Hypotensive drug urapidil hydrochloride composition water injection

A technology of urapidil and its composition, which is applied in the field of water injection of the antihypertensive drug urapidil composition, can solve the problems of increasing the risk of drug use for patients, the toxicity of patients, and affecting the quality of drugs, and achieves a level of fluidity suitable for clinical application. Improved, simple composition effect

Inactive Publication Date: 2015-12-02
杨献美
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because urapidil hydrochloride is easily soluble in water and slightly soluble in organic solvents (such as ethanol), urapidil hydrochloride is not easy to be refined by general purification processes such as recrystallization, and the quality of urapidil hydrochloride after refining It cannot meet the requirements of China's national drug standard WS-(X-116)-2003Z, especially the clarity of which is >No. 2 standard turbidity liquid, and the quality cannot meet the purity requirements of injection drugs. Therefore, the purification of urapidil is particularly important
[0006] Urapidil in the prior art has disadvantages such as poor stability, easy decomposition and deterioration, and difficult storage under special circumstances (such as high temperature and light), which are largely limits the wide application of the drug
Find that there is a certain amount of oxidative degradation product I in the urapidil in the prior art through a large number of experimental studies simultaneously, as impurity, it shows the risk that has toxicity to patient or is harmful in other respects, has had a strong impact on the quality of medicine, increases patient risk
The existing technology solves the problems of water solubility and stability by changing the excipients and preparation methods of the preparation. It must rely on specific prescriptions and processes to achieve its stable effect, which brings certain limitations to the preparation of preparations and the selection of excipients. sex

Method used

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  • Hypotensive drug urapidil hydrochloride composition water injection
  • Hypotensive drug urapidil hydrochloride composition water injection
  • Hypotensive drug urapidil hydrochloride composition water injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1: the preparation of urapidil crystal

[0027] (1) Dissolving crude urapidil into a mixed solution of ethanol and carbon tetrachloride whose volume is 10 times the weight of uradil at 35°C, the volume ratio of ethanol and carbon tetrachloride is 4:2.5;

[0028] (2) Decolorize by adding activated carbon whose weight is 0.2 times the weight of urapidil, and filter to obtain urapidil solution;

[0029] (3) Warm up the uradil solution to 40°C, add propyl ether dropwise to the uradil solution under the condition of stirring, the volume of propyl ether is 8 times the weight of uradil, and the dropwise addition is completed at a uniform speed within 0.5h. The stirring rate is 30rmp;

[0030] (4) After the dropwise addition, cool down to -10°C at a rate of 15°C / hour, continue stirring at a stirring rate of 15rmp for 2h, let stand for 3h to precipitate crystals, filter, wash, and vacuum-dry to obtain urapidil crystals.

[0031] The X-ray powder diffraction pattern ...

Embodiment 2

[0032] Embodiment 2: the preparation of urapidil composition

[0033] The composition is: 1 part by weight of urapidil crystal prepared by the present invention, and 0.04 part by weight of calcium chloride.

[0034] The preparation method is:

[0035] Get the prescription amount of uradil and calcium chloride, add water for injection to dissolve, add 2% gac of uradil weight and stir at room temperature for 30 minutes, filter to remove carbon, add water for injection to the filtrate to 2000ml, pass through a 0.22 μm filter membrane, and divide Fill it into a 2ml ampoule, sterilize it by autoclaving at 121°C for 45 minutes, and inspect it with light to get urapidil water injection.

Embodiment 3

[0036] Embodiment 3: the preparation of urapidil composition

[0037] The composition is: 1 part by weight of urapidil crystal prepared by the present invention, and 0.05 part by weight of calcium chloride.

[0038] The preparation method is:

[0039] Get the prescription amount of uradil and calcium chloride, add water for injection to dissolve, add 2% gac of uradil weight and stir at room temperature for 30 minutes, filter to remove carbon, add water for injection to the filtrate to 2000ml, pass through a 0.22 μm filter membrane, and divide Fill it into a 2ml ampoule, sterilize it by autoclaving at 121°C for 45 minutes, and inspect it with light to get urapidil water injection.

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PUM

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Abstract

The invention discloses a hypotensive drug urapidil hydrochloride composition water injection, and belongs to the technical field of medicines. The composition consists of urapidil hydrochloride and calcium chloride; urapidil hydrochloride is crystal; an X-ray powder diffraction diagram obtained by measurement by using Cu-Ka rays is represented in figure 1. The new crystal form of the urapidil hydrochloride provided by the invention is different from a crystal form structure in the prior art; a test shows that compared with the prior art, the hypotensive drug urapidil hydrochloride composition water injection has the advantages that the compound with the new crystal form is high in stability, the content of an impurity I is extremely low, and the total content of impurities is also controlled within a lower range; furthermore, with the prolonging of the storage time, the change of the content is smaller. Meanwhile, the dissolving property and the flowability of the urapidil hydrochloride crystal compound in water are obviously improved when compared with the prior art; the water injection prepared from the compound of the new crystal form is simple in constituent, high in stability and very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicines, and relates to an aqueous injection of the antihypertensive drug urapidil composition. Background technique [0002] Hypertension is a kind of common disease, frequently-occurring disease. With the improvement of people's living standards, the number of hypertensive patients is increasing day by day, especially the number of hypertensive crisis and severe hypertensive patients is constantly increasing, but there are few safe and effective injection drugs clinically used for this type of disease. High blood pressure affects work and life, and high blood pressure is the most important risk factor for coronary heart disease and cerebrovascular disease. 50% of myocardial infarction patients are hypertensive patients, and 76% of stroke patients have a history of hypertension. Therefore, the risk of high blood pressure is sudden death or disability. Hypertensive patients should learn how to take c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/513C07D239/545A61P9/12
Inventor 杨献美
Owner 杨献美
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