The aim of the present research work to study the effect of conjugation of the polymer on drug release from the matrix tablets. Sodium alginate L-cysteine conjugate was achieved by covalent attachment of thiol group of L-cysteine with the primary amino group of sodium alginate through the amide bonds formed by primary amino groups of the sodium alginate and the carboxylic acid group of L-cysteine. The synthesised sodium alginate L-cysteine conjugate was characterised by determining of charring point, Fourier transmission-infrared and differential scanning calorimetric analysis. To study the effect of conjugation on drug release pattern, the matrix tablets were prepared using various proportions of sodium alginate and sodium alginate L-cysteine conjugate along with atorvastatin calcium as model drug. The wet granulation technique was adopted and prepared matrix tablets were evaluated for various physical parameters. The in vitro drug release study results suggested that tablet formulated in combination of sodium alginate and sodium alginate L-cysteine conjugate S4 showed 100% after 8 h drug release whereas formulated with only sodium alginate S0 released 40% in 8 h.
The present research was envisaged to prepare gastroretentive beads to increase the retention time in stomach and to modulate the release pattern from the gel beads. The aim of the research work to study the compatibility between drug and other polymers by differential scanning calorimetric analysis, preparation of cod liver oil entrapped calcium pectinate gel beads of famotidine by emulsion gelation method and its evaluation. The gel beads were prepared by employing low methoxy pectin with degree of esterification less than 50% alone and with hydrophilic co polymers carbopol 934P, hydroxypropyl methylcellulose K15M and polycarbophil to study the effect of these co polymers on drug release. The prepared gel beads were subjected for various evaluations like topographical study of whole and dissected bead, percent drug entrapment efficiency, buoyancy and in vitro drug release study in conventional and modified flow through dissolution methods. The prepared beads showed ideal buoyancy, low methoxy pectin gel matrix could not sustain the drug release and presence of co polymers demonstrated sustained release. These observations suggested that cod liver oil entrapped calcium pectinate beads were promising as a carrier for intragastric floating drug delivery of famotidine.
The purpose of the present research investigation was to synthesis, characterisation of chitosan conjugates and its effect on drug permeation from transdermal rate controlling membrane. Chitosan conjugate was synthesised by conjugation with thioglycolic acid. The prepared chitosan conjugate was characterised by determining the charring point, Fourier transmission-infrared and differential scanning calorimetric analysis. The rate controlling membranes were prepared by various proportions of chitosan and chitosan conjugate, to moderate drug permeation through rate controlling membrane. The membrane moderated transdermal system consists of reservoir to hold the drug gel was prepared by 20% w/v ethylcellulose with a cavity in its center. An impermeable backing layer was prepared by 2% w/v ethylcellulose. Gel consists of carvedilol was prepared by sodium alginate and sodium carboxymethylcellulose in ethanol:water solvent system The rate controlling membranes prepared were evaluated by various parameters like thickness, folding endurance, swelling index, moisture content, moisture uptake, water vapor transmission rate, tensile strength test, measurement of gel strength, in vitro permeation study, ex vivo permeation study, compatibility study using differential scanning calorimetry and stability studies. All physical parameters evident that prepared membranes have good folding endurance and sufficient tensile strength. As the proportion of chitosan conjugate increases in membrane swelling index, moisture content, moisture uptake and permeability coefficient increases. The gel strength of chitosan conjugate was considerable less compared with chitosan.
The purpose of the present research envisaged was synthesize, characterize polycarbophil conjugate, to study the effect of conjugation on bioadhesion and drug release from the buccoadhesive tablet. The polycarbophil conjugate was synthesised by covalent attachment of thiol group of L-cysteine with the carboxylic acid group of polycarbophil. The synthesised conjugate was characterised by charring point determination, fourier transmission infra-red spectroscopic, differential scanning calorimetric analysis and measurement of gel strength. The bilayered buccoadhesive tablets provide the unidirectional diffusion. The drug core layer was prepared by various proportions of polycarbophil and polycarbophil conjugate with diltiazem hydrochloride. The backing layer was prepared by hydrophobic polymer Ethylcellulose. The buccoadhesive drug core was subjected to following evaluation tests such as weight uniformity, hardness, thickness, drug content, swelling index, moisture uptake, ex vivo bioadhesion strength, ex vivo bioadhesion time; in vitro drug release and in vitro drug permeation; ex vivo drug permeation was carried out in modified Franz diffusion cell. The study concluded that as the proportion of polycarbophil conjugate increased, increased drug release and drug permeation with enhanced ex vivo bioadhesive properties.
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