Antiretroviral Solid Forms with Anti-Oxidative Acids
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Solution Overview
Problem
Current antiretroviral drugs, particularly those used in HIV treatment, face challenges with solubility, stability, and bioavailability, leading to suboptimal therapeutic effects and plasma concentration when administered orally.
Innovation Solution
Development of new solid forms of antiretroviral compounds combined with anti-oxidative acids, such as hydroxycinnamic acids, which enhance solubility, bioavailability, and stability, and are prepared through processes like mixing, crystallization, and co-crystallization to form salts, polymorphs, or co-crystals.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If antiretroviral drugs are prepared in conventional solid forms, then manufacturing is simple, but solubility and bioavailability are poor
Solution Approach 1:
The patent applies parameter changes by transforming the solid form of antiretroviral drugs from conventional crystalline structures to amorphous forms, and by creating acid addition salts with different chemical parameters. This changes the physical and chemical parameters of the drug substance, resulting in improved solubility and bioavailability while maintaining manageable manufacturing processes
Solution Approach 2:
The patent creates composite materials by forming acid addition salts of antiretroviral drugs with specific acids (such as fumaric acid, maleic acid, citric acid). These composite salt forms combine the properties of the parent drug with the acid component, achieving enhanced solubility and bioavailability characteristics
2Quantity of substance
If antiretroviral drugs are administered orally in conventional forms, then administration is simple, but therapeutic plasma concentration is insufficient
Solution Approach 1:
By changing the physical state from crystalline to amorphous and by forming acid addition salts, the patent improves the dissolution rate and bioavailability of orally administered antiretroviral drugs. This allows achieving therapeutic plasma concentrations with simpler oral administration routes without requiring complex delivery systems
3Stability of the object's composition
If conventional solid forms are used, then storage is straightforward, but stability is poor
Solution Approach 1:
The patent improves drug stability by transforming conventional solid forms into amorphous forms and by forming stable acid addition salts. These parameter changes result in formulations with enhanced chemical and physical stability that maintain drug integrity during storage without requiring overly complex stabilization systems
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 combination of antiretroviral compounds with anti-oxidative acids results in improved solubility, increased bioavailability, and prolonged therapeutic plasma concentrations, leading to enhanced therapeutic efficacy and faster onset of action.
Implementation Method 1
Development of new solid forms of antiretroviral compounds combined with anti-oxidative acids, such as hydroxycinnamic acids, which enhance solubility, bioavailability, and stability, and are prepared through processes like mixing, crystallization, and co-crystallization to form salts, polymorphs, or co-crystals
Data Source
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AI summary
Disclosed are solid forms of antiretroviral compounds and anti-oxidative acids, and processes for their preparation. Pharmaceutical compositions using the solid forms are also disclosed.