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Hypotensive drug urapidil hydrochloride composition freeze-dried powder injection

A technology of freeze-dried powder injection and urapidil, which is applied in the field of medicine, can solve problems such as poor stability, toxicity to patients, and difficult storage, and achieve good stability, improved fluidity, and low content of insoluble particles.

Inactive Publication Date: 2015-12-30
QINGDAO HUAZHICAO PHARMA CO LTD
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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 Can not reach Chinese national drug standard WS-(X-116)-2003Z requirement, particularly wherein clarity>No. 2 standard turbidity liquid, quality can not meet the purity requirement of injection drug (referring to comparative example 1,2), 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 freeze-dried powder injection
  • Hypotensive drug urapidil hydrochloride composition freeze-dried powder injection
  • Hypotensive drug urapidil hydrochloride composition freeze-dried powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1: the preparation of urapidil crystal

[0032] (1) Grind the crude product of urapidil, pass it through an 80-mesh sieve, then add it into methanol whose volume is 6 times the weight of uradil, and stir at 130 rpm for 10 minutes;

[0033] (2) Add acetone with a volume 4 times the weight of urapidil under stirring at 90 rpm, and raise the temperature to 35°C at the same time;

[0034] (3) After the solution is added, let it stand for 3 hours, and add dropwise a mixed solution of petroleum ether and carbon tetrachloride with a volume of 8 times the weight of uradil at 0°C under the condition of stirring at 150 rpm, petroleum ether, tetrachloride The volume ratio of carbon chloride is 3:1, and the uniform dropwise addition is completed within 2 hours;

[0035] (4) After the dropwise addition, the temperature was lowered to -5°C, and the stirring was continued at a stirring rate of 110 rpm for 2 h, and the crystals were precipitated after standing for 1 h, filt...

Embodiment 2

[0037] Embodiment 2: the preparation of urapidil freeze-dried powder injection

[0038] Prescription: 3 parts by weight of urapidil crystal form compound prepared in Example 1, 15 parts by weight of trehalose;

[0039] Preparation steps: take the urapidil compound of the present invention, stir and dissolve it with water for injection, add the prescribed amount of trehalose, adjust the pH value to 5.0-6.5, then stir until the pH remains constant, then add water for injection until the volume of the solution is uradil 100 times its weight, then coarsely filter with activated carbon, pass through 1.0μm, 0.45μm, 0.22μm microporous membranes in turn to sterilize and filter, filter into a sterile room, measure the pH and content to pass, fill, and press half the plug , put it into a freeze-drying box that has been cooled to -25°C, freeze-dry at low temperature, press the plug out of the box, and roll the cover.

[0040] Described freeze-drying is:

[0041] Pre-freezing: freeze-dr...

Embodiment 3

[0044] Embodiment 3: the preparation of urapidil freeze-dried powder injection

[0045] Prescription: 3 parts by weight of urapidil crystal form compound prepared in Example 1, 18 parts by weight of trehalose;

[0046]Preparation steps: take the urapidil compound of the present invention, stir and dissolve it with water for injection, add the prescribed amount of trehalose, adjust the pH value to 5.0-6.5, then stir until the pH remains constant, then add water for injection until the volume of the solution is uradil 100 times its weight, then coarsely filter with activated carbon, pass through 1.0μm, 0.45μm, 0.22μm microporous membranes in turn to sterilize and filter, filter into a sterile room, measure the pH and content to pass, fill, and press half the plug , put it into a freeze-drying box that has been cooled to -25°C, freeze-dry at low temperature, press the plug out of the box, and roll the cover.

[0047] Described freeze-drying is:

[0048] Pre-freezing: freeze-dry...

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Abstract

The invention discloses a hypotensive drug urapidil hydrochloride composition freeze-dried powder injection and belongs to the technical field of medicine. The composition comprises urapidil hydrochloride and an excipient. The excipient is trehalose, and the urapidil hydrochloride is a novel crystal form compound. The X-ray powder diffraction pattern obtained through Cu-K alpha ray measurement is shown in the picture 1 and is different from urapidil hydrochloride reported in the prior art. Tests prove that compared with the prior art, the solubility and mobility in water of the novel crystal form compound are obviously improved, and the freeze-dried powder injection prepared through the novel crystal form compound is good in stability, good in stability after being combined with a solvent, extremely low in insoluble particle content, and quite suitable for clinic application.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a freeze-dried powder injection of a combination of antihypertensive drug urapidil. 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 ho...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/513C07D239/545A61P9/12
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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