In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride.
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.
Al-Saidan
Saleh M
SM
Department of Pharmaceutics, Faculty of Pharmacy, Health Science Center, Kuwait University, Kuwait.
Krishnaiah
Yellela S R
YS
Patro
Srinivas S
SS
Satyanaryana
Vemulapalli
V
D000284:Administration, Oral; D000328:Adult; D000818:Animals; D001826:Body Fluids / Q000187:drug effects / Q000378:metabolism; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations / Q000008:administration & dosage / Q000378:metabolism; D004110:Diltiazem / Q000008:administration & dosage* / Q000097:blood*; D004341:Drug Evaluation / Q000379:methods; D005685:Galactans / Q000008:administration & dosage* / Q000097:blood*; D006801:Humans; D008297:Male; D008351:Mannans / Q000008:administration & dosage* / Q000097:blood*; D053149:Plant Gums; D051381:Rats; D012995:Solubility / Q000187:drug effects; D013608:Tablets, Enteric-Coated; D014867:Water / Q000378:metabolism*
D003692:Delayed-Action Preparations; D005685:Galactans; D008351:Mannans; D053149:Plant Gums; D013608:Tablets, Enteric-Coated; D014867:Water; C007894:guar gum; D004110:Diltiazem