Enhanced Bioavailability and Reduced Metabolism of Salbutamol by Perbutanoyl-β-cyclodextrin after Oral Administration in Dogs
Article first published online: 11 MAR 2011
1995 Royal Pharmaceutical Society of Great Britain
Pharmacy and Pharmacology Communications
Volume 1, Issue 11, pages 517–520, November 1995
How to Cite
HIRAYAMA, F., HORIKAWA, T., YAMANAKA, M. and UEKAMA, K. (1995), Enhanced Bioavailability and Reduced Metabolism of Salbutamol by Perbutanoyl-β-cyclodextrin after Oral Administration in Dogs. Pharmacy and Pharmacology Communications, 1: 517–520. doi: 10.1111/j.2042-7158.1995.tb00369.x
- Issue published online: 11 MAR 2011
- Article first published online: 11 MAR 2011
- October 2, 1995, November 20, 1995
The in-vitro release of salbutamol, a bronchodilator, was studied after by complexation with perbutanoyl-β-cyclodextrin (TB-β-CyD).
A prolonged maintenance (at least 24 h) of higher and constant salbutamol levels in plasma was obtained after oral administration of the salbutamol complex in dogs; the area under the plasma salbutamol concentration curve up to 24 h post-administration of TB-β-CyD complex was about 5 times that of salbutamol alone. Furthermore, the plasma level of salbutamol glucuronide, a major metabolite of salbutamol, after the administration of TB-β-CyD complex was significantly lower than that after administration of the drug alone, probably because of the suppression of the metabolism of salbutamol in the gastrointestinal tract by TB-β-CyD complexation.
The present results indicate that TB-β-CyD may be a useful carrier for orally administered water-soluble drugs, especially for drugs which are metabolized extensively in the gastrointestinal tract.