Pharmaceutical intermediate Isosorbide Dinitrate Powder

CAS:87-33-2

MF:C6H8N2O8

MW: 236.14

EINECS:201-740-9

Specification​: 99% min Isosorbide Dinitrate Powder

Sample:Isosorbide Dinitrate Powder

Packaging:1kg/bag, 25kg/drum

Brand: Henrikang

Appearance:White Powder

Storage: Cool Dry Place

Shelf Life: 2 Years

Test Method: HPLC

Isosorbide Dinitrate Powder Usage and Synthesis.

Studies on the mechanism of action of nitrate also indicate that its mechanism of action against angina is complex, in general the mechanism of action of isosorbide nitrate against angina has the following aspects:

(1) Reduce myocardial oxygen consumption. Nitrate dilates the venous blood vessels, increases the venous volume, thus reducing the volume of return blood, heart volume decreases, myocardial wall tension decreases, and ejection time is shortened; in addition, the arterial vasculature is diastasised, and the left ventricular afterload is reduced, thus achieving the purpose of lowering myocardial oxygen consumption.

(2) Myocardial blood flow redistribution, which is conducive to the perfusion of the ischemic area. Nitrate selectively expands large coronary transport vessels, increasing the flow in the ischemic area; reduces left ventricular filling pressure, increases endocardial blood supply, and improves left ventricular compliance; it also stimulates the generation of collateral branches, opening up the existing collateral branches and increasing the nutrient blood flow to perfuse the ischemic area.

(3) In atherosclerosis or acute ischemia, endothelial cells are unable to release NO and PGI; however, they accelerate platelet aggregation and the release of contractile substances from vascular endothelial cells.

Exogenous nitrate can supplement the deficiency of endogenous NO and also promote the release of PGI. Nitrate itself has significant anti-platelet aggregation and anti-thrombosis effects. NO is known to be an important biomessenger and effector molecule, and nitrate is one of the NO donor drugs.

Uses and functions of Isosorbide Dinitrate.

The product is a fast-acting, long-acting nitrate anti-angina drug that works in the same way as nitroglycerin, and is mainly used to prevent episodes of angina pectoris before it occurs, but can also be used to relieve symptoms.

Pharmacological Effect of Isosorbide Dinitrate.

Isosorbide nitrate is absorbed completely after oral administration, but the hepatic first-pass effect is more significant, and it is metabolised to 2-mononitroisosorbide and 5-mononitroisosorbide. The plasma half-life is 30-60min, because of the significant first-pass effect and short half-life, isosorbide nitrate is more suitable for making extended-release formulations.

Isosorbide nitrate extended-release preparation of the absorption phase is significantly prolonged, the peak time is pushed back, the peak concentration is lower, the plasma concentration of isosorbide nitrate and its metabolites with the time change is gentle, its haemodynamic effect is smoother.

It can overcome the discomfort caused by the "sudden release" of the ordinary preparation, and isosorbide nitrate extended-release preparation can reduce the number of times of use and improve the compliance.

Preparation of Bulk Isosorbide Dinitrate Powder.

Sorbitol solution is obtained by dehydration cyclisation and esterification with nitric acid.

Specifically as follows: in the reaction bottle equipped with a stirrer, thermometer, add 50g of fuming nitric acid, concentrated sulfuric acid 7.5g, cooled to 10 ℃ with stirring, slowly added by dehydrated sorbitol 10g of solid and 1mL of water microthermal dissolution of the liquid obtained by keeping the reaction liquid temperature at 10 ~ 15 ℃, add the reaction reaction of the heat insulation reaction for 2h. Stirring will be poured into the reaction of 7 times the amount of iced water, stirring fully precipitated crystals.

Filtering, washing to neutral, drying, the crude product. Add the crude product into 1.5 times the amount of 95% ethanol, heat to dissolve, activated carbon decolourization reflux for 30min, while hot filtration, cooled to below 10 ℃, filtration precipitation of crystals, ethanol washing, low temperature drying, isosorbide nitrate, yield 70%.