Controlled release preparation containing doxazosin or salt thereof and preparation method thereof

Abstract

The invention provides a controlled release preparation for doxazosin or salts thereof, wherein, the controlled release preparation comprises a drug containing layer and a boosting layer which have the weight ratio of 1 : 0.5 to 3. The drug containing layer comprises the doxazosin or salts thereof and a carrier, and the carrier is vinylpyrrolidone polymers which occupy 40 percent and 99 percent of the weight of the drug containing layer; the boosting layer at least comprises permeability promoting polymers occupying 10 percent to 80 percent of the weight of the boosting layer, 10 percent to 80 percent water insoluble polymers and 3 percent to 60 percent osmotic pressure accelerators; a controllable speed release drug of the doxazosin or the salts which can be accepted by the doxazosin in pharmacy causes the preparation to achieve the purpose that the doxazosin or the salts which can be accepted by the doxazosin in pharmacy can be released within about 24 h through once drug feeding daily.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a controlled-release preparation containing an active drug doxazosin or a pharmaceutically acceptable salt thereof and a preparation method thereof. Background technique [0002] Doxazosin (Doxazosin, chemical name: [1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxane-2- Acetylene carbonyl)] piperazine), is a long-acting α 1 Receptor antagonists can effectively control the symptoms of diseases such as hypertension and benign prostatic hyperplasia (BPH). However, when using ordinary tablets, if the therapeutic dose is used directly, blood pressure may drop suddenly due to a sudden increase in blood drug concentration, which may cause adverse reactions such as fainting and orthostatic hypotension. Therefore, it is necessary to start from a small dose and gradually adjust the dose. For this reason, Pfizer Pharmaceutical Co., Ltd. has developed doxazosin GITS (Ca...

AI Technical Summary

Problems solved by technology

However, the osmotic pump controlled-release tablet with PEO as the main auxiliary material has inherent disadvantages: (1) the water absorption rate and hydration rate of polyoxyethylene are relatively slow, so the time lag of drug release is long, so that the drug cannot be rapidly recovered after taking it. (2) The typical glass transition temperature range of polyoxyethylene is 65°C to 67°C, so PEO does not have ideal thermal stability, and there are the following problems in the preparation and storage process of industrial production: during the granulation process Solvent drying is more difficult

Since the drying temperature should not usually exceed 40°C, it is easy to cause a high residual amount of organic solvent; if the drying is to be relatively complete, a relatively long drying time is required; the storage temperature of the tablet should not be too high, and the high storage temperature is easy to cause The physical and chemical properties of polyoxyethylene change, which affects the release behavior of the tablet; during high-speed tablet compression, if the die is used repeatedly to generate heat and the temperature reaches about 50°C, adverse phenomena such as sticking and punching are prone to occur. Special cooling facilities are required to control the temperature of the die