Rapid-acting insulin compositions with triphosphate

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Solution Overview

Problem

Current commercial insulin compositions have slow uptake and onset of action, which fails to rapidly match carbohydrate absorption profiles, leading to hyperglycemia during the early postprandial period and potential late hypoglycemia or weight gain.

Innovation Solution

A pharmaceutical insulin composition containing insulin and triphosphate, without saccharide multimers or EDTA, with triphosphate concentrations between 10 to 30 mM, and optionally including zinc and a tonicity agent like glycerol, to enhance rapid insulin uptake and onset of action.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If conventional insulin compositions are used, then insulin is administered to patients, but the uptake and onset of action are slow, resulting in hyperglycemia during the early postprandial period

Engineering Contradiction:
Improveuptake speedVSAvoidonset time
Core Design Contradiction:
SpeedVSLoss of time

Solution Approach 1:

The patent changes the chemical composition parameters of the insulin formulation by incorporating triphosphate at concentrations of 10-30 mM, which fundamentally alters the pharmacokinetic parameters of insulin absorption and onset of action

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite insulin formulation by combining insulin with triphosphate and optionally zinc, where the composite material exhibits enhanced absorption characteristics compared to conventional insulin formulations

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If conventional rapid-acting insulin analogs are used, then insulin activity is provided, but the time-action profile does not sufficiently match carbohydrate absorption, leading to late postprandial hypoglycemia

Engineering Contradiction:
Improveduration of actionVSAvoidmatching efficiency
Core Design Contradiction:
Duration of action of moving objectVSProductivity

Solution Approach 1:

The patent modifies the duration and shape of the insulin action curve by incorporating triphosphate, which accelerates both the onset and the overall time-action profile to better synchronize with carbohydrate absorption kinetics

Inventive Principle:
Principle #35Parameter changes

3Speed

If triphosphate is added to insulin composition, then uptake speed increases, but composition complexity increases

Engineering Contradiction:
Improveuptake speedVSAvoidcomposition complexity
Core Design Contradiction:
SpeedVSDevice complexity

Solution Approach 1:

The patent manages composition complexity by defining specific concentration ranges for triphosphate (10-30 mM) and optional zinc (0.2-5 mM), transforming a potentially complex formulation problem into a controlled parameter optimization

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentEP3630166B1Rapid-acting insulin compositions
Publication Date: 2022.04.06 ELI LILLY & CO
  • EP3630166B1 patent drawing
  • EP3630166B1 patent drawing
  • EP3630166B1 patent drawing

AI summary

The invention is a composition of insulin or insulin analog that has faster pharmacokinetic action than commercial formulations of rapid-onset insulin analog products.