EVALUATION OF CHRYSOPHYLLUM ALBIDUM (G. DON) FRUIT GUM AS A SUSTAINED RELEASE MATRIX IN TABLET FORMULATIONS
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ABSTRACT
The goal of designing sustained release or controlled release delivery system is to reduce the frequency of dosing or to increase effectiveness of the drug by localization at the site of action, reducing the dose required or providing uniform drug delivery. Natural gums and polymers have been employed as excipients in modified release dosage forms. The objectives of this study were to extract and determine the percentage yield of Chrysophyllum albidum gum, perform physicochemical studies and preliminary phytochemical screening, determine the compatibility of the gum with the active ingredients, formulate sustained release tablets with the gum as the sustaining matrix and compare the release profiles with those of a standard matrix former, hydroxyl propyl methyl cellulose (HPMC), and to determine the release mechanisms and kinetics of the formulations. A percentage yield of 18 ± 4 % w /w was obtained. The gum showed physicochemical properties consistent with natural gums employed as pharmaceutical excipients. Differential Scanning Calorimetry (DSC) and Fourier Transform Infrared (FTIR) spectroscopy studies did not show any incompatibility with chlorpheniramine maleate and theophylline hydrochloride. Tablet parameters were within pharmacopoeial limits. Dissolution studies showed an increase in retardation of drug release with increase in Chrysophylum albidum fruit gum (CAG) concentration. Batches containing 30 % CAG showed the most desirable T50% of approximately 12 h. Comparison with HPMC at the same concentration showed that CAG had better sustained release properties. Studies of the kinetics and mechanisms of drug release from CAG batches showed that at higher concentrations, the formulations demonstrated a super case II release kinetics. The mechanism of release combines swelling, erosion, and diffusion. Stability studies vii performed on the tablets after one year showed only slight changes in the T50% with no significant change in the drug content and the disintegration times. In conclusion, CAG possesses good pharmaceutical yield and tablets have good pharmacotechnical properties. Varying concentrations of CAG can be employed as a sustaining matrix in the formulation of chlorpheniramine and theophylline sustained release tablets.
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