Polypeptide Hydrogel Sustained-Release Solvent System
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Solution Overview
Problem
Current sustained-release pharmaceutical compositions using self-assembling peptides like Ac-(Arg-Ala-Asp-Ala)4-NH2 do not utilize organic solvents such as polyethylene glycol, dimethyl sulfoxide, or glycofurol, which are effective in forming hydrogels for long-term drug delivery.
Innovation Solution
A pharmaceutical composition combining a drug with the polypeptide Ac-(Arg-Ala-Asp-Ala)4-NH2 and at least one organic solvent selected from polyethylene glycol, dimethyl sulfoxide, or glycofurol, with specific ratios and molecular weights, to form a depot for sustained release.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If only water is used as a solvent in sustained-release preparations with polypeptide Ac-(Arg-Ala-Asp-Ala)4-NH2, then the preparation can be formulated simply, but the sustained-release ability and drug dissolution efficiency are insufficient
Solution Approach 1:
The patent changes the solvent parameter from pure water to an organic solvent system (polyethylene glycol, dimethyl sulfoxide, or glycofurol), which fundamentally alters the dissolution and release characteristics of the drug-polypeptide complex, enabling sustained release over periods of 1 month or more
Solution Approach 2:
The patent creates a composite solvent system combining organic solvents with the polypeptide Ac-(Arg-Ala-Asp-Ala)4-NH2, forming a novel pharmaceutical composition where the organic solvent and polypeptide work synergistically to achieve prolonged drug release
2Reliability
If organic solvents are used to improve drug dissolution, then the dissolution efficiency increases, but the safety and biocompatibility may be compromised
Solution Approach 1:
The patent selects organic solvents (polyethylene glycol, dimethyl sulfoxide, glycofurol) that are pharmaceutically acceptable, have short residence times in the body, and are rapidly metabolized or excreted, minimizing toxic accumulation while maintaining high dissolution efficiency
Solution Approach 2:
The polypeptide Ac-(Arg-Ala-Asp-Ala)4-NH2 acts as an intermediary between the organic solvent and the drug, forming a complex that mediates the interaction, reducing direct exposure of the drug to potentially toxic solvents while maintaining dissolution efficiency
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 composition effectively dissolves and sustains the release of the drug after administration, providing a safe and favorable sustained-release ability, suitable for intravitreal or intracameral administration for treating eye diseases.
Implementation Method 1
hydrogel preparations utilizing self-assembling peptides have been reported
Implementation Method 2
a pharmaceutical composition in which a drug and a polypeptide represented by Ac- (Arg-Ala-Asp-Ala) 4 -NH 2 are mixed with at least one organic solvent selected from the group consisting of polyethylene glycol, dimethyl sulfoxide, glycofurol, and N-methylpyrrolidone sustained-releases the drug
Implementation Method 3
a pharmaceutical composition comprising a drug, a polypeptide represented by Ac-(Arg-Ala-Asp-Ala) 4 -NH 2 , and an organic solvent, in which the organic solvent is at least one organic solvent selected from the group consisting of polyethylene glycol, dimethyl sulfoxide, glycofurol, and N-methylpyrrolidone
Data Source
AI summary
Found out is a pharmaceutical composition that sustained-releases a drug for a long term after administration into the body. Provided is a pharmaceutical composition comprising a drug and a polypeptide represented by Ac-(Arg-Ala-Asp-Ala)4-NH2, and further containing an organic solvent selected from the group consisting of polyethylene glycol, dimethyl sulfoxide, glycofurol, and N-methylpyrrolidone.