Pharmaceutical composition with functions of hemangiectasis and beta 1 receptor retardation

Abstract

The invention discloses a pharmaceutical composition with the functions of hemangiectasis and beta 1 receptor retardation, which comprises an active constituent-nebivolol hydrochloride or pharmaceutic salt and pharmaceutic adjuvant thereof. The invention is characterized in that the pharmaceutical composition prepared by the active ingredient-nebivolol hydrochloride or the pharmaceutic salt and the hydrophilic adjuvant thereof in a solid dispersion technology does not contain any solubilizer, and the weight ratio of the hydrophilic adjuvant to the active constituent is 5.0-1.0.

Description

technical field [0001] The invention relates to the technical field of medicine, and in particular relates to a method for preparing a pharmaceutical composition of nebivolol or its salt, which has a vasodilator effect and a β1 receptor block effect. Background technique [0002] Cardiovascular diseases include heart disease, hypertension, hyperlipidemia, etc., which have the characteristics of "high morbidity, high mortality, high disability, high recurrence rate" and "many complications", which threaten human life and health. number one killer. According to the World Heart Federation (2004), for every 3 people who die in the world, 1 of them dies from cardiovascular disease. Low- and middle-income countries account for 80% of deaths from cardiovascular disease, and the rate of death from cardiovascular disease in these countries continues to rise as obesity and smoking increase However, the mortality rate of cardiovascular disease is still much higher than that of other ...

AI Technical Summary

Problems solved by technology

[0004] The first generation of β-receptor blockers is represented by propranolol, which can block β1 and β2 receptors, and has many adverse reactions, especially not suitable for the treatment of dilated cardiomyopathy and heart failure

The second-generation β-receptor blockers are represented by metoprolol and bisoprolol, which selectively act on β1 receptors and have only a slight blocking effect on β2 receptors, but their antihypertensive effect is not obvious, and adverse reactions more

The third-generation β-blockers are represented by labetalol and carvedilol. Although they have anti-oxidative effects, they can effectively scavenge oxygen free radicals and reduce cardiomyocyte apoptosis, but they are non-selective. Receptors and α receptors also have a certain blocking effect, which can cause contraction of bronchial smooth muscle and vascular smooth muscle

[0006] Oral preparations need to have a certain bioavailability, and an important factor affecting the bioavailability of pharmaceutical preparations is the dissolution rate of active ingredients. The 2005 edition of the Chinese Pharmacopoeia stipulates that the dissolution rate of active ingredients in preparations should reach more than 70% in 45 minutes. Bivolol and its medicinal salts are almost insoluble in water, which makes the dissolution rate of the oral solid preparation prepared by the active ingredient poor and cannot reach the Pharmacopoeia standard; Chinese patent CN1140991A discloses a composition containing micronized nebivolol The possibility of preparing nebivolol or its pharmaceutically acceptable salts into oral preparations, nebivolol or its pharmaceutically acceptable salts are micronized and combined with a certain amount of wetting agent to meet the requirements, although this method is feasible, but Special equipment is required in the micronization process, which is very expensive and will increase the cost of the product, and in the preparation process, due to the low particle size, the loss is large and dust is easy to be generated

[0007] The Chinese patent CN101019858A is also combined with a certain amount of wetting agent after controlling the particle size, which also has the disadvantages of large loss and dust production, and the addition of a very small amount of wetting agent will increase the difficulty of preparation, which is harsh for the operator. requirements, otherwise it is easy to cause inhomogeneity of the sample

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