Solid dispersions in the development of a nimodipine floating tablet formulation and optimization by artificial neural networks and genetic programming (original) (raw)
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Dissolution enhancement is one of the major focus areas in drug delivery owing to increase in number of new drugs with a limited solubility. Conventional approaches to address this need include selecting suitable polymer(s) followed by optimizing various drug-polymer combinations to arrive at one providing requisite dissolution enhancement. What often lacks in such approaches is (a) evaluation of industrial feasibility to scale-up the developed solid dispersion method and (b) inclusion of solid dispersion into a suitable dosage form for convenient administration to the patient. Regulatory agencies globally are emphasizing on use of quality by design (Qbd) tools in product development. The present work focuses on devising a strategy to optimize a binary solid dispersion formulation with a limited number of statistically designed experiments (DoE) to arrive at a suitable formula and industrially doable process. Polymer screening was undertaken using phase solubility studies with a mod...
International Journal of Applied Pharmaceutics, 2024
Objective: To employ Design of Experiment (DOE) for designing a floating matrix tablet of Domperidone Maleate (DM) using novel direct compression grade polymer METHOCEL K4M DC2 that offers advantages of extended or sustained release, providing for cost-effective manufacturing. Methods: To prepare floating matrix tablets containing DM, the direct compression method was employed. The tablets were optimised using a 2 2 Central Composite Design (CCD). Concentration of the sustained release polymer METHOCEL DC2 K4M grade (X1= A) and Concentration of the floating agent potassium bicarbonate (KHCO3) (X2= B) were the independent variables selected whereas floating lag time (Y1), drug release at 1 h (Y2), 4 h (Y3), 6 h (Y4) and 8 h (Y5) were the 5 dependent variables employed in the study design. Fourier Transform Infrared (FTIR) analysis was utilised to analyse drug-excipient compatibility, revealing no discernible interaction, and various mathematical models were employed to study the drug release mechanism. Results: The prepared tablets were evaluated for weight, thickness, hardness, friability, and assay and the results were found to be satisfactory. The optimised formulation predicted by the software was found to have a desirability value of 0.982, containing 60 mg of METHOCEL DC2 K4M and 20 mg of KHCO3, was prepared and evaluated. Predicted and experimental results were found to be comparable for all the responses. All formulations were shown to fit well into Zero-order release kinetics, but the optimised formulation (F4), with R 2 = 0.9893 and n= 2.2797, exhibited the best fitting in both the Zero-order and Korsmeyers-Peppas model. Conclusion: The study conducted revealed that floating tablets of DM could be developed using KHCO3 as a gas-generating agent with sustained drug release till 14 h using polymer METHOCEL DC2 K4M.
Floating matrix tablets of domperidone formulation and optimization using simplex lattice design
Iranian journal of pharmaceutical research : IJPR, 2011
The purpose of this research was to prepare a floating matrix tablet containing domperidone as a model drug. Polyethylene oxide (PEO) and hydroxypropyl methylcellulose (HPMC) were evaluated for matrix-forming properties. A simplex lattice design was applied to systemically optimize the drug release profile. The amounts of PEO WSR 303, HPMC K15M and sodium bicarbonate were selected as independent variables and floating lag time, time required to release 50% of drug (t50) and 80% of drug (t80), diffusion coefficient (n) and release rate (k) as dependent variables. The amount of PEO and HPMC both had significant influence on the dependent variables. It was found that the content of PEO had dominating role as drug release controlling factor, but using suitable concentration of sodium bicarbonate, one can tailor the desired drug release from hydrophilic matrixes. The linear regression analysis and model fitting showed that all these formulations followed Korsmeyer and Peppas model, which...
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The aim of the present work is to formulate evaluate and develop a dissolution profile for an orally administrable extended tablet of nisoldipine, a calcium channel blocker drug by using various controlled release polymers including Methocel K100LVCR, Hydroxypropyl Cellulose (HPC-L), Hydroxypropyl cellulose (HPC-M), Lactose Monohydrate NF, Sodium Lauryl Sulphate (SLS), Eudragit L30D-55, Glyceryl behenteNF, Collodial silicon dioxide NF (Aerosil200), Magnesium Sterate NF, Methocel E50, Methocel K100M CR in various ratios with active pharmaceutical ingredient (API) which show comparable dissolution profile with the reference product. The tablets were evaluated for drug content, weight variation, hardness, thickness, friability, film coating, high performance liquid chromatography, stability profile, and zero order kinetics in-vitro drug release study. The drug excipients compatibility studies indicated that the studied excipients have no interaction with drug .the excipients were compa...
Asian Journal of Biomedical and Pharmaceutical Sciences, 2018
Objective: Felodipine is a calcium channel blocker used for hypertensive and unstable angina treatments. The sustained release formulations of felodipine have advantages of achieving good therapeutic effects, increasing a bioavailability, decreasing dosing times per day and reducing side effects. The aim of our study was to study the formulation screening, then use an experiment design for formulating a hydrophilic matrix sustained release Tablet of felodipine. Methods: The optimization process had the influences of the chosen excipients (including HPMC E4M, HPMC E15LV) on the drug release. Three dependent variables were percentages of released felodipine at the sampling times 2 h, 6 h, 10 h (Y2, Y6, Y10, respectively). Results: The release profile from the optimized formula almost met the predicted release profile and similar to reference Tablets. The kinetics of drug release the optimized Tablets and reference Tablets were also followed the Korsmeyer-Peppas model. Conclusion: The ...