Amlodipine benazepril pharmaceutical composition

Abstract

The invention relates to an amlodipine and benazepril composition which is a tablet. The amlodipine benazepril tablet is obtained by treating amlodipine besylate and benazepril hydrochloride as active components, aerosil as a lubricant, lactose and microcrystalline cellulose as fillers and sodium carboxymethyl starch as a disintegrant and adopting a direct powder tabletting technology. The method has the advantages of simple process, and energy and time saving; and the prepared tablet has the advantages of stable quality, high dissolvability, and good disintegration.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a pharmaceutical composition of amlodipine and benazepril, and the pharmaceutical composition is a tablet. Background technique [0002] Hypertension is a major risk factor for death from cardiovascular disease, and its prevalence accounts for 10% to 30% of adults. The effective rate of treating hypertension with a single drug is only 40%, although increasing the dosage can improve the efficacy , but it also increases the incidence of adverse reactions. In order to improve the efficacy, reduce the incidence of cardiovascular events, and reduce target organ damage, angiotensin-converting enzyme inhibitors and calcium antagonists are usually used in combination to treat hypertension, which is safe and effective , is well tolerated. [0003] Amlodipine besylate (amlodipine besylate) is the second generation of long-acting dihydropyridine calcium antagonists, which can relax coro...

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Problems solved by technology

[0006] 1. The dissolution rate of amlodipine besylate in the prepared amlodipine benazepril tablets is low, which is not suitable for rapid onset of action of the drug and has a certain impact on clinical application

Thereby, need to adopt improved method to prepare amlodipine benazepril tablet, for example, can improve its stripping by micronization, in actual preparation, after hydrophobic material pulverizes, along with the reduction of particle size, surface free can increase, the particles are prone to re-agglomeration, so the actual benefit of crushing is not high; on the other hand, due to the small size of the hydrophobic material and the increase of the specific surface area, the hydrophobicity of the tablet will also be enhanced. On the contrary, it is not conducive to the dissolution of the tablet;

[0007] 2. The general preparation process uses magnesium stearate as a lubricant. Magnesium stearate is a hydrophobic substance. After excessive dosage or excessive stirring, it will cover the surface of the particles and affect the infiltration of water, resulting in amlodipine and benazepril tablets. Delayed disintegration (or dissolution) is not conducive to rapid therapeutic effect of the drug;

[0008] 3. The preparation of amlodipine and benazepril tablets by traditional wet granulation and tableting process: the process is complicated, and factors such as the amount of binder added, the drying time of granules, and the time of alcohol granulation and sieving have to be considered, and the number of machines required for production is large , The space is large, and because some factors need to rely on experience to judge, it may cause unstable product quality and large differences between batches, etc.

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