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Urapidil composition freeze-dried powder injection for treating hypertension

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

Inactive Publication Date: 2015-11-18
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 It cannot meet the requirements of the Chinese National Drug Standard WS-(X-116)-2003Z, especially the clarity>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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  • Urapidil composition freeze-dried powder injection for treating hypertension
  • Urapidil composition freeze-dried powder injection for treating hypertension
  • Urapidil composition freeze-dried powder injection for treating hypertension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1: Preparation of urapidil crystals

[0029] (1) Mix acetone, ethanol, and N,N-dimethylformamide into a mixed solvent, and the volume ratio of acetone, ethanol, and N,N-dimethylformamide is 2:4:1;

[0030] (2) Take urapidil raw material, dissolve it in a mixed solvent of acetone, ethanol, N,N-dimethylformamide whose volume is 6 times the weight of uradil in step (1), heat up to 35°C, Stir until completely dissolved to obtain urapidil solution;

[0031] (3) Under the condition of a stirring speed of 560r / min, add the urapidil solution in step (2) into acetone whose volume is 5 times the weight of urapidil, mix to form a suspension, and mix at 10°C / min Cool down to -10°C at a faster rate;

[0032] (4) Perform suction filtration, wash the filter cake, and then vacuum-dry the filter cake to obtain a crystalline powder, which is the urapidil compound.

[0033] The X-ray powder diffraction pattern obtained by measuring the obtained urapidil crystal using Cu-Kα ra...

Embodiment 2

[0034] Example 2: Preparation of urapidil freeze-dried powder injection

[0035] Prescription: 3 parts by weight of the urapidil crystal form compound prepared in Example 1 and 1.5 parts by weight of low molecular weight dextran.

[0036] Preparation:

[0037] Take the urapidil compound of the present invention, stir and dissolve it with water for injection, add the prescribed amount of low-molecular dextran, adjust the pH value to 5.0-6.5, and then stir until the pH remains constant, then add water for injection until the volume of the solution is uradil 150 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 pH and content after passing, fill, press half stopper , put it into a freeze-drying box that has been cooled to -40°C, freeze-dry, press the plug out of the box, and roll the cover.

[0038] Described freeze-drying is:

[0039] Pre...

Embodiment 3

[0040] Example 3: Preparation of urapidil freeze-dried powder injection

[0041] Prescription: 3 parts by weight of the urapidil crystal form compound prepared in Example 1 and 2.25 parts by weight of low molecular weight dextran.

[0042] Preparation:

[0043]Take the urapidil compound of the present invention, stir and dissolve it with water for injection, add the prescribed amount of low-molecular dextran, adjust the pH value to 5.0-6.5, and then stir until the pH remains constant, then add water for injection until the volume of the solution is uradil 150 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 pH and content after passing, fill, press half stopper , put it into a freeze-drying box that has been cooled to -40°C, freeze-dry, press the plug out of the box, and roll the cover.

[0044] Described freeze-drying is:

[0045] Pre...

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Abstract

The invention discloses a urapidil composition freeze-dried powder injection for treating hypertension, belonging to the technical field of medicines. The composition comprises urapidil and an excipient. Urapidil is a compound in a new crystal form and is different from urapidil reported in the prior art. An X-ray powder diffraction pattern obtained through measurement by using a Cu-Kalpha ray is shown in a drawing 1 in the specification. Through tests, compared with the prior art, the compound in the new crystal form has good stability and lower impurity I content. The total impurity content is also controlled in a lower range and is slightly changed with increase of the storage time. The powder injection has the beneficial effects that the solubility and flowability of the powder injection in water are obviously improved compared with the solubility and flowability of the prior art; and the freeze-dried powder injection prepared by utilizing the compound in the new crystal form has good stability after undergoing compatibility with solvents, has low content of insoluble particles and is very suitable to apply clinically.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a freeze-dried powder injection of urapidil composition for treating hypertension. 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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/513C07D239/545A61P9/12
Inventor 刘学键
Owner QINGDAO HUAZHICAO PHARMA CO LTD
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