Telmisartan is a non-peptide active pharmaceutical ingredient functioning as a selective angiotensin II receptor blocker (ARB). Manufactured via multi-step organic synthesis, it is designed for solid oral dosage formulation. The production process relies on strict control of critical intermediates, heterocyclization reactions, and multi-stage crystallization to achieve specific polymorphic forms required for optimal bioavailability. It serves as a primary active component in cardiovascular therapeutics targeting hypertension and associated renal complications.
Product Information
|
Parameter |
Technical Specification |
|
International Nonproprietary Name (INN) |
Telmisartan |
|
CAS Number |
144701-48-4 |
|
Molecular Formula |
C33H30N4O2 |
|
Molecular Weight |
514.62 g/mol |
|
Structural Formula Class |
Biphenyl-benzimidazole derivative |
|
Therapeutic Category |
Cardiovascular Agent / Angiotensin II Receptor Blocker (ARB) |
|
Pharmacopeial Compliance |
USP / EP / BP |
|
Storage Conditions |
Preserve in tight containers, store below 25°C, protect from moisture and light |
|
Shelf Life |
36 Months |
Quality & Specification
|
Test Parameter |
Acceptance Criteria (USP/EP Standards) |
|
Appearance |
White or almost white crystalline powder |
|
Identification (IR / HPLC) |
Matches reference standard |
|
Assay (Calculated on dried basis) |
98.0% – 102.0% |
|
Loss on Drying |
≤ 0.5% |
|
Residue on Ignition |
≤ 0.1% |
|
Heavy Metals |
≤ 10 ppm |
|
Individual Specified Impurity |
≤ 0.10% |
|
Total Impurities |
≤ 0.5% |
|
Residual Solvents (GC) |
Compliant with ICH Q3C limits (Methanol, Acetone, Toluene) |
|
Particle Size Distribution ($D_{90}$) |
Customization available per direct compression or granulation requirements |
Manufacturing & Supply
|
Operational Metric |
Production Standard |
|
Facility Compliance |
Current Good Manufacturing Practice (cGMP) |
|
Synthesis Route |
Verified non-infringing proprietary route via customized condensation and ring-closure steps |
|
Batch Scale |
Commercial scale (100 kg to 500 kg per batch) |
|
Process Control |
Automated Distributed Control Systems (DCS) for reaction temperature and pressure regulation |
|
Purification Method |
Multi-stage recrystallization and activated carbon treatment for heavy metal removal |
|
Supply Capacity |
Multi-metric tons annual production capacity with dedicated campaign scheduling |
Documentation
Drug Master File (DMF): Open/Closed part available for regulatory submission in ICH regions.
Certificates: Written Confirmation (WC) for active substances exported to the European Union, CEP (Certificate of Suitability) support data.
Analytical Packages: Certificate of Analysis (CoA) provided per commercial batch; HPLC chromatograms, residual solvent test reports, and particle size distribution curves included.
Compliance Dossiers: ICH Q3A/Q3B impurity profiles, Genotoxic impurity assessment reports, TSE/BSE free declarations, and melamine-free statements.
Packaging
|
Packaging Layer |
Material Specification |
|
Inner Layer |
Double-tied low-density polyethylene (LDPE) pharmaceutical-grade bags |
|
Secondary Layer |
Food/Pharma-grade aluminum foil barrier bag, vacuum heat-sealed to prevent moisture ingress |
|
Outer Container |
Rigid fiber drum or HDPE drum equipped with tamper-evident security seals |
|
Standard Net Weight |
25 kg / drum |
|
Labeling |
Compliant with international GDP standards including product name, CAS number, batch number, net weight, manufacturing date, retest date, and storage instructions |
Pharmaceutical Application
Essential Hypertension Management: Formulated into oral tablets to manage primary hypertension by blocking vasoconstrictive pathways. It effectively lowers systemic blood pressure and reduces cardiovascular morbidity in adult populations.
Cardiovascular Risk Reduction: Utilized in secondary prevention medications designed for patients with manifested atherothrombotic cardiovascular disease or type 2 diabetes with documented end-organ damage.
Diabetic Nephropathy Protection: Incoporated into combination or single-agent formulations prescribed to slow the progression of renal disease in hypertensive type 2 diabetic patients.
Fixed-Dose Combinations (FDCs): Employed as an active core component in combination therapies alongside diuretics (such as hydrochlorothiazide) or calcium channel blockers (such as amlodipine) for synergistic blood pressure control.
FAQ
Q: What is the standard batch size available for commercial orders?
A: Standard commercial batches are manufactured at multi-hundred-kilogram scales, with customized batch pooling available upon agreement.
Q: Is the Drug Master File (DMF) accessible for regulatory filings?
A: Yes, comprehensive DMF documentation is active and available for cross-referencing in major regulated markets upon submission of a letter of access.
Q: What polymorphic form is delivered in commercial shipments?
A: The material is supplied consistently as Form A, verified via X-ray powder diffraction (XRPD) to ensure predictable dissolution and bioavailability profiles during formulation.
Q: How are moisture-sensitive parameters controlled during transit?
A: Shipments utilize double-bagged polyethylene layers enclosed in vacuum-sealed aluminum foil liners inside rigid drums, protecting the API from humidity and light degradation.
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