Formulation Development and Evaluation of Bilayer Tablets of Lisinopril for Immediate Release and Glipizide for Sustained Release

Priya, B (2014) Formulation Development and Evaluation of Bilayer Tablets of Lisinopril for Immediate Release and Glipizide for Sustained Release. Masters thesis, College of Pharmacy, Madras Medical College, Chennai.

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Abstract

The present work involves the formulation development, optimization and In-vitro evaluation of bilayer tablet containing Lisinopril in the immediate release layer and Glipizide in the sustained release layer, using sodium starch glycolate as a super disintegrant for the immediate release layer and the hydrophilic matrix HPMC K100M, hydrophobic matrix Ethyl cellulose are used in the sustained release layer. Bilayer tablet showed as initial burst effect to provide dose of immediate release layer Lisinopril to control the blood pressure level and the sustained release of Glipizide for 24hours to control the blood glucose level. The developed formulation shows an alternative to the conventional dosage form for the treatment of diabetes along with diabetic hypertension and nephropathy. Under the preformulation studies, API (Active Pharmaceutical Ingredient) characterization and drug-excipient compatibility studies were carried out. The API characterization showed compliance with the drug characteristics. The polymers and other excipients were selected based on the satisfying results produced during drug-excipient compatibility studies to develop the final formulation. Immediate and sustained release tablets were formulated by wet granulation method because of the poor flow property of the blends. The formulated granules were evaluated for precompression studies which showed that the flow property was good. The formulated tablets were found to be within the limits with respect to uniformity of weight, hardness, thickness, diameter and friability.  The disintegration time of IR tablets containing SSG 8% was found to be optimum. The drug content of the formulated IR and SR tablets were found to be within limits. Based on the in vitro dissolution studies of IR tablets, formulation L3 was optimised and selected for final bilayer tablets. Based on the in vitro dissolution studies of SR tablets, formulation G5 containing EC and HPMC K100M (1:4). It released the drug 99.82% in 24hours. This formulation G5 was optimised and selected for bilayer tablets. The optimised IR and SR formulations were compressed into bilayer tablets. The formulated bilayer tablets were found to be within the limits with respect to uniformity of weight, hardness, thickness, diameter and friability. The drug content of the bilayer tablets were estimated by simultaneous estimation method and it was found to be within the pharmacopoeial limit. The in vitro dissolution studies of optimised bilayer tablets were released the drug upto 24 hours. The release kinetics of the optimized tablets showed that it follows zero order release kinetics. The release of the drug from the dosage form was found to be by dissolution and non fickian release. Stability studies of optimized bilayer tablets were carried out according to ICH guidlines. It indicated that the bilayer tablets are stable and does not show any significant changes in the physical characteristics, drug content and dissolution. The results obtained were found to be within the limits. Success of the in vitro drug release studies recommends the product for the further invivo studies, which may improve patient compliance. From the literature, it is seen that Lisinopril as an individual dosage form is used in the management of hypertension in patients with type I and type II diabetes mellitus. Glipizide is given as alone or in combination with other antidiabetic drugs in patients with type II diabetes. Lisinopril potentiate the effect of Glipizide. Hence the bilayer tablets of Lisinopril and Glipizide were used to improve patient compliance towards the effective management diabetes along with diabetic hypertension and nephropathy. Combination of Lisinopril as an immediate release layer and Glipizide as a sustained release layer reduces polytherapy to monotherapy. From the results, formulated bilayer tablet provides better in vitro release from immediate release layer as well as sustained release layer. The data obtained from in vitro release study for sustained release layer were fitted to various mathematical model like zero order, first order, Higuchi model and Peppas model. The results of mathematical model fitting of data obtained indicated that, the best fit model was zero order. Thus the release of the drug from the dosage form was found to be by dissolution and non fickian release.

Item Type: Thesis (Masters)
Uncontrolled Keywords: Bilayer Tablets; Lisinopril; Glipizide
Subjects: PHARMACY > Pharmaceutics
Depositing User: Ravindran C
Date Deposited: 09 Oct 2017 06:13
Last Modified: 09 Oct 2017 06:13
URI: http://repository-tnmgrmu.ac.in/id/eprint/3650

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