Response surface optimization of sustained release metformin-hydrochloride matrix tablets: influence of some hydrophillic polymers on the release (original) (raw)
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Brazilian Journal of Pharmaceutical Sciences, 2011
Metformin hydrochloride is an antidiabetic agent which improves glucose tolerance in patients with type 2 diabetes and reduces basal plasma levels of glucose. In this study, a simplex centroid experimental design with 69 runs was used to select the best combination of some hydrophilic polymers that rendered a 24 h in-vitro release profile of metformin.HCl. The Korsmeyer-Peppas model was used to model the dissolution profiles since it presented the best fit to the experimental data. Further, a cubic model predicted the best formulation of metformin.HCl containing polyvinyl pyrrolidone, ethyl cellulose, hydroxypropyl methyl cellulose, carrageenan, sodium alginate, and gum arabic at 6.26, 68.7, 6.26, 6.26, 6.26 and 6.26 % levels, respectively. The validation runs confirmed the accuracy of the cubic model with six components for predicting the best set of components which rendered a once-a-day modified release hydrophilic matrix tablet in compliance with the USP specifications.
Metformin HCL, the only available biguanide, remains the first line drug therapy for patients with Type 2 diabetes mellitus acts by decreasing hepatic glucose output and peripheral insulin resistance. It has relatively short plasma half life, low absolute bioavailability. The overall objective of the present work was to develop an oral sustained release metformin tablet prepared by direct compression method, using hydrophilic hydroxyl propyl methylcellulose and Xanthan gum polymer as rate controlling factor. All the batches were evaluated for thickness, weight variation, hardness, and drug content uniformity and in vitro drug release. Mean dissolution time is used to characterize drug release rate from a dosage form and indicates the drug release retarding efficiency of polymer. Hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h whereas when combined with Xanthan gum could slow down the release of drug and can be successfully employed for f...
2019
Original Research Article Metformin hydrochloride (MET) is an oral hypoglycaemic agent which improves glucose tolerance in patients with type 2 diabetes and diminishes basal plasma levels of glucose. The aim of this study was to develop and optimize MET matrix tablets for SR application. The SR matrix tablet of MET was prepared by wet granulation technique using Sodium carboxymethyl cellulose and hydroxyl propyl methylcellulose of different viscosity grades (HPMC K4M, HPMC K15M, and HPMC K100M). The influence of varying the polymer ratios was evaluated. The excipients used in this study did not modify physicochemical properties of the drug. MET has relatively short plasma half-life, low absolute bioavailability. The need for the administration 2 to 3 times a day when larger doses are required can decrease patient fulfilment. SR formulation that would maintain plasma level for 8-12 h might be sufficient for daily dosing of MET. SR products are needed for MET to prolong its duration o...
PREPARATION AND IN VITRO EVALUATION OF SUSTAINED RELEASE TABLET FORMULATIONS OF METFORMIN HCL
An attempt was to formulate the oral sustained release metformin hydrochloride matrix tablets by using hydroxypropyl methylcellulose of different viscosity grades (HPMC K4M, HPMC K15M, and HPMC K100M). The tablets were prepared by wet granulation technique. The granules were evaluated for angle of repose, loose bulk density, tapped and bulk density. It shows satisfactory results. The tablets were subjected to thickness, weight variation, drug content, hardness, friability, and in vitro release studies. The in vitro dissolution study was carried out for 8 h using USP dissolution apparatus II (paddle) in 900mL 0.1 N HCl as dissolution media. The release mechanisms were explored and explained with zero order, first order, Higuchi, Kromayer's and Hixon-Croweel equations. The optimized formulation was found to be buoyant for 8 h in stomach. It is cleared that the drug release from matrix tablets prepared by HPMC K100M provides a better result in preparation of SR formulation of metformin hydrochloride.