Medicinal urapidil composition for treating severe hypertension

Abstract

The invention relates to a medicinal urapidil composition for treating severe hypertension and belongs to the technical field of medicine. The composition comprises urapidil and arginine. The urapidil is a new crystal compound, the X-ray powder diffraction diagram, obtained by using Cu-K alpha rays for measuring, of the urapidil is shown in figure 1, and the crystal structure of the urapidil is different from that of urapidil in the prior art. According to experiments, compared with the prior art, the new crystal compound has the advantages that the compound is good in stability and extremely low in impurity I content, total impurity content is controlled in a relative low range, and the total impurity content change along with storage time is relatively small, and the solubility and flowability of the new crystal compound in water are improved evidently. Powder injection prepared by the new crystal compound is good in stability, good in stability after being combined with solvent, extremely low in insoluble particle content and quite 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 severe 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 to take care of life...

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 medicines (see Comparative Examples 1 and 2), so , 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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