Carvedilol sustained-release capsule

Abstract

The invention relates to the field of pharmaceutical preparations, in particular to a carvedilol sustained-release capsule. The carvedilol sustained-release capsule is characterized by consisting of a drug-containing pill core and a sustained-release layer, wherein the drug-containing pill core contains a blank pill core and carvedilol; the sustained-release layer contains a film-forming material and a pore-forming agent; the drug-containing pill core also contains a solubilizer; a weight ratio of the solubilizer to the active ingredients is (1:8)-(3:8); the sustained-release layer accounts for 12.6-16.1 percent of the total weight of the micro pill; the pore-forming agent consists of a methacrylic acid-ethyl acrylate (1:1) copolymer and a methacrylic acid-ethyl acrylate (1:2) copolymer; the pore-forming agent accounts for 6-11 percent of the total weight of the sustained-release layer. According to the carvedilol sustained-release preparation, only a micro pill is needed to be prepared, and a sustained-release effect can be achieved. Moreover, the medicine is slowly and fully released in main absorption parts at the pH of 5.5-6.8, the drug action time is prolonged, and the phenomenon that the safety risk of a patient is increased due to the local drug overdose caused by drug short-rate pulse release is avoided.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to carvedilol sustained-release capsules. Background technique [0002] Carvedilol was developed by the Boehringer Mannhei company in Germany. It was first approved by the FDA for marketing in the United States on September 14, 1995. Its chemical name is (±) 1-carbazole-4-oxyl-3-[2 -(2-methoxyphenoxy)ethylamino]-2-propanol. Carvedilol has nonselective beta-blocker, alpha-blocker and antioxidant properties. Dilates blood vessels by selectively blocking alpha1 adrenergic receptors. Carvedilol reduces peripheral resistance through vasodilation and inhibits the renin-angiotensin-aldosterone system through β-blockade. Vasorenin activity is reduced and fluid retention rarely occurs. Carvedilol has no intrinsic sympathomimetic activity and, like propranolol, is membrane stable. [0003] WO2005051322 discloses a sustained-release preparation of carvedilol and its salts. The p...

AI Technical Summary

Problems solved by technology

[0005] The carvedilol sustained-release capsule preparations prepared by the above patents are all prepared by mixing and filling three different speed pellets, and the dosage is greatly affected by the mixing uniformity of the three pellets and the content of each pellet. The ratio of the three and the changes in their respective contents all affect the quality and release degree of the final product, thereby affecting the efficacy of the drug

Moreover, the sustained-release pellets in the disclosed sustained-release preparations are all coated with pH-dependent film-forming materials, which will quickly dissolve in the corresponding pH portion of the gastrointestinal tract in the body and release a large amount of drugs. Although this sustained-release preparation can delay drug release, but it cannot be released smoothly, and the blood drug concentration of the patient will form a sharp step peak after taking the drug, which is not in line with the characteristics of sustained-release preparations that can stabilize the blood drug concentration

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