Development and In Vitro Assessment of Novel Bilayer Tablets Containing Glimepiride and Metformin

Type 2 diabetes mellitus requires combination therapy to achieve effective glycemic control. Bilayer tablet formulations combining immediate and sustained drug release offer improved therapeutic outcomes. Glimepiride and Metformin hydrochloride are commonly prescribed together due to their complementary mechanisms of action. The aim of the current research was to formulate bilayer tablets of Glimepiride and Metformin hydrochloride to enhance therapeutic utility in the management of type 2 diabetes mellitus.

Bilayer tablets were developed with Glimepiride in the immediate-release layer using the superdisintegrant croscarmellose sodium, and Metformin hydrochloride in the sustained-release layer using microcrystalline cellulose and HPMC K100M as key excipients. The formulations were optimized by evaluating immediate-release characteristics of Glimepiride and sustained-release profiles of Metformin hydrochloride. The optimized formulation (F6) demonstrated 99.92% immediate release of Glimepiride within 45 minutes, while Metformin hydrochloride showed a sustained release of 99.87% over a period of 12 hours. The study indicates the successful development of bilayer tablets of Glimepiride and Metformin hydrochloride, which can be effectively used for the management of type 2 diabetes mellitus.

Introduction

Type 2 diabetes is more accurately described as a chronic metabolic disorder characterized by hyperglycemia due to insulin resistance and progressive β-cell dysfunction. Essentially, persistent elevation of blood glucose because of relative deficiency of insulin leading to insulin resistance.^1-6Glimepiride is a second generation sulfonylureaand Metformin hydrochloride, a biguanide, is first of two classes of commonly used pharmacological agents for management of diabetes mellitus.^7-11Glimepiride stimulates insulin secretion from pancreatic beta cells, while Metformin hydrochloride inhibits hepatic glucose production, thereby reducing blood glucose levels.^12-19Key reason for using combination therapy is to decrease need for use of each drug at that dosage, so that potential for dose dependent side effect and adverse reactions is minimized. Emphasizing the therapeutic implications for diabetes management, the combined use of Glimepiride and Metformin offers improved glycemic control through complementary mechanisms. This dual-action approach enhances treatment efficacy by providing both immediate and sustained blood glucose regulation. Such formulations can improve patient compliance and overall clinical outcomes in the management of type 2 diabetes mellitus.

Glimepiride and Metformin exhibit a synergistic effect, making them highly effective in lowering blood glucose levels.^20-24Depending on drug, a bilayer tablet can be used as an elegant strategy to ensure that chemical incompatibilities among dissimilar drugs do not lead to problems; a method of physically separating these drugs in different layers and allowing for their different release profiles – immediate (IR) for one drug, sustained (SR) forother.^25-28This format is particularly influenced when combining two drugs that require different release kinetics or two drugs that require different release profiles including both a loading dose (IR) &a sustained dose (SR). Disease is diabetes with type 2, and it is progressive illness caused by numerousunderneath pathophysiological mechanisms.²⁹Often, mono-therapy does not preserve adequate glycemic management and hence, treatment failure can develop.³⁰An optimal mix of glucose-lowering substances should include balancing mechanisms, orient toward multigene disease pathways, be administered at all disease stages, and be tolerated without increasing danger of hypoglycemia, heart-related complications, or putting on weight.^31-32The present study aims to formulate and evaluate a bilayer tablet ^33-40consisting of an immediate-release layer with crosscarmellose sodium and a sustained-release layer containing Glimepiride and Metformin hydrochloride, using extended-release polymers (MCC and HPMC K100M).

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Materials

Glimepiride (GM) & Metformin HCl (MF) were kindly provided by M/s Shree Icon Laboratories as gift samples, Vijayawada, India. Loba Chemie Pvt Ltd., Mumbai, India procured crosscarmellose sodium, microcrystalline cellulose, HPMC K100M, povidone K30, magnesium stearate, talc, isopropyl alcohol and quinoline yellow. Pharmaceutical grade excipients were used in the study.

Atmakuri L. R, Vetapalem R, Talasila E. G. K. M, Potluri H, Alluri R, Ghanta V. K. Development and In Vitro Assessment of Novel Bilayer Tablets Containing Glimepiride and Metformin. Biomed Pharmacol J 2026;19(3).

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