In vitro/in vivo evaluation of hydrochlorothiazide in experimental hydrochlorothiazide/triamterene combination tablets in beagle dogs.
The purpose of this study was to compare experimental formulations containing hydrochlorothiazide (CAS 58-93-5)/triamterene (HCT/TRI) in vitro and in vivo to a commercial tablet formulation (standard). The beagle dog was verified as a good model and was used for the in vivo studies. The commercial tablet and the experimental fast release formulation (FR) resulted in 100% release of HCT within 30 min in dissolution tests, whereas, the slow release formulation (SR) released only 54% HCT after 4 h. Relative bioavailability of the FR and SR formulations were 82 and 41%, respectively, compared to the commercial tablet. The experimental results indicate that HCT absorption occurs throughout the small intestine.
Ritschel
W A
WA
Division of Pharmaceutics and Drug Delivery Systems, College of Pharmacy, University of Cincinnati Medical Center.
Turkoglu
M
M
Lipps
D
D
Warner
A
A
Sakr
A
A
D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004285:Dogs; D004338:Drug Combinations; D005260:Female; D006852:Hydrochlorothiazide / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007202:Indicators and Reagents; D008297:Male; D012995:Solubility; D013607:Tablets; D014223:Triamterene / Q000008:administration & dosage / Q000493:pharmacokinetics*
D003692:Delayed-Action Preparations; D004338:Drug Combinations; D007202:Indicators and Reagents; D013607:Tablets; D006852:Hydrochlorothiazide; D014223:Triamterene