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 lowviscosity (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°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.
Samples of indomethacin and kaolin or microcrystalline cellulose (Avicel) were prepared by solvent deposition or simple blending methods. Dissolution rates of these samples were studied. The surface adsorption of indomethacin on the studied adsorbents was shown to improve the dissolution rate of the drug in water. The solvent-deposited samples of indomethacin on kaolin or Avicel in the ratio 1:4 released 25% of the drug at 34 or 60 min, respectively (t25%), while 25% of the pure drug was released at 140 min. Meanwhile, the t25% of the corresponding drug-adsorbent simple blends were 108 and 110 min, respectively. The effect of addition of polyvinyl pyrrolidone (PVP) as a third component to indomethacin-adsorbent was studied and showed further improvement in in vitro availability of the drug-kaolin adsorbents.
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