Epalrestat double-layered osmotic pump controlled release tablet and preparation method thereof

Abstract

The invention provides an epalrestat double-layered osmotic pump controlled release tablet and a preparation method thereof. An osmotic pump comprises a drug-containing layer, a boosting layer and a coating film; the drug-containing layer comprises the following components in percentages by weight: 30%-40% of epalrestat, 30%-50% of a swelling agent, 1%-10% of a pH regulator, 5%-15% of a solubilizer and 1%-3% of a lubricant; the boosting layer comprises the following components in percentages by weight: 60%-75% of a swelling agent, 5%-30% of an osmotically active substance and 1%-3% of a lubricant; and the semi-permeable coating film for 100 tablets comprises the following components: 5 g-15 g of a semi-permeable polymer material and 0.5 g-3 g of a water-soluble pore-forming agent. By the epalrestat double-layered osmotic pump controlled release tablet, drugs can be released in vivo at a constant speed, and the drug release behavior is not influenced by factors such as the pH value of amedium environment, enzyme, gastrointestinal peristalsis and food, so that the stability of blood concentration can be maintained, the toxic and side effects of the drugs can be relieved, the administration times can be reduced, and the compliance of patients can be improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an epalrestat double-layer osmotic pump controlled-release tablet and a preparation method thereof. Background technique [0002] Diabetic peripheral neuropathy (Diabetic Peripheral Neuropathy, DPN) is a common chronic complication of diabetes. Sensory neuropathy. DPN is not the main cause of death in diabetic patients, but it can increase the risk of disability in patients. In severe cases, diabetic foot and extremity gangrene will develop, leading to amputation and disability, which will adversely affect the quality of life of patients. [0003] The polyol pathway is a pathogenesis of diabetic peripheral neuropathy, and aldose reductases (ARIs) can reduce sorbitol flux through the polyol pathway to treat diabetic peripheral neuropathy. The chemical name of Epalrestat is 5-[(1Z,2E)-2-methyl-3-phenyl-2-propenylidene]-4-oxo-2-thio-thiazolidineacetic acid, ...

AI Technical Summary

Problems solved by technology

At present, there are only 3 domestic companies with approval documents: Yangzijiang Pharmaceutical, Shandong Dyne Marine Biopharmaceutical, and Beijing Younit Pharmaceutical, and all of them produce ordinary preparations with a specification of 50 mg. During treatment, they need to be administered 3 times a day for patients. It brings inconvenience, and at the same time, it causes large fluctuations in effective blood drug concentration, and large toxic and side effects

Then there was the report of epalrestat sustained-release preparation, CN104940156A enteric-coated sustained-release tablet, the drug release is slow and non-constant, the gastrointestinal environment of the human body has a greater impact on the absorption and release of the drug, and there is a certain blood drug concentration fluctuation

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