Back to Search
Start Over
In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride.
- Source :
-
AAPS PharmSciTech [AAPS PharmSciTech] 2005 Jul 14; Vol. 6 (1), pp. E14-21. Date of Electronic Publication: 2005 Jul 14. - Publication Year :
- 2005
-
Abstract
- The objective of the study was to develop guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride. Matrix tablets of diltiazem hydrochloride, using various viscosity grades of guar gum in 2 proportions, were prepared by wet granulation method and subjected to in vitro drug release studies. Diltiazem hydrochloride matrix tablets containing either 30% wt/wt low-viscosity (LM1), 40% wt/wt medium-viscosity (MM2), or 50% wt/wt high-viscosity (HM2) guar gum showed controlled release. The drug release from all guar gum matrix tablets followed first-order kinetics via Fickian-diffusion. Further, the results of in vitro drug release studies in simulated gastrointestinal and colonic fluids showed that HM2 tablets provided controlled release comparable with marketed sustained release diltiazem hydrochloride tablets (D-SR tablets). Guar gum matrix tablets HM2 showed no change in physical appearance, drug content, or in dissolution pattern after storage at 40 degrees C/relative humidity 75% for 6 months. When subjected to in vivo pharmacokinetic evaluation in healthy volunteers, the HM2 tablets provided a slow and prolonged drug release when compared with D-SR tablets. Based on the results of in vitro and in vivo studies it was concluded that that guar gum matrix tablets provided oral controlled release of water-soluble diltiazem hydrochloride.
- Subjects :
- Administration, Oral
Adult
Animals
Body Fluids drug effects
Body Fluids metabolism
Cross-Over Studies
Delayed-Action Preparations administration & dosage
Delayed-Action Preparations metabolism
Drug Evaluation methods
Humans
Male
Plant Gums
Rats
Solubility drug effects
Tablets, Enteric-Coated
Diltiazem administration & dosage
Diltiazem blood
Galactans administration & dosage
Galactans blood
Mannans administration & dosage
Mannans blood
Water metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1530-9932
- Volume :
- 6
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- AAPS PharmSciTech
- Publication Type :
- Academic Journal
- Accession number :
- 16353958
- Full Text :
- https://doi.org/10.1208/pt060105