Nitrosomorpholine Impurity Control in Esreboxetine Tablet Formulation
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for fibromyalgia are limited by variability in efficacy, tolerability issues, and the need for Drug Enforcement Administration (DEA) scheduling, failing to effectively address the widespread musculoskeletal pain and associated symptoms in patients.
Innovation Solution
A pharmaceutical composition comprising esreboxetine free base or its pharmaceutically acceptable salts, such as esreboxetine succinate, formulated into a tablet dosage form with specific excipients like hydroxypropyl methylcellulose, directly compressible starch, microcrystalline cellulose, and magnesium stearate, to provide a uniform blend that reduces pain in fibromyalgia.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current approved treatments for fibromyalgia are used, then some pain relief may be achieved, but variability in efficacy from patient to patient increases and tolerability issues arise
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of the morpholine compound to create specific enantiomeric forms with improved therapeutic profiles. The invention focuses on controlling stereochemistry parameters to achieve consistent efficacy while reducing adverse effects, thereby resolving the contradiction between reliability and tolerability.
2Reliability
If current approved treatments for fibromyalgia are used, then some therapeutic effect is achieved, but the need for Drug Enforcement Administration (DEA) scheduling limits treatment options
Solution Approach 1:
The patent changes the chemical parameters of existing treatments by developing new enantiomeric forms of morpholine compounds with improved safety profiles. This allows the therapeutic effect to be maintained while reducing the restrictions that would otherwise limit treatment availability and versatility.
3Stability of the object's composition
If a pharmaceutical composition is formulated with multiple excipients, then the uniform blend and stability improve, but the manufacturing complexity increases
Solution Approach 1:
The patent applies parameter changes by optimizing the ratios and selection of excipients in the pharmaceutical formulation. By carefully controlling the parameters of the formulation composition, the invention achieves stable uniform blends while maintaining ease of manufacture through standardized manufacturing processes.
Data Source
AI summary
(S)-2-((S)-(2-ethoxyphenoxy)(phenyl)methyl)-4-nitrosomorpholine is useful for analysis of a pharmaceutical composition. Also disclosed herein are methods of determining the quality of pharmaceutical compositions, and dosage forms comprising a reduced level of (S)-2-((S)-(2-ethoxyphenoxy)(phenyl)methyl)-4-nitrosomorpholine. Therapeutic uses of the pharmaceutical compositions and dosage forms are also described herein.