Nilotinib sustained release tablet and preparation method thereof

By using a multi-layer sustained-release tablet design, combining a buoyancy-aiding layer and a drug-containing sustained-release layer, the problem of short retention time of nilotinib in the gastrointestinal tract is solved, improving the solubility and bioavailability of nilotinib, and enhancing patient compliance and safety.

CN121059547APending Publication Date: 2025-12-05NEOFORM BIOPHARMACEUTICAL LTD
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Patent Information

Application Number
CN202511198161.0
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-08-26
Publication Date
2025-12-05

AI Technical Summary

Technical Problem

Nilotinib's low solubility and low permeability result in a short residence time in the gastrointestinal tract. Existing extended-release tablets cannot effectively improve bioavailability and patient compliance, and food affects drug absorption, increasing the risk of cardiotoxicity.

Method used

The tablet employs a multi-layer sustained-release design, including a float-aid layer and a drug-containing sustained-release layer. It utilizes a high-viscosity hydrophilic polymer to control the drug's floating and slow release in the stomach, and improves solubility and bioavailability through an amorphous nilotinib solid dispersion, thereby reducing the frequency of dosing.

Benefits of technology

This allows for prolonged retention and slow release of nilotinib in the stomach, improving drug solubility and bioavailability, reducing dosing frequency and the risk of cardiotoxicity, and improving patient compliance.

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Abstract

The invention discloses a nilotinib sustained release tablet and a preparation method thereof, the nilotinib sustained release tablet comprises a bleaching assisting layer and a drug-containing sustained release layer, the bleaching assisting layer is prepared from a hydrophilic polymer with the viscosity of 2000 mpa.s-6000 mpa.s, a hydrophobic bleaching assisting agent, an adhesive and a lubricant; the drug-containing sustained-release layer is prepared from the following raw materials: an amorphous solid dispersion containing nilotinib or salt thereof, a hydrophilic polymer with the viscosity of 40 mpa.s-2000 mpa.s, a water-soluble filler, a flow aid and a lubricant. The nilotinib sustained-release tablet can effectively prolong the retention time of nilotinib in the stomach, slowly release the medicine in the stomach, improve the solubility and bioavailability of the medicine and reduce the overall dosage, so that the adverse reaction of the medicine is reduced, and meanwhile, on the basis of ensuring that the nilotinib sustained-release tablet is not affected by food effects, the nilotinib sustained-release tablet only needs to be orally taken once every day, and the curative effect of the nilotinib sustained-release tablet is greatly improved. The medicine taking compliance of a patient is improved by reducing the medicine taking times.
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