 suppositories. Although Tau tended to attenuate the absorption-enhancing effect of C12, several C12-Tau suppositories kept high bioavailability values, which were much higher than control. Histopathological studies showed that Tau exerted the cytoprotective action and that C12-Tau suppositories were better than C10 suppositories in safety. Considering the balance between efficacy and safety, the suppository containing 10- or 20-mg C12 with 30-mg Tau is better than C10 suppositories as commercial products and could be promising for practical use in human.

Original languageEnglish
Pages (from-to)330-335
Number of pages6
JournalBiological and Pharmaceutical Bulletin
Volume29
Issue number2
Publication statusPublished - Feb 2006

Fingerprint

lauric acid
Suppositories
Taurine
Rectal Absorption
rebamipide

Keywords

  • Absorption enhancer
  • Cytoprotection
  • Histopathology
  • Rabbit
  • Suppository
  • Taurine

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide. / Miyake, Masateru; Minami, Takanori; Oka, Yoshikazu; Kamada, Naoki; Yamazaki, Hiroyuki; Kato, Yusuke; Mukai, Tadashi; Toguchi, Hajime; Odomi, Masaaki; Ogawara, Ken Ichi; Higaki, Kazutaka; Kimura, Toshikiro.

In: Biological and Pharmaceutical Bulletin, Vol. 29, No. 2, 02.2006, p. 330-335.

Research output: Contribution to journalArticle

Miyake, M, Minami, T, Oka, Y, Kamada, N, Yamazaki, H, Kato, Y, Mukai, T, Toguchi, H, Odomi, M, Ogawara, KI, Higaki, K & Kimura, T 2006, 'Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide', Biological and Pharmaceutical Bulletin, vol. 29, no. 2, pp. 330-335.
Miyake, Masateru ; Minami, Takanori ; Oka, Yoshikazu ; Kamada, Naoki ; Yamazaki, Hiroyuki ; Kato, Yusuke ; Mukai, Tadashi ; Toguchi, Hajime ; Odomi, Masaaki ; Ogawara, Ken Ichi ; Higaki, Kazutaka ; Kimura, Toshikiro. / Optimization of suppository preparation containing sodium laurate and taurine that can safely improve rectal absorption of rebamipide. In: Biological and Pharmaceutical Bulletin. 2006 ; Vol. 29, No. 2. pp. 330-335.
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