Abstract
Objective: The main objective of the present investigation is to develop a sustained-release (SR) formulation to optimize the postprandial elevation of glucose level in type 2 Diabetic subjects using combination therapy. In the present research work, bilayer sustained release formulation of metformin hydrochloride (MFH) and gliclazide (GLZ), based on monolithic-matrix technology was developed and evaluated. Methods: The formulations of metformin hydrochloride layer and gliclazide layer that contain polyox WSR coagulant and different viscosity grades of hydroxyl propyl methylcellulose (HPMC) as sustained-release matrix were prepared by direct compression and wet granulation method respectively. The bilayer tablets were prepared after carrying out the optimization of metformin layer and evaluated for various pre-compression and post-compression parameters. For the best formulation selected on basis of in vitro evaluation of tablets, Fourier-transform infrared spectroscopy (FT-IR) studies and comparison of in vitro dissolution profile of developed formulation with the innovator were performed. Results: Metformin hydrochloride and gliclazide showed sustained release of drug by diffusion mechanism and followed first-order kinetics. The best formulation of metformin hydrochloride (M7) and gliclazide (G8) show 99.93% and 99.65% of drug release in 24 h respectively. The similarity factor (f2) was 79.95 for metformin hydrochloride and 73.62 for gliclazide when compared with the innovator. Conclusion: The monolith diffusion-controlled bilayer tablets of metformin hydrochloride and gliclazide offer improved patient compliance and convenience with better postprandial hyperglycemic control with once-a-day dosing. The sustained release of the drug up to 24 h regulate antidiabetic activity round the clock with minimal side effects.
Highlights
Insulin is an anabolic hormone responsible for the maintenance of glucose homeostasis in the human body
Lack of adequate insulin levels in our body leads to several chronic metabolic disturbances of carbohydrate, fat, and protein that is often termed as diabetes mellitus (DM) which is a serious and lifelong condition [2]
The Fourier-transform infrared spectroscopy (FT-IR) spectrum of metformin hydrochloride and gliclazide in formulations was as shown in fig. 3C
Summary
Insulin is an anabolic hormone responsible for the maintenance of glucose homeostasis in the human body. Type 2 DM is a heterogeneous disorder characterized by multiple problems in the pancreatic β-cell, liver, and peripheral tissue such as skeletal muscles and adipose tissue These multiple complications are well managed by combination therapy using two antidiabetic drugs. Diabetes needs much attention as glucose levels that tend to increase after a meal, have to maintain for the whole day for proper activity of the body [9]. To combat such conditions, sustained-release (SR) formulations that regulate antidiabetic activity round the clock need to develop to optimize the postprandial elevation of glucose levels [10]
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