5-ASA Free Acid Formulation for Ulcerative Colitis
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Patients with ulcerative colitis who are intolerant or unresponsive to 5-aminosalicylic acid (5-ASA) and corticosteroid preparations require alternative treatments due to insufficient effects and significant side effects associated with current therapies.
Innovation Solution
A pharmaceutical composition containing a compound represented by the formula (1) or its pharmaceutically acceptable salt, administered orally in varying doses and frequencies, targeting patients with active ulcerative colitis who have not responded to or are intolerant to 5-ASA and corticosteroid therapies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If corticosteroid preparation is used to treat ulcerative colitis, then strong efficacy is achieved, but side effects such as infectious diseases, hyperglycemia, adrenal gland disorder, and osteoporosis increase
Solution Approach 1:
The patent extracts and isolates the active ingredient 5-aminosalicylic acid from its conventional salt forms (mesalazine, sulfasalazine, olsalazine) to create a free acid formulation. This extraction approach aims to achieve the therapeutic efficacy of 5-ASA while avoiding the side effects associated with conventional salt preparations, particularly allergic reactions and gastrointestinal disturbances
Solution Approach 2:
The patent changes the chemical parameter of the 5-ASA compound by administering it in its free acid form rather than as conventional salts. This parameter change (from salt to free acid) is intended to modify the pharmacological profile to reduce side effects while maintaining efficacy. The patent also employs enteric coating technology to change the release parameter, ensuring the drug is released only in the distal colon where it exerts its therapeutic effect
2Reliability
If 5-ASA preparation is used to treat ulcerative colitis, then treatment is provided, but allergic reactions with fever and diarrhea occur
Solution Approach 1:
The patent extracts and isolates the active ingredient 5-aminosalicylic acid from its conventional salt forms (mesalazine, sulfasalazine, olsalazine) to create a free acid formulation. This extraction approach aims to achieve the therapeutic efficacy of 5-ASA while avoiding the side effects associated with conventional salt preparations, particularly allergic reactions and gastrointestinal disturbances
Solution Approach 2:
The patent employs an enteric coating as an intermediary layer that protects the 5-ASA free acid from premature release and degradation in the upper gastrointestinal tract. This coating acts as a mediator that ensures the drug reaches the distal colon intact, where it is released to exert its therapeutic effect while minimizing direct contact with sensitive tissues that could trigger allergic reactions
3Adaptability or versatility
If apheresis is used to treat refractory ulcerative colitis, then treatment option is provided, but physically heavy burden and long restraint on patient occur
Solution Approach 1:
The patent develops an oral pharmaceutical composition that enables patients to self-administer treatment at home without requiring hospitalization or complex medical procedures. The oral formulation allows patients to take the medication themselves, eliminating the need for apheresis procedures that require medical staff intervention and hospital facilities, thereby reducing both patient burden and medical resource requirements
4Adaptability or versatility
If tacrolimus oral administration is used to treat refractory ulcerative colitis, then treatment option is provided, but serious side effects such as renal dysfunction and pancreatic dysfunction occur requiring complicated trough level control
Solution Approach 1:
The patent extracts and isolates the active ingredient 5-aminosalicylic acid from its conventional salt forms to create a free acid formulation with a different safety profile. Unlike tacrolimus which causes serious organ toxicity, the 5-ASA free acid formulation targets local inflammation in the colon without systemic immunosuppression, thereby avoiding renal and pancreatic dysfunction while eliminating the need for complicated trough level monitoring
Data Source
AI summary
Provided is a pharmaceutical composition for treating ulcerative colitis, comprising a compound represented by a formula (1) or a pharmaceutically acceptable salt thereof, wherein the compound or the pharmaceutically acceptable salt is administered in an amount of 600 mg or more per day to an ulcerative colitis patient.