Hypotensive drug urapidil hydrochloride composition water injection

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...

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

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