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TITLE:

FORMULATION OF GASTRO RETENTIVE MATRIX TABLETS FOR ANTIHYPERTENSIVE DRUGS USING NATURAL GUMS AND LOW-DENSITY POLYMERS: EFFECT OF FORMULATION FACTORS ON IN VITRO DISSOLUTION RATES

AUTHORS:

Sreenivasa Reddy N, Mahendra Kumar CB, Ramesh A

ABSTRACT:

The objective of the study was to develop Gastro retentive matrix tablets for antihypertensive drugs. The matrix tablets of antihypertensive drug captopril with 12 formulations coded as F1 to F12 with variant ratios of polymer were prepared in the preliminary studies by direct compression method. Hydrophilic and hydrophobic low density polymers like HPMC M15K and HPMC M4K and natural gums like Karaya gum, Xanthan gum, Pullulan gum, Gellan gum and Guar gum were used. The pre-compression parameters, and compatibility of drug with various excipient was studied using HPTLC, FTIR and DSC. The tablets were directly compressed and evaluated for compliance with pharmacopeia limits. The results of floating lag time (FLT), total floating lag time (TFT), and in vitro dissolution studies indicated that formulation F9 was shown better drug release, floating lag time characteristics compared to other formulations. The decrease in release kinetics of the drug was observed on increasing polymer ratio. Based on the preliminary formulation (F1-F12) and evaluation, optimization technique was adopted using 32 factorial design and statistical ANOVA (software). Ten formulations designed and formulated with code R1 to R10. The pre-compression, post-compression parameters including buoyancy of R1 to R10 were investigated, and optimized formulae were developed with predicted values. The optimized matrix tablets coded as FC were prepared by direct compression, evaluated for pre & post compression parameters, buoyancy, and in vitro cumulative drug release. The predicted values of optimized technique, and actual values of formulation FC after evaluation were found nearer. The in vitro drug release curve fitting kinetics was studied. and found to be non-fickian, and by diffusion . Key words: Captopril, Karaya gum, Xanthan gum, Pullulan gum, Gellan gum, Floating lag time.

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