Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Medicine urapidil composition for treating senile hypertensive crisis

A technology of urapidil and a composition is applied in the field of drug urapidil composition for treating hypertensive crisis in the elderly, can solve the problems of poor stability, difficult storage, toxicity of patients, etc., and achieves good stability and insoluble particles. Low content and improved flowability

Inactive Publication Date: 2015-11-25
QINGDAO HUAZHICAO PHARMA CO LTD
View PDF2 Cites 0 Cited by
  • 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, urapidil hydrochloride is not easy to be refined by general purification processes such as recrystallization, and the quality of urapidil hydrochloride after refining cannot reach the national standard of China. The requirements of the drug standard WS-(X-116)-2003Z, especially the clarity of which is >No. 2 standard turbidity liquid, 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Medicine urapidil composition for treating senile hypertensive crisis
  • Medicine urapidil composition for treating senile hypertensive crisis
  • Medicine urapidil composition for treating senile hypertensive crisis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Preparation of urapidil crystals

[0026] (1) Grind the crude product of urapidil, pass through a 90-mesh sieve, and add it to a mixed solution of N-methylacetamide and ethanol whose volume is 10 times the weight of uradil. The volume ratio is 1:3, and the temperature is raised to 30°C while stirring; the stirring speed is 180 rpm; add activated carbon, stir for 50 minutes and then sterile filter;

[0027] (2) Add distilled water while stirring, and lower the temperature to -15°C at the same time; the stirring speed is 240 rpm; the volume of distilled water is 7 times the weight of urapidil, and the adding speed is 95 ml / min; the cooling rate is 10°C / min. Hour;

[0028] (3) After adding the mixed solvent, the obtained crystals were left to stand for crystallization; filtered, washed, and vacuum-dried for 6 hours to obtain the urapidil compound.

[0029] The X-ray powder diffraction pattern obtained by measuring the obtained urapidil crystal using Cu-Kα ra...

Embodiment 2

[0030] Example 2: Preparation of urapidil composition

[0031] The composition is: 1 part by weight of urapidil crystal prepared by the present invention, and 0.001 part by weight of anhydrous sodium carbonate.

[0032] The preparation method is:

[0033] (1) Weigh urapidil crystals and anhydrous sodium carbonate in proportion and mix them thoroughly;

[0034] (2) Dispense into sterilized vials and stopper them.

Embodiment 3

[0035] Example 3: Preparation of urapidil composition

[0036] The composition is: 1 part by weight of urapidil crystal prepared by the present invention, and 0.0015 part by weight of anhydrous sodium carbonate.

[0037] The preparation method is:

[0038] (1) Weigh urapidil crystals and anhydrous sodium carbonate in proportion and mix them thoroughly;

[0039] (2) Dispense into sterilized vials and stopper them.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a medicine urapidil composition for treating senile hypertensive crisis, and belongs to the technical field of medicines. The composition comprises urapidil and anhydrous sodium carbonate. The urapidil is crystal, and an X-ray powder diffraction pattern shown in Figure 1 is obtained through Cu-Kalpha radioactive measurement. The new crystalline form of urapidil provided by the invention is different from a crystal structure in the prior art. Experiments show that the composition with the new crystalline form is high in stability and very low in content of an impurity I compared with those in the prior art; the content of all impurities is controlled at a lower range, and the content of the impurities is reduced along with the extension of storage time; the solubility and the flowability of the composition in water are obviously improved compared with those in the prior art; a powder-injection prepared from the composition is high in stability, high in stability after being mixed with a solvent, very low in content of insoluble particles, and very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a drug urapidil composition for treating hypertensive crisis in the elderly. 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 ta...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/513A61K47/04C07D239/545A61P9/12
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products