Pharmaceutical Salt Composition for Moisture-Stable HDAC Inhibitors
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Solution Overview
Problem
Existing alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide compounds face issues with moisture absorption leading to instability, increased production costs, and difficulties in maintaining a solid state, which complicates mass production and requires special storage conditions.
Innovation Solution
A pharmaceutical composition comprising alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate or tartrate compounds in the form of tablets, granules, powders, capsules, or injections, prepared by forming a free base solution and adding phosphoric or tartaric acid, using specific solvents to enhance stability and reduce hygroscopicity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide compound is used as HDAC inhibitor, then medicinal efficacy is improved, but hygroscopicity increases causing physicochemical instability
Solution Approach 1:
The patent applies parameter changes by converting the hygroscopic alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide compound into its phosphate or tartrate salt forms. This chemical transformation changes the physical and chemical parameters of the compound, resulting in salts with reduced hygroscopicity and improved physicochemical stability while preserving the HDAC inhibitory activity. The salt formation process modifies the molecular structure to eliminate the moisture-absorbing property without affecting the therapeutic effect.
2Stability of the object's composition
If purification operations are increased to remove related substances from moisture absorption, then stability is improved, but production cost increases
Solution Approach 1:
The patent applies preliminary action by performing salt formation during the synthesis process itself, rather than requiring separate purification steps after the compound is formed. By converting to phosphate or tartrate salts at an early stage, the compound's stability is enhanced proactively, preventing the formation of moisture-related impurities. This eliminates or reduces the need for subsequent expensive purification operations to remove hydrolysis products or other moisture-induced related substances.
3Stability of the object's composition
If separate freezing storage device is used to maintain solid state, then stability is improved, but device complexity increases
Solution Approach 1:
The patent applies parameter changes by transforming the compound into phosphate or tartrate salt forms that possess inherently superior thermal and hygroscopic stability. This chemical modification changes the physical parameters of the substance, allowing it to maintain its solid state and stability under ambient storage conditions without requiring freezing temperatures. The salt forms have higher melting points and lower moisture affinity, eliminating the need for complex frozen storage infrastructure.
Data Source
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AI summary
The present invention relates to a pharmaceutical composition containing an alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate compound (hereinafter referred to as CG200745PPA) or a derivative thereof, and can provide a pharmaceutical composition in a tablet, granule, powder, capsule, dry syrup or injection form. By providing the composition in various forms, a suitable form can be selected and easily applied when oral administration is difficult.