Rosuvastatin azelnidipine composition

A technology of rosuvastatin and azedipine, which is applied in the direction of drug combination, metabolic disease, cardiovascular system disease, etc., can solve the problems of difficult control of drug effect and inconvenient taking, and achieve convenient taking, stable physical and chemical indicators, and reduced The effect of myocardial infarction

Inactive Publication Date: 2009-01-07
QINGDAO HUANGHAI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the drug effect is difficult to control, and it is inconvenient to take

Method used

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  • Rosuvastatin azelnidipine composition
  • Rosuvastatin azelnidipine composition
  • Rosuvastatin azelnidipine composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation of Azedipine:

[0044] Acetate of 1-benzhydryl-3-azetidinylamidinoacetate

[0045]

[0046] In a 2000ml reaction flask, add 1500ml of dichloromethane, 153g (0.5mol) of 1-benzhydryl-3-azetidinyl cyanoacetate, 35ml (0.6mol) of absolute ethanol, and ice-salt bath Cool at -5°C, pass through dry hydrogen chloride gas (prepared by 140g of sodium chloride) for 2h, stir the reaction solution below -5°C for 3h, overnight at 0°C, pass through nitrogen at -5°C for 2h, and pass through at -5°C Add ammonia gas for 3 hours, add 1000ml of cold 10% ammonia water under stirring, separate the organic layer, dry over anhydrous sodium sulfate, concentrate to dryness at room temperature in vacuo, add 500ml of acetonitrile and 46g (0.6mol) of ammonium acetate to the residue, and react the mixture at 55°C for 2h , cooled, filtered, the mother liquor was concentrated to dryness in vacuum, crystallized by adding toluene, filtered to obtain 117 g of acetate, with a yield of 61%. ...

Embodiment 2

[0051] Preparation of Rosuvastatin:

[0052]

[0053] In a 500ml reaction bottle, add rosuvastatin calcium 30g, water 150ml, ethanol 150ml, add dropwise 10% sodium carbonate aqueous solution 50ml under stirring, add, filter, wash calcium carbonate with 50% ethanol aqueous solution 100ml, combine filtrate, use 10% hydrochloric acid aqueous solution neutralized the pH5, extracted 3 times with 300 ml of dichloromethane, combined the dichloromethane layers, washed with saturated saline, recovered the dichloromethane to obtain 24 g of rosuvastatin.

Embodiment 3

[0055] Preparation of Rosuvastatin Azeldipine Salt:

[0056]

[0057] Add an organic solvent such as 600ml of dichloromethane into a 1000ml reaction flask, add 58.3g of azedipine and 48.2g of rosuvastatin under stirring, stir at 45°C until completely dissolved, concentrate in vacuo to dryness, add 200ml of methanol, and heat to 55 ℃, add 2g of activated carbon, heat filter, cool to crystallize, and filter to obtain rosuvastatin azeldipine salt 98g, mp76℃, FAB-MS: m / z 1087[M+Na] +

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Abstract

A pharmaceutical composition is an organic salt formed by an organic acid rosuvastatin and an organic base azelnidipine with a molar ratio of 1:1. The pharmaceutical composition can be made into any dosage forms together with a pharmaceutically-acceptable carrier for reducing blood pressure and blood lipid, reducing myocardial infarction and treating cerebral apoplexy. The inventive pharmaceutical composition has the advantages of stable physiochemical indexes, controllable product quality, and convenient administration.

Description

technical field [0001] The present invention relates to an organic salt formed by organic acid rosuvastatin and organic base azelnidipine, and the medicinal effect of the composition on lowering blood fat and blood pressure, in particular to the rosuvastatin alzeldipine composition Background technique [0002] The morbidity and mortality of cardiovascular, cerebrovascular and renal vascular diseases in my country are increasing year by year, and there is a trend of gradually getting younger. Hypertension and hyperlipidemia are the main causes of diseases such as atherosclerosis, angina pectoris, myocardial infarction, cerebral infarction, and kidney damage. A large number of research data show that many hypertensive patients are accompanied by lipid metabolism disorders, and the content of cholesterol and triglycerides in the blood is significantly higher than that of normal people. Many hyperlipidemias are often combined with hypertension, and the two are causally related...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61K31/4427A61P9/12A61P3/06A61P9/10
Inventor 孙桂荣高义才安良吴康王素云
Owner QINGDAO HUANGHAI PHARM CO LTD
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