Pregabalin sustained release composition and preparation method thereof

Abstract

The present invention provides a pregabalin sustained release composition, which comprises: (a) an active ingredient comprising pregabalin or a pharmaceutically acceptable salt or a hydrate thereof; (b) a matrix forming agent; (c) a swelling agent; (d) a filler; and (e) a gel, wherein the swelling agent is a combination comprising one or at least two selected from cross-linked sodium carboxymethylcellulose, cross-linked sodium carboxymethyl starch, low-substituted hydroxypropyl cellulose, calcium carboxymethyl cellulose and polyoxyethylene, and the filler comprises a combination comprising one or a plurality of materials selected from microcrystalline cellulose, lactose and pregelatinized starch. According to the invention, the pregabalin sustained-release composition can rapidly expand in volume when contacting an aqueous medium to excess the diameter (13 mm) of the stomach pylorus of human body, so that the residence time of pregabalin in the stomach can be increased by prolonging the gastric emptying time so as to improve the absorption of the pregabalin in the small intestine and the ascending colon; and the pregabalin sustained-release composition provided by the invention realizes 24-hour slow release, can realize QD (quaque die) administration, reduces the administration frequency and improves the compliance of patients.

Description

technical field [0001] The invention relates to the technical field of pregabalin preparations, in particular to a pregabalin sustained-release composition and a preparation method thereof. Background technique [0002] Pregabalin is indicated for the treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPN) and postherpetic neuralgia (PHN). The drug acts as a calcium ion channel modulator, inhibiting the α2-δ subunit of the voltage-dependent calcium channel in the central nervous system. It reduces the influx of calcium ions, and subsequently reduces the release of excitatory neurotransmitters such as glutamate, norepinephrine, and substance P, thereby effectively controlling neuropathic pain, and has anti-anxiety and anti-convulsant effects. [0003] Clinical studies have shown that the absorption of pregabalin in the gastrointestinal tract is uneven, and it is well absorbed in the human small intestine and ascending colon, but is rarely absorbed ...

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Problems solved by technology

[0003] Clinical studies have shown that the absorption of pregabalin in the gastrointestinal tract is heterogeneous, and it is well absorbed in the human small intestine and ascending colon, but is rarely absorbed in the intestinal segment outside the hepatic flexure of the colon

This means that the average absorption window of pregabalin is about 6 hours or less. Therefore, if pregabalin is made into a conventional sustained-release dosage form, the drug released will not be effectively absorbed after passing through the hepatic flexure of the colon after more than 6 hours. waste of drugs

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