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


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.


Public Health Sodium Internal Medicine Healthy Volunteer Release Rate 
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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

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