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Decanoic Acid Induced Enhancement of Rectal Absorption of Hydrophilic Compounds in Rats

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Abstract

The enhancing effect of decanoic acid (CIO) on the rectal absorption of phenolsulfonphtalein (PSP) was analyzed with a pharmacokinetic model. The transfer index of PSP from the rectal lumen to the epithelial layer in the presence of C10 was proportional to the product of the C10 disappearance rate from the rectal lumen and its calcium ion sequestration capacity. The enhancement of rectal PSP absorption by different doses of C10 was also predictable by using a permeability index, Pa, of PSP, which was defined as a proportionality constant relating transfer index and the product value described above. The Pa values of various hydrophilic compounds with different molecular weights were also estimated from their rectal bioavailability in the presence of C10. A linear relationship was observed between Pa values and reciprocal values of the square root of individual molecular weight. These findings suggest that the Pa index is related to the permeant’s diffusion coefficient through paracellular aqueous openings formed by C10.

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REFERENCES

  1. N. Yata, Y. Higashi, T. Murakami, R. Yamajo, W. M. Wu, K. Taku, Y. Sasaki, and Y. Hideshima. A possible mechanism of absorption promoters. J. Pharmacobio-Dyn. 6:s-78 (1983).

    Google Scholar 

  2. K. Takahashi, T. Murakami, A. Kamata, R. Yumoto, Y. Higashi, and N. Yata. Pharmacokinetic analysis of absorption enhancing action of dacanoic acid derivatives in rats. Pharm. Res. in accepted.

  3. M. Tomita, M. Shiga, M. Hayashi, and S. Awazu. Enhancement of colonic drug absorption by the paracellular permeation route. Pharm. Res., 5:341–346 (1988).

    Google Scholar 

  4. P. K. Knoefel and K. C. Huang. Biochemorphology of renal tubular transport: hippuric acid and related substances. J. Pharmacol. Exp. Ther. 126:296–303 (1959).

    Google Scholar 

  5. W. W. Weber, J. N. Micel, D. J. Hearse, and G. S. Drummond. N-acetylation of drugs. Pharmacogenetic studies in rabbits selected for their acetylation characteristics. Drug Metabo. Dispos. 4:94–101 (1976).

    Google Scholar 

  6. W. M. Wu, T. Murakami, Y. Higashi, and N. Yata. Enhancement of the rectal absorption of sodium ampicillin by N-acylamino acids in rats. J. Pharm. Sci. 76:508–512 (1989).

    Google Scholar 

  7. K. Yamaoka and T. Nakagawa. A nonlinear least squares program based on differential equations, MULTI(RUNGE), for microcomputers. J. Pharmacobio-Dyn. 6:595–606 (1983).

    Google Scholar 

  8. M. C. Steward. Paracellular non-electrolyte permeation during fluid transport across rabbit gall-bladder epithelium. J. Physiol. 322:419–439 (1982).

    Google Scholar 

  9. M. Tomita, M. Hayashi, T. Horie, T. Ishizawa, and S. Awazu. Enhancement of colonic drug absorption by transcellular permeation route. Pharm. Res. 5:786–789 (1988).

    Google Scholar 

  10. M. Tomita, T. Ogawa, H. Ouchi, M. Hayashi, and S. Awazu. Differences in the enhancing effects of sodium caprate on colonic and jejunal drug absorption. Pharm. Res. 5:648–653 (1992).

    Google Scholar 

  11. K. Nishimura, Y. Nozaki, A. Yoshimi, S. Nakamura, M. Kitagawa, N. Kakeya, and K. Kitao. Studies on promoting effects of carboxylic acid derivatives on rectal absorption of β-lactam antibiotics in rats. Chem. Pharm. Bull. 33:282–291 (1985).

    Google Scholar 

  12. T. Sawada, M. Tomita, M. Hayashi, and S. Awazu. Paracellular channel characterized by non-electrolyte permeation through the colonic membrane of the rats. J. Pharmacobio-Dyn. 12:634–639 (1989).

    Google Scholar 

  13. J. B. M. M. van Bree, A. G. de Boer, M. Danhof, L. A. Gincel, and D. D. Breimer. Characterization of an in vitro blood-brain barrier: effects of molecular size and lipophilicity on cerebrovascular endothelial transport rates of drugs. J. Pharmacol. Exp. Ther. 247:1233–1239 (1988).

    Google Scholar 

  14. N. H. Yoshida and M. S. Roberts. Solute molecular size and transdermal iontophoresis across excised human skin. J. Controlled Release 25:177–195 (1993).

    Google Scholar 

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Takahashi, K., Murakami, T., Yumoto, R. et al. Decanoic Acid Induced Enhancement of Rectal Absorption of Hydrophilic Compounds in Rats. Pharm Res 11, 1401–1404 (1994). https://doi.org/10.1023/A:1018983620622

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  • DOI: https://doi.org/10.1023/A:1018983620622

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