Modified-release tablet formulations containing phosphodiesterase inhibitors

A modified-release tablet formulation for PDE inhibitors, using hydrophilic matrix-forming agents and excipients, addresses the challenge of gastrointestinal adverse events by controlling release in the upper GI tract, enhancing tolerability and maintaining systemic exposure.

JP7727543B2Active Publication Date: 2025-08-21UNION THERAPEUTICS AS
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Patent Information

Application Number
JP2021541105
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Priority Date
2019-01-15
Filing Date
2020-01-14
Publication Date
2025-08-21
Estimated Expiration
2040-01-14

AI Technical Summary

Technical Problem

Existing modified-release formulations of phosphodiesterase (PDE) inhibitors, particularly PDE4 inhibitors, face challenges in achieving the desired release profile and are associated with significant gastrointestinal adverse events due to high local concentrations in the intestine, necessitating a formulation that maintains systemic exposure while reducing these adverse effects.

Method used

A modified-release tablet formulation comprising PDE inhibitors, hydrophilic matrix-forming agents, fillers, glidants, lubricants, and optional coatings, designed to release the active ingredient slowly in the upper gastrointestinal tract, minimizing local concentrations and reducing gastrointestinal adverse events.

Benefits of technology

The formulation achieves improved tolerability and sustained systemic exposure by controlling the release of PDE inhibitors in the upper GI tract, significantly reducing gastrointestinal adverse events compared to immediate-release tablets.

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Patent Text Reader

Abstract

The present invention relates to modified-release tablet formulations for the oral administration of phosphodiesterase inhibitors, which are useful in the treatment, prevention, or amelioration of skin diseases or conditions.
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Citation Information

Patent Citations

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    JP2013529602A

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    US20050186276A1

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    WO2015197534A2