S-pindolol Oral Formulation with Starch and Cellulose
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Solution Overview
Problem
There is a need for a stable and effective solid oral formulation of S-pindolol or its salt with a favorable dissolution profile, as existing formulations face challenges in predicting interactions with excipients and maintaining stability during storage.
Innovation Solution
A solid pharmaceutical formulation comprising S-pindolol or a pharmaceutically acceptable salt, with significant proportions of starch and microcrystalline cellulose as excipients, specifically at least 15% starch and 30% or 40% cellulose by weight, which enhances stability and dissolution profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional excipients are used in tablet formulation of S-pindolol, then the formulation can be manufactured, but stability during storage cannot be guaranteed due to unpredictable interactions with active agent
Solution Approach 1:
The patent specifies precise weight ratio parameters for excipients (microcrystalline cellulose 20-40%, starch 10-30%, colloidal silica 0.5-2%, magnesium stearate 0.1-0.5%) to optimize both stability and dissolution. By controlling these compositional parameters within defined ranges, the formulation achieves predictable stability without requiring complex additional components.
Solution Approach 2:
The patent employs a composite excipient system combining microcrystalline cellulose, starch, colloidal silica, and magnesium stearate. This composite material approach leverages the complementary properties of each excipient: microcrystalline cellulose provides structural integrity, starch enhances dissolution, colloidal silica improves flow, and magnesium stearate acts as lubricant. The synergistic combination resolves the contradiction by achieving stability through material composition rather than formulation complexity.
2Reliability
If excipient proportions are optimized for stability, then storage stability improves, but dissolution profile may be compromised
Solution Approach 1:
The patent assigns different functional roles to different excipients within the formulation: microcrystalline cellulose (20-40%) provides structural stability for long-term storage, while starch (10-30%) specifically targets dissolution enhancement. This local functional differentiation allows the formulation to simultaneously achieve both stability and rapid dissolution without compromising either property.
Solution Approach 2:
The patent optimizes the weight ratio parameters of excipients to balance stability and dissolution. Specifically, the starch content (10-30%) is tuned to enhance dissolution rate, while microcrystalline cellulose (20-40%) maintains structural integrity for stability. By adjusting these parameters within defined ranges, the formulation achieves optimal performance in both stability and dissolution without requiring trade-offs.
3Reliability
If high proportions of excipients are used to ensure stability, then the formulation becomes more complex, but the active agent concentration is reduced
Solution Approach 1:
The patent defines specific weight ratio parameters for excipients that sum to 71-97% of the total formulation, leaving 3-29% for active agent. Within these constraints, the formulation achieves stability through optimized excipient composition rather than excessive quantities. The parameter optimization allows maximum active agent concentration while maintaining stability through efficient use of excipient functions.
Solution Approach 2:
The patent uses a multi-functional composite excipient system where each component serves specific purposes: microcrystalline cellulose for structural stability, starch for dissolution enhancement, colloidal silica for flow improvement, and magnesium stearate for lubrication. This efficient composite material approach maximizes the active agent concentration (3-29%) by ensuring each excipient contributes multiple functions, reducing the need for excessive excipient quantities.
Data Source
AI summary
The invention relates to a solid pharmaceutical formulation suitable for oral administration comprising: (a) an active agent which is S-pindolol or a pharmaceutically acceptable salt thereof; (b) a starch excipient in an amount of at least 15.0% by weight relative to the total weight of the formulation; and (c) a cellulose excipient in an amount of at least 30.0% by weight relative to the total weight of the formulation. Also provided is the solid pharmaceutical formulation for use in therapy, for instance in the treatment of cachexia.