Antiretroviral Solid Dispersion Matrix Without Surfactants
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Solution Overview
Problem
The challenge is to create a pharmaceutical dosage form for antiretroviral active ingredients with high bioavailability and improved solubility without chemical degradation during thermal processing, while avoiding the use of undesired excipients like surfactants with HLB values from 12 to 18.
Innovation Solution
A pharmaceutical dosage form comprising antiretroviral active ingredients in the form of a solid dispersion or solid solution within a matrix that includes an amino(meth)acrylate copolymer, specifically without pharmaceutically acceptable surfactants with an HLB value from 12 to 18, and with the inclusion of a mono carboxylic acid or alcohol with 12 to 22 carbon atoms, formulated using a melt extrusion process.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If surfactants with HLB values from 12 to 18 are used to enhance solubility and bioavailability of antiretroviral active ingredients, then solubility and bioavailability are improved, but chemical degradation occurs during thermal processing
Solution Approach 1:
The patent removes surfactants with HLB values from 12 to 18 from the formulation entirely, extracting the harmful component while maintaining the therapeutic function through alternative means (amino(meth)acrylate copolymer matrix without surfactants).
Solution Approach 2:
The patent replaces complex surfactant systems with a simpler amino(meth)acrylate copolymer matrix that achieves solubility enhancement through its inherent properties rather than requiring additional surfactant excipients.
2Productivity
If melt extrusion process is used to produce solid dispersion, then manufacturing efficiency is improved, but chemical degradation occurs during thermal processing
Solution Approach 1:
The patent modifies the chemical composition parameters of the matrix system by using amino(meth)acrylate copolymers with specific functional groups that are more resistant to thermal degradation during melt extrusion, allowing the process to proceed at standard temperatures without excessive degradation.
3Device complexity
If undesired excipients like surfactants are avoided, then formulation complexity is reduced, but achieving high bioavailability becomes more difficult
Solution Approach 1:
The amino(meth)acrylate copolymer matrix performs multiple functions simultaneously: it provides structural support, enhances solubility of the antiretroviral active ingredients, and eliminates the need for separate surfactant components, thereby reducing formulation complexity while maintaining bioavailability.
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
This approach enhances the solubility and bioavailability of antiretroviral active ingredients, such as lopinavir and ritonavir, while maintaining stability and reducing chemical degradation, as demonstrated by improved in vitro and in vivo bioavailability testing and storage stability.
Implementation Method 1
antiretroviral active ingredients in the form of a solid dispersion or solid solution in a matrix
Implementation Method 2
antiretroviral active ingredients in the form of a solid dispersion or solid solution in a matrix
Implementation Method 3
formulated using a melt extrusion process
Data Source
AI summary
The invention relates to a pharmaceutical dosage form comprising one or more antiretroviral active ingredients in the form of a solid dispersion or solid solution in a matrix, wherein said matrix comprises an amino(meth)acrylate copolymer, characterized in that the matrix does not contain any essential amounts of pharmaceutically acceptable surfactants with an HLB value from 12 to 18 and in that the matrix comprises a mono carboxylic acid or an alcohol with 12 to 22 carbon atoms or both.