Increased gastro-intestinal absorption of hexobarbital by hydrophilization
- 27 Downloads
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.
KeywordsPublic Health Sodium Internal Medicine Healthy Volunteer Release Rate
Unable to display preview. Download preview PDF.
- Breimer, D. D. (1974) Thesis, Nijmegen, The Netherlands.Google Scholar
- Breimer, D. D., andJ. M. van Rossum (1974)J. Chromatog. 88, 235.Google Scholar
- Breimer, D. D., C. Honhoff, W. Zilly, E. Richter andJ. M. van Rossum (1975)J. Pharmacokin. and Biopharm. 3, 1.Google Scholar
- Bremer, D. D., andA. G. de Boer (1975)Europ. J. Clin. Pharmacol. 9, 169.Google Scholar
- Breimer, D. D. (1976)Brit. J. Anaesth. 48, 643.Google Scholar
- Breimer, D. D. (1977)Clin. Pharmacokin. 2, 93.Google Scholar
- Finholt, S., andS. Solvang (1968)J. Pharm. Sci. 57, 1322.Google Scholar
- Lagas, M., andC. F. Lerk (1977)Pharm. Weekblad 112, 845.Google Scholar
- Lerk, C. F., A. J. M. Schoonen andJ. T. Fell (1976)J. Pharm. Sci. 65, 843.Google Scholar
- Lerk, C. F., M. Lagas, J. T. Fell andP. Nauta (1978)J. Pharm. Sci. 67, 935.Google Scholar
- Lerk, C. F., M. Lagas, L. Lie-A-Huen, P. Broersma andK. Zuurman (1979)J. Pharm. Sci. 68, 634.Google Scholar