Description
Valsartan belong to non peptide, orally active angiotensin Ⅱ ( AT ) receptor antagonist. It is highly selective for Ⅰ type ( AT1 ) receptor, can be competitive antagonism to without any excitement. It can also be mediated by inhibition of AT1 receptor adrenal cells release aldehyde sterol, but for potassium caused by the release of valsartan no inhibition, it also suggests that valsartan for AT1 receptor selectivity.
The experiments of various types of hypertensive animal models showed that valsartan had a good hypotensive effect, which had no significant effect on cardiac systolic function and heart rate. Animals with normal blood pressure do not have a blood pressure lowering effect. The uptake was rapid and bioavailability was 23 %. The binding rate of plasma protein was 94% ~ 97%. About 70% of the excrement is excreted, and 30% of the renal excretion is in the original form. T1 over 2 beta is about 9 hours. It is not affected by the combination of food and food.
The blood pressure began to decline after 2 hours after taking a patient with high blood pressure, and the maximum blood pressure effect was reached between 4 and 6 hours. The hypotensive effect lasts for 24 hours. The maximal effect of blood pressure was decreased by 2 ~ 4 weeks after continuous use. It can be used in combination with hydrochlorothiazide, and the blood pressure can be enhanced.
Uses
Blood pressure medicine. Valsartan for angiotensin Ⅱ ( Ang Ⅱ) receptor antagonist, can selectively block Ang Ⅱ combined with AT1 receptor ( its specificity of AT1 receptor of antagonism effect about 20000 times greater than AT2 ), thus inhibiting vascular contraction and the release of aldosterone, antihypertensive effect.
Contraindications
The packaging for valsartan includes a warning stating the drug should not be used with the renin inhibitor aliskiren in people with diabetes mellitus. It also states the drug should not be used in people with kidney disease.
Valsartan falls in FDA pregnancy category D and includes a black box warning for fetal toxicity. Discontinuation of these agents is recommended immediately after detection of pregnancy and an alternative medication should be started. The US labeling makes no recommendation regarding continuation or discontinuation of valsartan for breast-feeding mothers. The Canadian labeling does not recommend use by nursing women.
Specification
| Item |
Specification |
Result |
| Appearance |
White to almost white powder |
White powder |
| Identification |
Infrared absorption: The IR spectrum is consistent with that obtained with the reference |
Conforms |
| The retention time of the major peak in the chromatogram of the Assay preparation corresponds to that in the chromatogram of the Standard preparation, as obtained in the Assay. |
Conforms |
| Absorbance |
NMT 0.02% |
Conforms |
| Water |
NMT 2.0% |
0.51% |
| Residue on ignition |
NMT 0.1% |
0.07% |
| Heavy metals |
NMT 0.001% |
Complies |
| Related compounds ( HPLC ) |
Compound A NMT 1.0% |
0.59% |
| Compound B NMT 0.2% |
0.04% |
| Compound C NMT 0.1% |
0.05% |
| Any other individual impurity NMT 0.1% ( excluding compound A ) |
0.07% |
| Total impurities NMT 0.3% ( excluding compound A ) |
0.16% |
| Residual solvents ( GC ) |
Ethyl acetate NMT 5000ppm |
305ppm |
| Dichloromethane NMT 600ppm |
Undetected |
| Methanol NMT 3000ppm |
Undetected |
| N, N - Dimethylformamide NMT 880PPM |
Undetected |
| Assay ( HPLC ) |
98.0%~102.0% |
99.65% |
Advantages:
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Valsartan 137862-53-4 Pharmaceutical Raw Materials
Valsartan 137862-53-4 Pharmaceutical Intermediate
Valsartan 137862-53-4 Raw Chemical Product
Valsartan 137862-53-4 Supplier & manufactuer
China
