Hydroxyalkyl Methylcellulose Sustained Release Composition
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Solution Overview
Problem
Conventional oral dosage forms, such as capsules or tablets, can be difficult for patients, especially children or the elderly, or those with dysphagia, to swallow, particularly when highly dosed drugs require large dosage forms or divided doses.
Innovation Solution
A sustained release composition using hydroxyalkyl methylcellulose with a specific substitution pattern, allowing for the formation of a stable hydrogel at body temperature, even at lower concentrations than traditional HPMC, to regulate the release of active ingredients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional HPMC is used at typical concentrations (30-60% by weight) to provide sustained release, then the sustained release property is improved, but the dosage form size increases making it difficult to swallow
Solution Approach 1:
The patent changes the chemical parameters of the cellulose ether by introducing specific substitution patterns (s23/s26 ratio ≤ 0.30) and hydroxyalkyl molar substitution (MS(hydroxyalkyl)) values. These parameter changes enable the polymer to form stable hydrogels at much lower concentrations (5-50% by weight) while maintaining sustained release properties, thereby reducing dosage form size and improving swallowability
Solution Approach 2:
The patent uses composite cellulose ether materials with specific combinations of methyl substitution (s23 and s26 values) and hydroxyalkyl substitution (MS(hydroxyalkyl)). This composite structure creates a polymer that forms more efficient hydrogel networks at lower concentrations, resolving the contradiction between sustained release effectiveness and dosage form size
2Volume of moving object
If the concentration of hydroxyalkyl methylcellulose is reduced to decrease dosage form size, then the swallowability is improved, but the sustained release property may be compromised
Solution Approach 1:
The patent identifies specific parameter ranges for hydroxyalkyl methylcellulose that enable low-concentration sustained release: s23/s26 ratio ≤ 0.30, MS(hydroxyalkyl) within specific ranges, and concentration of 5-50% by weight. These parameter changes ensure that even at reduced concentrations, the polymer maintains its ability to form stable hydrogels and control drug release
Solution Approach 2:
The patent employs a more efficient polymer structure that acts as a shorter-lived, more effective excipient. The specific substitution pattern creates a polymer that forms hydrogels more rapidly and maintains structure more effectively at lower concentrations, compensating for the reduced amount through enhanced per-unit effectiveness
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
The composition achieves sustained release of active ingredients over an extended period, reducing the size of the dosage form and improving swallowability without compromising release properties, and can be formulated with a reduced amount of excipients.
Implementation Method 1
HPMC is used in commercial oral pharmaceutical formulations as a component of a polymeric matrix providing sustained release of a drug
Implementation Method 2
HPMC is used in commercial oral pharmaceutical formulations as a component of a polymeric matrix providing sustained release of a drug
Implementation Method 3
when a hydroxyalkyl methylcellulose with a specific substitution pattern is used as an excipient in admixture with a physiologically active ingredient, it is capable of forming a stable hydrogel in an aqueous environment at body temperature
Data Source
AI summary
A sustained release composition for oral administration comprises particles of a physiologically active ingredient mixed with a hydroxyalkyl methylcellulose, wherein the ether substituents are methyl groups, hydroxyalkyl groups, and optionally alkyl groups being different from methyl,the hydroxyalkyl methylcellulose has an MS(hydroxyalkyl) of 0.05 to 1.00, and hydroxy groups of anhydroglucose units are substituted with methyl groups such that [s23/s26−0.2*MS(hydroxyalkyl)] is 0.30 or less, andwherein the concentration of hydroxyalkyl methylcellulose is 0.1-10% by dry weight of the active ingredient.