Linagliptin & Metformin Hydrochloride Bilayer Tablets (IR & ER Variants)
Healthy Inc is a specialized global supplier and exporter of advanced endocrinology, metabolic-support, and advanced-delivery diabetic therapeutics. We provide ultra-high-purity, kinetically synchronized Linagliptin & Metformin Hydrochloride Immediate-Release (IR) and Extended-Release (ER) Bilayer Tablets, manufactured in WHO–GMP certified, high-precision modified-release oral solid dosage facilities. This “Dual-Action Incretin & Biguanide Synergy” is a massive-volume, highly lucrative export to diabetic care clinics, internal medicine networks, retail pharmacy chains, and government health ministries in LATAM, the CIS, Africa, and Southeast Asia, serving as the globally mandated step-up intervention for patients with Type 2 Diabetes Mellitus whose blood sugar remains uncontrolled on Metformin monotherapy.
Product Overview
This highly advanced Fixed-Dose Combination masterfully synchronizes two of the world’s most effective and complementary diabetic mechanisms. It simultaneously shuts down the liver’s overproduction of glucose while actively amplifying the pancreas’s natural, meal-triggered insulin response.
The “Hepatic Restrictor & Incretin Amplifier” Specialist:
- Mechanism 1 (The Biguanide Anchor – Metformin): Metformin is the absolute global gold standard for early diabetes. It works primarily in the liver, activating the AMPK enzyme to violently suppress hepatic gluconeogenesis (the liver dumping excess sugar into the blood). Furthermore, it actively increases the peripheral sensitivity of muscle cells, allowing them to absorb and burn glucose without requiring extra insulin.
- Mechanism 2 (The DPP-4 Blockade – Linagliptin): While Metformin handles the baseline glucose, Linagliptin handles the post-meal spikes. It violently blocks the Dipeptidyl Peptidase-4 (DPP-4) enzyme, rescuing the body’s natural incretin hormones (GLP-1 and GIP) from destruction. This triggers the pancreas to release precise, glucose-dependent bursts of insulin exactly when the patient eats, while actively suppressing glucagon.
- The Synergistic Compliance Shield: By combining these two distinct pathways into a single Bilayer or Extended-Release tablet, physicians can achieve massive reductions in HbA1c (often > 1.5%) without the extreme weight gain or dangerous, life-threatening hypoglycemia associated with older sulfonylurea combinations (like Glimepiride).
Product Composition & Strength
We supply this product as a Precision-Engineered, API-Segregated Bilayer Tablet, packed exclusively in highly secure, moisture-resistant Alu-Alu blister strips or heavy-gauge HDPE bottles to ensure the absolute chemical stability of the highly hygroscopic combination.
| Active Ingredient | Strength | Primary Clinical Function |
|---|---|---|
| Linagliptin / Metformin HCl (IR) | 2.5 mg / 500 mg 2.5 mg / 850 mg 2.5 mg / 1000 mg | Twice-Daily Standard: Immediate-release units designed to be taken twice a day with meals to provide rapid, meal-time incretin spikes alongside baseline hepatic suppression. |
| Linagliptin / Metformin HCl (ER) | 5 mg / 1000 mg (ER) | Once-Daily Premium Standard: High-efficacy Extended-Release therapy designed for ultimate patient compliance, delivering the full daily dose of Linagliptin while slowly trickling Metformin into the gut over 24 hours to prevent severe gastrointestinal side effects. |
| Excipients | Hypromellose (HPMC) / Copovidone / Microcrystalline Cellulose / Magnesium Stearate / Premium Moisture-Barrier Film | ER Polymer / Binder / Diluent / Lubricant (Engineered utilizing elite Bilayer Rotary Presses to physically separate the delicate 2.5mg/5mg Linagliptin dose from the massive, moisture-drawing Metformin layer, preventing cross-degradation) |
*Pack Sizes: 10×10 Alu-Alu Blisters or Bottles of 60 (Optimized specifically for strict, massive-volume chronic diabetic dispensing regimens).
