Tamsulosin Solid Composition Using Low-Solubility Disintegrant
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Solution Overview
Problem
Current pharmaceutical compositions of tamsulosin require expensive excipients and complex processes, and there is a need for a stable dosage form with a suitable drug release profile that is simpler and quicker to produce, as well as smaller total weight formulations.
Innovation Solution
A solid pharmaceutical composition comprising tamsulosin or its pharmaceutically acceptable salt/solvate, a matrix former, and a disintegrant with low water solubility, dispersed in a matrix former, which allows for a stable and efficient drug release profile without the need for expensive hydrogel-forming polymers, using a simple and fast process.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hydrogel-forming polymers and expensive excipients are used to achieve sustained-release, then drug release profile is improved, but manufacturing cost increases
Solution Approach 1:
The patent replaces expensive hydrogel-forming polymers with a combination of conventional matrix formers and disintegrants that are cheaper and more readily available. The matrix former provides structural support while the disintegrant ensures drug release, achieving sustained-release效果 without requiring costly specialized polymers.
Solution Approach 2:
The patent changes the formulation parameters by using specific ratios of matrix former to disintegrant, and controlling the water solubility of the disintegrant to be less than 0.2 g/ml. This parameter optimization achieves effective drug release profiles using conventional, cost-effective materials rather than expensive hydrogel polymers.
2Reliability
If complex formulations with multiple components are used to achieve sustained-release, then drug release profile is improved, but process complexity increases
Solution Approach 1:
The patent extracts the essential functions of sustained-release into two separate components: the matrix former provides structural integrity and controlled water penetration, while the disintegrant provides the mechanism for drug release. This separation of functions simplifies the overall process compared to using complex multi-component hydrogel systems.
Solution Approach 2:
The matrix former serves multiple functions simultaneously: it provides structural support, controls water penetration rate, and maintains formulation stability. The disintegrant similarly provides multiple functions: it facilitates drug release, maintains granule integrity, and ensures complete disintegration. This multi-functionality reduces the need for additional specialized components.
3Reliability
If large amounts of hydrogel-forming polymer are used to ensure sufficient drug release in colon, then drug release is improved, but total dosage form weight increases
Solution Approach 1:
The patent optimizes the water solubility parameter of the disintegrant to be less than 0.2 g/ml, which allows it to remain relatively insoluble in the colon environment and maintain granule structure. This parameter control enables effective drug release without requiring large amounts of polymer material, thus keeping the dosage form weight low.
Solution Approach 2:
The disintegrant is specifically designed to have low water solubility (<0.2 g/ml) to maintain its function in the colon where water availability is limited. This localized property optimization ensures effective drug release in the target location without requiring excessive polymer content throughout the entire dosage form.
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 a stable and efficient drug release profile with reduced use of hydrogel-forming polymers and simpler processing, resulting in a cost-effective and efficient pharmaceutical formulation.
Implementation Method 1
at least a part of said drug (a) and at least a part of said disintegrant (c) are dispersed in said matrix former (b)
Data Source
AI summary
The present invention relates to a stable pharmaceutical composition comprising tamsulosin or a pharmaceutically acceptable salt or solvate thereof in a solid dosage form and to a process for preparing such a composition.