Polymer-Active Agent Conjugates for Rapid Onset and Sustained Action
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current pharmaceutical compositions of polymer-active agent conjugates often fail to provide a balance between rapid onset and sustained pharmacological activity, with many products offering only prolonged activity at the expense of initial effectiveness.
Innovation Solution
A composition comprising two populations of polymer-active agent conjugates with different weight average molecular weights, where the first population has polymers ranging from 100 Daltons to 120,000 Daltons and the second population from greater than 100 Daltons to 120,000 Daltons, allowing for a combination that provides both quick onset and sustained activity.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If polymer-active agent conjugates with high molecular weight polymers are used, then the duration of action is extended, but the onset of action becomes slower
Solution Approach 1:
The patent divides the conjugate population into two distinct segments: one with lower molecular weight polymers (100-20,000 Daltons) that provides rapid onset, and another with higher molecular weight polymers (20,000-120,000 Daltons) that provides extended duration. This segmentation allows each population to fulfill different pharmacokinetic requirements, resolving the contradiction between fast onset and sustained action.
Solution Approach 2:
The patent changes the molecular weight parameter of the polymer component to create two distinct populations with different pharmacokinetic profiles. By controlling the molecular weight distribution within specific ranges, the patent optimizes the balance between rapid onset (lower MW) and prolonged action (higher MW), directly addressing the technical contradiction.
2Duration of action of moving object
If polymer conjugation is applied to increase half-life, then the frequency of dosing is reduced, but the initial pharmacological activity is decreased
Solution Approach 1:
The patent segments the conjugate population to include lower molecular weight conjugates that retain higher initial activity and faster onset, combined with higher molecular weight conjugates that provide extended half-life. This segmentation ensures that the lower MW component compensates for the reduced initial activity of polymer-conjugated forms.
Solution Approach 2:
The patent creates a composite conjugate system combining two populations with different molecular weight characteristics. The composite formulation integrates the advantages of both low MW (high activity, fast onset) and high MW (long half-life, reduced dosing frequency) conjugates, achieving a balanced pharmacokinetic profile that satisfies both initial efficacy and sustained action requirements.
Data Source
AI summary
Compositions comprising two different populations of polymer-active agent conjugates, wherein the weight average molecular weight of the polymers associated with each population is different, are provided. Also provided are methods preparing such compositions and methods for administering such compositions.