PMSB and 5-ASA Rectal Composition for IBD Stability
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Solution Overview
Problem
Existing treatments for inflammatory bowel diseases (IBD) like ulcerative colitis and Crohn's disease have limited efficacy due to the instability and physical properties of active ingredients, particularly prednisolone metasulfobenzoate (PMSB), which degrades easily, limiting their therapeutic utility.
Innovation Solution
A pharmaceutical composition combining PMSB with 5-aminosalicylic acid (5-ASA) or their pharmaceutically acceptable salts in a solid formulation, preferably for rectal administration as an enema, without buffers, and including a viscosity enhancer like guar gum, to enhance stability and synergistic therapeutic action.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If prednisolone metasulfobenzoate (PMSB) is used as an active ingredient for treating IBD, then anti-inflammatory therapeutic action is achieved, but the compound degrades easily during storage and administration, limiting its therapeutic utility
Solution Approach 1:
The patent combines PMSB with 5-aminosalicylic acid (5-ASA) or its derivatives into a single pharmaceutical composition. This merging of two active ingredients creates a synergistic effect where 5-ASA acts as a stabilizing agent that protects PMSB from degradation while both compounds work together to treat IBD, thereby resolving the contradiction between therapeutic utility and stability
Solution Approach 2:
The invention creates a composite pharmaceutical formulation containing both PMSB and 5-ASA in specific ratios. This composite material approach allows the two compounds to interact in a way that enhances overall stability while maintaining therapeutic efficacy, as 5-ASA provides a protective environment for the more labile PMSB molecule
2Reliability
If existing drug therapies are used to reduce intestinal inflammation, then some therapeutic effect is achieved, but the treatments cannot cure IBD and require lifelong medication
Solution Approach 1:
The patent designs a formulation that maintains continuous therapeutic action through the synergistic interaction of PMSB and 5-ASA. The composition ensures sustained release and action of both active ingredients, providing continuous anti-inflammatory effect that addresses the need for long-term management while potentially reducing treatment duration through enhanced efficacy
3Reliability
If 5-ASA is administered to act locally on diseased area, then anti-inflammatory action is achieved by inhibiting leukocyte chemotaxis and scavenging free radicals, but the effectiveness depends on achieving sufficient mucosal concentration
Solution Approach 1:
The patent merges PMSB with 5-ASA in a single composition, where PMSB acts as a delivery vehicle and stabilizer that facilitates the transport and retention of 5-ASA at the mucosal surface. This combination ensures sufficient local concentration of 5-ASA is achieved and maintained for effective anti-inflammatory action
Data Source
AI summary
A stable and/or synergistic pharmaceutical composition comprising: a) prednisolone metasulfobenzoate (PMSB) or its acceptable salts, preferably prednisolone metasulfobenzoate sodium and b) 5 -ASA, derivatives or pharmaceutically acceptable salts thereof, which is suitable for rectal administration.