+8615902165735
API
0102030405
Telmisartan, Telmisartan API, Telmisartan USP
Products Specification
|
Product Name: |
Telmisartan |
||
|
CAS NO.: |
144701-48-4 |
||
|
Items |
Unit |
Standards |
|
|
Appearance |
- |
Off white to white crystal powder |
|
|
Assay (on dry basis) |
% |
≥99.0 |
|
|
Residue on ignition |
% |
≤0.1 |
|
|
Loss on drying |
% |
≤0.5 |
|
|
Heavy metals |
- |
N.D |
|
|
Residual dissolution |
- |
N.D |
|
|
Conclusion: |
The Product complies with in house standard. |
||
|
Package: |
1kg bag. |
||
|
Storage |
Store in cool, dry and clean places. |
||
Product introduction
1. Basic Properties
Chemical Name: 4'-[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid
Molecular Formula: C₃₃H₃₀N₄O₂
Molecular Weight: 514.63 g/mol
Appearance: White or off-white crystalline powder
Solubility: Practically insoluble in water, freely soluble in DMSO, slightly soluble in methanol
Molecular Formula: C₃₃H₃₀N₄O₂
Molecular Weight: 514.63 g/mol
Appearance: White or off-white crystalline powder
Solubility: Practically insoluble in water, freely soluble in DMSO, slightly soluble in methanol
2. Pharmacological Action
Mechanism: Selective antagonist of angiotensin II type 1 (AT₁) receptors, inhibiting vasoconstriction and aldosterone secretion
Antihypertensive Features: Potent and long-acting (half-life ~24 hours)
Partial PPAR-γ receptor activation may improve insulin sensitivity
Antihypertensive Features: Potent and long-acting (half-life ~24 hours)
Partial PPAR-γ receptor activation may improve insulin sensitivity
3. Clinical Applications
Indications: Essential hypertension (monotherapy or combination therapy)
Cardiovascular risk reduction in high-risk patients (approved in some countries)
Dosage: Typically 40-80 mg/day, maximum 80 mg/day
Advantages: Dual hepatic/renal excretion (no dose adjustment in renal impairment)
Food does not affect absorption
Cardiovascular risk reduction in high-risk patients (approved in some countries)
Dosage: Typically 40-80 mg/day, maximum 80 mg/day
Advantages: Dual hepatic/renal excretion (no dose adjustment in renal impairment)
Food does not affect absorption
4. Pharmacokinetics
Absorption: Oral bioavailability 40-60%, peak plasma concentration in 0.5-1 hour
Metabolism: Minimal CYP450 metabolism (low drug interaction risk)
Excretion: 97% fecal excretion, <1% renal excretion
5. Adverse Effects
Common (>1%): Dizziness, back pain, nasopharyngitis
Rare but serious: Angioedema, hyperkalemia, liver dysfunction
Metabolism: Minimal CYP450 metabolism (low drug interaction risk)
Excretion: 97% fecal excretion, <1% renal excretion
5. Adverse Effects
Common (>1%): Dizziness, back pain, nasopharyngitis
Rare but serious: Angioedema, hyperkalemia, liver dysfunction
6. Contraindications & Precautions
Contraindications:
Pregnancy (Category D teratogenicity)
Severe cholestasis or biliary obstruction
ARB hypersensitivity
Cautions:
Bilateral renal artery stenosis
Volume-depleted patients
7. Research Progress
Potential New Uses:
Adjunctive therapy for metabolic syndrome (PPAR-γ activation)
Investigational for non-alcoholic fatty liver disease (NAFLD)
Contraindications:
Pregnancy (Category D teratogenicity)
Severe cholestasis or biliary obstruction
ARB hypersensitivity
Cautions:
Bilateral renal artery stenosis
Volume-depleted patients
7. Research Progress
Potential New Uses:
Adjunctive therapy for metabolic syndrome (PPAR-γ activation)
Investigational for non-alcoholic fatty liver disease (NAFLD)