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Acid diltiazem compound with good stability, and pharmaceutical composition

A technology for diltiazem hydrochloride and a composition, which is applied in the field of high-purity diltiazem hydrochloride compounds and pharmaceutical compositions, can solve the problems of a large number of impurities in diltiazem hydrochloride, inconvenient use, storage and transportation, unstable angina pectoris, etc., and achieves insoluble particles of finished products. Qualification, reduce market risk, and improve the effect of clarity

Inactive Publication Date: 2014-09-17
天津梅花医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0033] (4) Unstable angina
[0042] During the research process, repeating the method of the above patent literature, the obtained diltiazem hydrochloride has more impurities, higher total amount of impurities, and poor stability
The diltiazem hydrochloride produced by the prior art has very strict requirements on storage and protection from light, and is inconvenient in use, storage and transportation

Method used

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  • Acid diltiazem compound with good stability, and pharmaceutical composition
  • Acid diltiazem compound with good stability, and pharmaceutical composition
  • Acid diltiazem compound with good stability, and pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] Preparation of diltiazem hydrochloride compound

[0110] Proceed as follows:

[0111]

[0112] Step 1: Preparation of Compound II: Add Compound III (100g) into a pressure-resistant reactor: Reaction solvent: Dimethylaminochloroethane: Potassium carbonate = 1:10:1:3, replace the system with nitrogen 5 times, Stir and heat up to 120°C to 160°C to react for 8-15 hours, cool to room temperature, filter, and concentrate the filtrate to obtain Compound II, 87.5g;

[0113] The second step: preparation of compound Ⅰ: add compound Ⅱ to dry dichloromethane, compound Ⅱ:dichloromethane=1:30, stir for 10 minutes, filter to remove inorganic salts, transfer the filtrate into a reaction flask, add acetyl chloride, Compound Ⅲ: Acetyl chloride = 1:0.6, stirred, heated and refluxed for 6 hours, after the reaction was completed, concentrated under reduced pressure until the volume was about half of the volume before concentration,

[0114] Stir, cool to room temperature, filter, wash th...

Embodiment 2

[0116] The described diltiazem hydrochloride pharmaceutical composition of every 1000 bottles, its formula consists of:

[0117]

[0118] Preparation process: Take 70% of the prescribed amount of water for injection, at a temperature of 65-85°C, add the prescribed amount of edetate calcium sodium, stir to dissolve; add the prescribed amount of diltiazem hydrochloride, stir until dissolved, then add the prescription to the solution Amount of mannitol, stirred until completely dissolved; measure the initial pH value, according to the initial pH value, use 10% hydrochloric acid solution or 10% sodium hydroxide solution to adjust the pH value range to 4.0-6.0; add 0.05% of water for injection Use charcoal, stir, and stand for 30 minutes; filter to remove charcoal, add water for injection to the prescribed amount, mix well; use 0.45 μm and 0.22 μm microporous membrane filter; fill; freeze-dry, start the freeze-dryer, and After the sample was pre-frozen at -45°C for 6 hours, star...

Embodiment 3

[0120] The described diltiazem hydrochloride pharmaceutical composition of every 1000 bottles, its formula consists of:

[0121]

[0122] The preparation process is the same as in Example 1.

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Abstract

The invention discloses an acid diltiazem compound, a preparation method and a pharmaceutical composition thereof. The acid diltiazem compound disclosed by the invention has the advantages that the acid diltiazem compound is high in chemical purity, good in stability, especially good in stability of light and heat; the maximal impurity is smaller than 0.1%; the pharmaceutical composition of the acid diltiazem compound prepared by a specific technology is good in light resistance, good in stability, easy to implement, significant in economic benefit, and obvious in advantages; not only is the problem of poor stability of the acid diltiazem successfully solved, but also the production cost is reduced; industrialization can be achieved; and the acid diltiazem compound is clinically applied.

Description

technical field [0001] The invention relates to medicines in the field of medicine, in particular to a high-purity diltiazem hydrochloride compound and a pharmaceutical composition. Background technique [0002] Diltiazem hydrochloride is a calcium ion channel blocker, which is characterized by its ability to selectively act on vascular smooth muscle, directly dilate coronary arteries and peripheral blood vessels, reduce blood pressure without reflex heart rate acceleration, and does not increase myocardial oxygen consumption. Safe and effective drugs for the treatment of hypertension, coronary heart disease and angina pectoris. In 1974, it was listed in the United States, Japan, France, Spain and other countries successively. Injection therapy is often used in foreign countries. The development of diltiazem in my country started relatively late, and it was successfully trial-produced and put into production in 1985. Diltiazem is widely used in the treatment of cardiovascul...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D281/10A61K31/554A61P9/12A61P9/10
Inventor 梅开忠黄欣
Owner 天津梅花医药有限公司