A novel colon targeted tablet formulation was developed using natural polysaccharides such as chitosan and guar gum as carriers and diltiazem hydrochloride as model drug. The prepared blend of polymer-drug tablets were coated with two layers, inulin as an inner coat followed by shellac as outer coat and were evaluated for properties such as average weight, hardness and coat thickness. In vitro release studies of prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid (SCF) in order to mimic the conditions from mouth to colon. It was observed that 4% w/v of rat cecal contents in saline phosphate buffer (SCF) incubated for 24 h provides suitable conditions for in vitro evaluation of the formulations prepared. The drug release from the coated system was monitored using UV/ Visible spectroscopy. In vitro studies revealed that the tablets coated with inulin and shellac have controlled the drug release in stomach and small intestinal environment and released maximum amount of drug in the colonic environment. Among the polymers used, chitosan was found to be the suitable polymer for colon targeting. The study revealed that polysaccharides as carriers and inulin and shellac as coating materials can be used effectively for colon targeting of drugs for treating local as well as systemic disorders.
A novel colon targeted tablet formulation was developed using pectin as carrier and diltiazem HCl and indomethacin as model drugs. The tablets were coated with inulin followed by shellac and were evaluated for average weight, hardness and coat thickness. In vitro release studies for prepared tablets were carried out for 2 h in pH 1.2 HCl buffer, 3 h in pH 7.4 phosphate buffer and 6 h in simulated colonic fluid. The drug release from the coated systems was monitored using UV/Vis spectroscopy. In vitro studies revealed that the tablets coated with inulin and shellac have limited the drug release in stomach and small intestinal environment and released maximum amount of drug in the colonic environment. The study revealed that polysaccharides as carriers and inulin and shellac as a coating material can be used effectively for colon targeting of both water soluble and insoluble drugs.
The present study envisages the preparation of microspheres containing indomethacin (IM) as model drug and bees wax as carrier, and to compare the in vitro release and pharmacokinetics of prepared IM formulation with commercially available oral formulation MicrocidSR. The microsphere formulations were prepared by meltable emulsified dispersion and cooling induced solidification. Surface morphology of microspheres has been evaluated using scanning electron microscopy (SEM). The SEM images revealed the spherical shape of microspheres and more than 98.0% of the isolated microspheres were in the size range 115-855 mum. Differential scanning calorimetry (DSC) and Fourier transform infrared (FTIR) spectroscopy studies indicated that the drug after encapsulation with bees wax was stable and compatible. A single dose randomized complete cross over study of IM (75 mg) microspheres was carried out on 8 healthy Albino sheeps. Plasma IM concentrations and other pharmacokinetic parameters obtained were statistically analyzed. The T (max), C (max), AUC(O-24) and T (1/2) values of MicrocidSR and optimized formulation were 3.0 h, 2038 +/- 51.31 ng/ml, 9528 +/- 129.65 ng/ml h(-1), and 2.59 +/- 0.02 h(-1); and 3.2 h, 1940 +/- 22.61 ng/ml, 8751 +/- 41.32 ng/ml h(-1), and 2.68 +/- 0.02 h(-1), respectively. Beeswax microspheres showed controlled release and it can be concluded that both the prepared formulation and MicrocidSR are bioequivalent.
A series of polyvinyl alcohol (PVA)-hydroxy propyl methyl cellulose (HPMC) based films and gelrite (gellan gum) based in situ gels were formulated with ciprofloxacin hydrochloride as the drug. Drug diffusion studies were carried out for both the film and in situ gel formulations. The prepared PVA/HPMC blends have been characterized for tensile strength behavior and percent elongation at break. Fourier transfer infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies were carried out to study the compatibility of the drug and polymers used. Drug diffusion results indicate that the film and gel formulations containing ciprofloxacin were compatible and showed a prolonged drug release pattern. The gelrite formulation was non-irritant and had a good gelling property compared to PVA/HPMC blends.
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