Pharmaceutical urapidil composition dry suspension for treating severe hypertension

Abstract

The invention relates to pharmaceutical urapidil composition dry suspension for treating severe hypertension and belongs to the technical field of medicine. The suspension is made from urapidil, instant sorbitol, lauryl sodium sulfate, tamarind gum, and aspartame. The urapidil is a novel-crystal form compound, an X-ray powder diffraction pattern obtained by measurement using Cu-KAlpha ray is shown in 1, the urapidil is different from that reported in the prior art, testing shows that the novel-crystal form compound is better than the prior art in stability and has very low impurity I content, total impurity content is also under control in a range of low content, and the content has slight changes over storage time. The urapidil crystal compound provided by the invention has significant improvement in water solubility and fluidity when compared to the prior art. The dry suspension made from the novel-crystal form compound is good in stability, high in bioavailability and very suitable for clinical application.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a dry suspension of 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 ...

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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