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Ozagrel compound, preparation method and pharmaceutical composition of ozagrel compound

A compound and composition technology, applied in the field of medicine, can solve the problems of local circulation disorders, tissue hypoxia, allergic reactions, etc., and achieve the effects of good resolubility, little change in insoluble particles, and good stability

Active Publication Date: 2015-03-11
北京科创鼎诚医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Insoluble particles in intravenous infusion can cause harm to the human body. For example, larger insoluble particles can cause local circulation disorders and cause vascular embolism; too many particles can cause local blockage and insufficient blood supply, and further lead to tissue hypoxia and edema. And phlebitis, can also cause granuloma, allergic reaction, pyrogen-like reaction, etc., all of which can cause harm to the human body

Method used

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  • Ozagrel compound, preparation method and pharmaceutical composition of ozagrel compound
  • Ozagrel compound, preparation method and pharmaceutical composition of ozagrel compound
  • Ozagrel compound, preparation method and pharmaceutical composition of ozagrel compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] [Example 1] Ozagrel compound

[0059] 1) Prepare mixed solution A by mixing dimethylformamide and methanol at a volume ratio of 1:4;

[0060] 2) Take the raw drug of ozagrel, and add the mixed solution A prepared in step 1) under an ultrasonic field with a power of 0.6KW, wherein the ratio of the volume of the mixed solution A to the mass of the raw drug of ozagrel is 6ml: 1g; after all dissolved, turn off the ultrasonic field, add 0.1% g / ml activated carbon to the obtained solution for decolorization, and filter to obtain a clear solution;

[0061] 3) Prepare mixed solution B with tetrahydrofuran and chloroform at a volume ratio of 1:3.5;

[0062] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) at a stirring speed of 850r / min, where the amount of mixed solution B added is 8 times the volume of mixed solution A, and cool down after adding After standing at 3°C ​​for 2.5 hours, crystals were precipitated and dried to obtain the oz...

preparation Embodiment 1

[0070] [Preparation Example 1] Sodium Ozagrel for Injection

[0071] Specification: 20mg (calculated as ozagrel sodium)

[0072] prescription:

[0073]

[0074] Preparation Process:

[0075] (1) Weigh the prescribed amount of ozagrel prepared in Example 1, add water for injection with a volume of 40% of the prescribed amount, add dropwise the prescribed amount of 1moL / L sodium hydroxide solution to dissolve the main ingredient, and add water for injection to the prescription Measure 80% of the volume, adjust the pH to about 9.0 with 1mol / L sodium hydroxide, add 0.1% (g / ml) activated carbon for room temperature adsorption, stir for about 20 minutes, decarbonize and filter, add water for injection to the total amount , sterile filtration;

[0076] (2) Intermediate determination (pH value and content) of the filtrate;

[0077] (3) Subpackage after passing the test, adopt quick-freezing method, and freeze-dry; the freeze-drying adopts the following process: the freeze drye...

preparation Embodiment 2

[0079] [Preparation Example 2] Sodium Ozagrel for Injection

[0080] Specification: 40mg (calculated as ozagrel sodium)

[0081] prescription:

[0082]

[0083] Preparation process: same as formulation example 1, except that the ozagrel used is the ozagrel prepared in example 2.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to an ozagrel compound, a preparation method and a pharmaceutical composition of the ozagrel compound. The X-ray powder diffraction spectrogram obtained by Cu-K alpha-ray measurement is shown in a figure 1; and the structural formula is as shown in a formula (I). The ozagrel compound is a novel crystal form which is different from that in the prior art. The novel crystal form ozagrel compound has humidity, temperature and illumination stability obviously superior to those of the ozagrel in the prior art; sodium ozagrel for injection, prepared from the ozagrel compound of such crystal form, is high in redissolving performance, and insoluble particles have smaller change after an injection solution is combined; after redissolving, the contents of specific impurities I and II in the solution are obviously less than those in the prior art.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an ozagrel compound, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Thrombotic disease is one of the main diseases that endanger human life and health, especially cardiovascular and cerebrovascular diseases. The death rate caused by cardiovascular and cerebrovascular diseases in the world has been ranked second in the total death population, and it is expected to rise to the first place by 2020. The morbidity and mortality of cardiovascular and cerebrovascular diseases in my country are increasing year by year. According to statistics, there are more than 2 million new cerebral embolism and heart embolism patients in my country every year. [0003] Ozagrel is a new type of anti-platelet aggregation drug. It is the first specific thromboxane synthase A2 (TXA2) inhibitor launched by Ono Pharmaceutical Co., Ltd. in Japan un...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/56A61K31/4174A61K9/19A61P7/02A61P9/10
Inventor 李琦杨磊
Owner 北京科创鼎诚医药科技有限公司
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