Advertisement

Pharmaceutisch Weekblad

, Volume 2, Issue 1, pp 541–547 | Cite as

Increased gastro-intestinal absorption of hexobarbital by hydrophilization

  • M. Lagas
  • C. F. Lerk
  • D. D. Breimer
Original Articles

Abstract

This paper reports a comparative evaluation of thein vivo andin vitro availability of pure and hydrophilised hexobarbital from capsules. Hydrophilization of the poorly soluble hydrophobic drug was performed by coating the powder particles with hydrophilic methylcellulose. Liquid penetration into plugs of the treated powder, disintegration times andin vitro release rates became independent of the liquid wetting potency and were extremely fast compared with the pure drug. A bioavailability study in eight healthy volunteers showed a strongly increased extent and rate of absorption of the treated drug compared with the pure drug. The absorption rate of the hydrophilised free acid of hexobarbital was almost as rapid as that of the sodium salt.

Keywords

Public Health Sodium Internal Medicine Healthy Volunteer Release Rate 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Breimer, D. D. (1974) Thesis, Nijmegen, The Netherlands.Google Scholar
  2. Breimer, D. D., andJ. M. van Rossum (1974)J. Chromatog. 88, 235.Google Scholar
  3. Breimer, D. D., C. Honhoff, W. Zilly, E. Richter andJ. M. van Rossum (1975)J. Pharmacokin. and Biopharm. 3, 1.Google Scholar
  4. Bremer, D. D., andA. G. de Boer (1975)Europ. J. Clin. Pharmacol. 9, 169.Google Scholar
  5. Breimer, D. D. (1976)Brit. J. Anaesth. 48, 643.Google Scholar
  6. Breimer, D. D. (1977)Clin. Pharmacokin. 2, 93.Google Scholar
  7. Finholt, S., andS. Solvang (1968)J. Pharm. Sci. 57, 1322.Google Scholar
  8. Lagas, M., andC. F. Lerk (1977)Pharm. Weekblad 112, 845.Google Scholar
  9. Lerk, C. F., A. J. M. Schoonen andJ. T. Fell (1976)J. Pharm. Sci. 65, 843.Google Scholar
  10. Lerk, C. F., M. Lagas, J. T. Fell andP. Nauta (1978)J. Pharm. Sci. 67, 935.Google Scholar
  11. Lerk, C. F., M. Lagas, L. Lie-A-Huen, P. Broersma andK. Zuurman (1979)J. Pharm. Sci. 68, 634.Google Scholar

Copyright information

© Bohn, Scheltema & Holkema 1980

Authors and Affiliations

  • M. Lagas
    • 1
  • C. F. Lerk
    • 1
  • D. D. Breimer
    • 2
  1. 1.Laboratory for Pharmaceutical TechnologyUniversity of GroningenAW Groningen
  2. 2.Department of Pharmacology, Subfaculty of PharmacyUniversity of LeidenRA Leiden

Personalised recommendations