Technical & Logistics Specifications
Critical data for Pharmaceutical Importers, Endocrinology Distributors, and Hospital Procurement Boards.
| HS Code | 3004.90.99 (Medicaments containing other active substances – Endocrinology / Antidiabetic FDC) |
| CAS Numbers | 668270-12-0 (Linagliptin) / 1115-70-4 (Metformin HCl) |
| Dosage Form | Film-Coated Bilayer Tablet (Immediate Release or Extended Release variants) |
| Packaging | Heavy-Gauge Alu-Alu Blisters or Desiccant-Integrated HDPE Bottles (STRICTLY MANDATORY). Metformin is extremely hygroscopic (pulls moisture from the air), which will destroy the Linagliptin component. Strict barrier packaging guarantees absolute chemical stability across Zone IVb tropical climates. |
| Storage | Store strictly below 25°C in a dry place. Protect heavily from Moisture. |
Manufacturing Authority
Marketed and Distributed by Healthy Inc from WHO-GMP & ISO 9001:2015 certified units.
- Macro/Micro Bilayer Segregation Engineering (CRITICAL COMPLIANCE): Compounding a 1000 mg dose and a 2.5 mg dose into the same pill is an extreme thermodynamic challenge. Our facilities utilize advanced climate-controlled (RH < 40%) Bilayer Rotary Presses. We physically separate the Metformin matrix from the Linagliptin matrix into two distinct, color-coded layers within the same tablet. This guarantees flawless Content Uniformity (CU) for the Linagliptin micro-dose, completely eliminates API cross-talk, and ensures absolute clinical reliability for long-term metabolic management.
Therapeutic Indications (Human Use)
Indicated for the comprehensive, step-up management of metabolic dysfunction:
- Type 2 Diabetes Mellitus: As an adjunct to diet and exercise to improve glycemic control in adult patients when treatment with both linagliptin and metformin is appropriate.
- Step-Up Therapy: The mandated second-line intervention for patients inadequately controlled on maximally tolerated doses of Metformin alone.
Dosage & Administration
Recommended Dosage (Strictly as per Endocrinologist Guidelines):
- Immediate-Release (IR): Typically taken twice daily (e.g., 2.5mg/500mg or 2.5mg/1000mg BID).
- Extended-Release (ER): Typically taken once daily (e.g., 5mg/1000mg) with the evening meal.
- Administration (THE MEALTIME RULE): To drastically reduce the severe gastrointestinal side effects (nausea, violent diarrhea) associated with Metformin, these tablets MUST be taken with meals. Extended-Release tablets must be swallowed whole and never crushed, chewed, or split.
Safety Warnings (CRITICAL Regulatory & Clinical Data):
- BLACK BOX WARNING (Lactic Acidosis): Metformin accumulation can trigger a rare but highly fatal (50% mortality) metabolic complication known as Lactic Acidosis. The risk massively increases in patients with renal impairment, sepsis, or excessive alcohol intake.
- The Renal Paradox (CRITICAL CLINICAL DISTINCTION): While standalone Linagliptin is 100% safe for failing kidneys, Metformin is highly toxic in severe renal disease. Therefore, this combination drug is strictly contraindicated in patients with an eGFR < 30 mL/min/1.73 m². Renal function must be verified before prescribing.
- Radiologic Contrast Warning: Therapy must be temporarily halted before any imaging procedure involving intravascular iodinated contrast materials, as this can crash the kidneys and trigger acute Lactic Acidosis.
- Acute Pancreatitis & Severe Arthralgia: Like all DPP-4 inhibitors, patients must be warned to immediately report severe, radiating back pain (pancreatitis) or crippling, sudden joint pain.
Global Export & Contract Manufacturing Services
Healthy Inc stands as a premier Pharmaceutical Exporter in India, dedicated to serving international Pharma Traders, Wholesalers, and Diabetic Care Networks. As a verified Medicine Supplier in Mumbai, we offer flexible Third Party Manufacturing (Contract Manufacturing) services for Advanced Antidiabetics, Bilayer FDCs, and Extended-Release Formulations. Whether you are looking for a reliable Government Tender Supplier for metabolic clinics in Africa or a B2B Pharma Marketplace partner for Latin America, our highly regulated logistics network ensures timely, secure delivery of WHO-GMP certified products.