Formulation design, optimization and evaluation of domperidone maleategastro retentive floating tablets

[摘要] The main objective of present research work is to formulate the of Domperidone Maleate floating tablets. Domperidone Maleate, an antiemetic and a prokinetic agent belongs to BCS Class-II and Indicated for treatment of upper gastrointestinal motility disorders by blocking the action of Dopamine. The Floating tablets of Domperidone Maleate were prepared employing different concentrations of HPMCK4M and Guar Gum in different combinations as a release rate modifiers by Direct Compression technique using 32 factorial design. The concentration of HPMCK4M and Guar Gum was selected as independent variables, X1 and X2 respectively whereas, time required for drug dissolution t10%, t50%,t75%,t90%were selected as dependent variables. Totally nine formulations were designed and are evaluated for hardness, friability, thickness, Assay, Floating Lag time, In-vitro drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1, C2). According to SUPAC guidelines the formulation (F5) containing combination of 18.75% HPMCK4M and 18.75% Guar Gum, is the most similar formulation (similarity factor f2=89.03, dissimilarity factor f1= 11.539& No significant difference, t= 0.169) to marketed product (DOMSTAL OD). The selected formulation (F5) follows Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.925).

[学科分类] 药理学