In the pharmaceutical industry, Glibenclamide 5 mg (also known internationally as Glyburide) is a second-generation sulfonylurea antidiabetic agent. As a pharmacist, I classify this as a “secretagogue,” meaning its primary function is to stimulate the pancreas to produce more insulin. The 5 mg strength is a standard therapeutic dose for maintaining glycemic control.

Primary Clinical Uses

• Type 2 Diabetes Mellitus (T2DM): Indicated as an adjunct to diet and exercise to improve glycemic control in adults with Type 2 diabetes.

• Monotherapy or Combination: It can be used alone or in combination with other oral hypoglycemic agents like Metformin when a single drug does not provide adequate blood sugar control.

• Neonatal Diabetes: In specific genetic cases (KCNJ11 mutations), Glibenclamide is often the drug of choice to replace insulin injections.

Mechanism of Action

Glibenclamide works by targeting the pancreatic beta cells to increase insulin secretion.

ATP-Sensitive Potassium Channels: It binds to the SUR1 receptors on the surface of pancreatic beta cells, closing the ATP-sensitive potassium ($K^+_{ATP}$) channels.

Depolarization: This closure leads to the depolarization of the cell membrane.

Calcium Influx: Depolarization opens voltage-gated calcium channels, allowing an influx of calcium into the cell.

Insulin Release: The rise in intracellular calcium triggers the exocytosis (release) of stored insulin granules into the bloodstream

The Manufacturer’s Perspective: Formulation & Export

From a manufacturing and global trade standpoint, Glibenclamide 5 mg is a high-volume essential product:

• Micronization for Bioavailability: Glibenclamide is practically insoluble in water, which can lead to inconsistent absorption. As a WHO-GMP manufacturer, we utilize micronized API to ensure a uniform particle size, resulting in a predictable and consistent blood-sugar-lowering effect.

• Risk of Hypoglycemia: Due to its long half-life and potent mechanism, Glibenclamide carries a higher risk of hypoglycemia, especially in the elderly. We ensure our Product Information Leaflets (PIL) and labeling provide clear warnings regarding dose titration and food intake.

• Stability for Global Trade: The product is relatively stable, but we utilize Alu-Alu or high-grade PVC/PVDC blister packaging to ensure a 36-month shelf life for export to Zone IVb regions (Africa, SE Asia, and Latin America).

• B2B & Dossier Support: We provide full CTD/eCTD Dossiers and comparative dissolution studies against the innovator (Daonil) to support our B2B partners in international registration.