Pharmaceutical Bulk Valsartan Powder

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Valsartan Powder Usage and Synthesis.

1, Valsartan does not act on angiotensin-converting enzyme (ACE), renin and other receptors, and does not inhibit ion channels involved in blood pressure regulation and sodium balance;

Valsartan has no inhibitory effect on angiotensin-converting enzyme and does not affect bradykinin levels in the body, thus causing fewer coughing side effects than angiotensin-converting enzyme inhibitors.

2, Reduce elevated blood pressure without affecting heart rate.

3, For most patients, a single oral dose produces an antihypertensive effect within 2 hours, the peak effect is reached in 4-6 hours, and the antihypertensive effect is maintained until more than 24 hours after taking the drug. Maximum antihypertensive efficacy is achieved after 2-4 weeks of treatment and is maintained during long-term therapy. Combination with thiazide diuretics can further enhance the antihypertensive effect.

4, the sudden termination of valsartan treatment, does not cause hypertension "rebound" or other side effects.

5, does not affect the total cholesterol, triglyceride, blood glucose and uric acid levels in hypertensive patients.

Uses and functions of Valsartan.

Valsartan is a widely used antihypertensive drug in clinical practice, which has the advantages of low side effects and good tolerability, and can also be used for the treatment of hypertension in patients with diabetes mellitus and kidney disease.

1, Absorption:

(1) Valsartan is rapidly absorbed after oral administration and its absorption varies widely, with a mean absolute bioavailability of 23% (23 ± 7) and a linear pharmacokinetic profile over the dose range studied. When taken once daily, valsartan rarely caused accumulation and plasma concentrations were similar in men and women.

(2) Taking valsartan with a meal reduced AUC by 48% and peak blood concentration (Cmax) by 59%. Whether or not taken with or without a meal, blood concentrations were similar after 8 h. The reduction in AUC or Cmax had no significant effect on clinical efficacy, and the product can be taken with or without a meal.

2.Distribution:

The vast majority (94-97%) of valsartan is bound to serum proteins (mainly albumin) and reaches steady state within 1 week. The steady-state volume of distribution is about 17L, and plasma clearance is relatively slow (about 2L/h) compared with hepatic blood flow (30L/h).

3, Clearance:

(1) Valsartan is metabolised with multi-exponential decay kinetics (α-phase half-life <1 hour, terminal half-life about 9 hours).

(2) Valsartan is mainly excreted in its native form, 70% from faeces and 30% from urine.

Pharmacological Effects of Valsartan Raw.

Valsartan is an orally effective and specific angiotensin II (AT1) receptor antagonist, which selectively acts on the AT1 receptor subtype and blocks the binding of Ang II to the AT1 receptor (its specific antagonism of the AT1 receptor is approximately 20,000 times greater than that of the AT2 receptor), thereby inhibiting vasoconstriction and aldosterone release, resulting in an antihypertensive effect.

Valsartan does not act on angiotensin-converting enzyme (ACE), renin, and other receptors, and does not inhibit ion channels related to blood pressure and sodium balance; it has no inhibitory effect on angiotensin-converting enzyme, and it does not affect bradykinin levels in vivo, resulting in fewer side effects of coughing than angiotensin-converting enzyme inhibitors.　Valsartan reduces elevated blood pressure without affecting the heart rhythm.

In most patients, a single oral dose produces an antihypertensive effect within 2 hours, with a peak effect in 4-6 hours. The antihypertensive effect is maintained until more than 24 hours after the dose, and maximum antihypertensive efficacy is achieved after 2-4 weeks of treatment and is maintained during long-term therapy. Combination with thiazide diuretics can further enhance the antihypertensive effect.

Abrupt termination of valsartan therapy does not cause "rebound" hypertension or other side effects.　Valsartan does not affect total cholesterol, triglycerides, blood glucose and uric acid levels in hypertensive patients.

Production method of Bulk Valsartan Powder.

2'-Cyanobiphenyl-4-aldehyde (I) and L-valine methyl ester were subjected to reductive amination and the compound (II) obtained was then acylated with valeroyl chloride and chromatographed to give compound (II).

Then it was reacted with Bu3SnN3 to introduce tetrazole and then hydrolysed to give the product.

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