Paroxetine Controlled Release Formulation via pH-Sensitive Polymers
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Solution Overview
Problem
Conventional paroxetine formulations release the active ingredient in the stomach and small intestine, which can lead to undesirable side effects and reduced efficacy, as they do not effectively target the large intestine for controlled release.
Innovation Solution
A controlled release formulation of paroxetine or its pharmaceutically acceptable salt, designed to release at least 50-90% of the active ingredient in the large intestine, utilizing pH-sensitive polymers and enteric coatings to bypass the stomach and small intestine, ensuring release occurs between pH 5.5 to 8, typically within 7 to 10 hours post-ingestion.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional paroxetine formulations are used, then the active ingredient is released in the stomach and small intestine, but this causes undesirable side effects and reduced efficacy
Solution Approach 1:
The patent applies local quality by creating different release characteristics in different regions of the gastrointestinal tract. The formulation uses pH-sensitive polymers and enteric coatings that remain intact in the acidic stomach environment (pH 1-3) and neutral small intestine (pH 6-7.4), but dissolve specifically in the large intestine (pH 5.5-8), thereby concentrating the therapeutic action where needed while avoiding harmful effects in other regions.
Solution Approach 2:
The patent uses pH-sensitive polymers and enteric coatings as intermediary substances that mediate between the paroxetine active ingredient and the gastrointestinal environment. These polymers act as protective barriers that prevent premature release in the stomach and small intestine, and only allow release when the specific pH conditions of the large intestine are encountered.
2Reliability
If controlled release formulation is used to target large intestine, then side effects are reduced and efficacy is enhanced, but formulation complexity increases
Solution Approach 1:
The patent exploits parameter changes, specifically pH changes, to control drug release. The formulation contains pH-sensitive polymers that undergo solubility changes at different pH levels: remaining insoluble in the stomach (pH 1-3) and small intestine (pH 6-7.4), but becoming soluble in the large intestine (pH 5.5-8). This natural physiological parameter variation simplifies the control mechanism compared to active pumping systems.
Solution Approach 2:
The patent employs composite materials by combining paroxetine with pH-sensitive polymers and enteric coatings to create a multi-layered formulation system. This composite structure integrates the active ingredient with functional materials that provide the controlled release capability, achieving complex functionality through material composition rather than mechanical complexity.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
This formulation significantly reduces paroxetine release in the stomach and small intestine, achieving sustained release in the large intestine, thereby enhancing therapeutic efficacy and reducing side effects for conditions such as depression, anxiety, and obesity.
Implementation Method 1
utilizing pH-sensitive polymers and enteric coatings to bypass the stomach and small intestine, ensuring release occurs between pH 5.5 to 8
Implementation Method 2
ensuring release occurs between pH 5.5 to 8, typically within 7 to 10 hours post-ingestion
Data Source
AI summary
The present invention provides a delayed and/or controlled release formulation of paroxetine or a pharmaceutically acceptable salt thereof that is formulated to release a substantial portion of the active ingredient (e.g., paroxetine) in the large intestine of an individual in need thereof. In one embodiment, the present invention provides a controlled release paroxetine composition comprising paroxetine or a pharmaceutically acceptable salt thereof, in a controlled release swallow pharmaceutical formulation, that upon administration, releases the paroxetine substantially in the large intestine. For example, the controlled release paroxetine formulation may be formulated to release greater than about 50% of the paroxetine in the large intestine.