Cefdinir Amine Salts for Enhanced Water Solubility
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Solution Overview
Problem
Cefdinir's poor solubility in various organic solvents and water limits its bioavailability and formulation development as a pharmaceutical product, despite its potent antibiotic properties.
Innovation Solution
Development of pharmaceutically acceptable primary, secondary, and tertiary amine salts of cefdinir with hydroxy-containing organic amines, such as ethanolamine and 1-deoxy-1-methylamino-sorbitol, to enhance water solubility, which are incorporated into various pharmaceutical dosage forms like film tablets and extended release tablets.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If cefdinir is used in free base form or with non-hydroxy amine salts, then antibiotic efficacy is maintained, but water solubility remains poor
Solution Approach 1:
The patent changes the chemical structure parameter of the amine salt by incorporating hydroxy groups at specific positions (positions 1, 2, or 3 of the amine chain). This structural modification fundamentally alters the solubility parameter of cefdinir salts, transforming them from poorly water-soluble to highly water-soluble while preserving antibiotic activity.
Solution Approach 2:
The invention creates composite molecular structures by combining cefdinir with hydroxy-containing amine groups. The resulting composite amine salts integrate the antibiotic properties of cefdinir with the enhanced hydrophilicity of hydroxy amines, achieving both therapeutic efficacy and improved solubility in a single compound.
2Reliability
If conventional amine salts are used, then synthesis methods are well-established, but bioavailability is limited due to poor solubility
Solution Approach 1:
By modifying the amine salt structure to include hydroxy groups, the patent changes the physicochemical parameters of the compound. This structural parameter change directly improves bioavailability by enhancing water solubility, allowing the reliable antibiotic efficacy of cefdinir to be realized in vivo.
3Quantity of substance
If cefdinir solubility is improved through salt formation, then bioavailability increases, but the complexity of salt synthesis increases
Solution Approach 1:
The patent systematically varies parameters of the amine component (hydroxy group position and type) to optimize solubility. By establishing a structure-activity relationship, the invention provides a predictable framework for synthesis that reduces process complexity despite the specialized nature of the salts.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The cefdinir amine salts exhibit improved water solubility compared to the free base form and non-hydroxy amine salts, enabling effective treatment of bacterial infections while maintaining antibiotic efficacy in diverse dosage forms.
Implementation Method 1
pharmaceutically acceptable salts of cefdinir, specifically to primary, secondary and tertiary amine salts of cefdinir
Implementation Method 2
organic amine salts of cefdinir, wherein said organic amines comprise at least one hydroxy group
Data Source
AI summary
Present invention relates to pharmaceutically acceptable salts of cefdinir, specifically to primary, secondary and tertiary amine salts of cefdinir, preperation methods and pharmaceutical compositions comprising them.