Solid Preparation Dissolution via Polysorbate 80 Surfactant

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Solution Overview

Problem

Solid preparations containing an insulin sensitizer and an insulin secretagogue exhibit undesirable dissolution properties, specifically a slower dissolution rate of the insulin secretagogue compared to preparations with the secretagogue as a single active ingredient.

Innovation Solution

Incorporating a polyoxyethylene sorbitan fatty acid ester, such as Polysorbate 80, into the solid preparation to enhance the dissolution properties of the insulin secretagogue, thereby improving its bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If an insulin sensitizer and an insulin secretagogue are combined in a solid preparation, then the therapeutic effect is enhanced, but the dissolution rate of the insulin secretagogue decreases

Engineering Contradiction:
Improvetherapeutic effectVSAvoiddissolution rate
Core Design Contradiction:
ReliabilityVSSpeed

Solution Approach 1:

A water-soluble polymer is introduced as an intermediary substance between the insulin sensitizer and insulin secretagogue. This polymer acts as a dissolution promoter that specifically enhances the dissolution rate of the insulin secretagogue without affecting the insulin sensitizer, thereby resolving the contradiction between maintaining combined therapeutic effect and improving dissolution rate

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The dissolution properties are improved by changing the physical-chemical parameters of the formulation through the addition of water-soluble polymers. The polymer modifies the microenvironment around the insulin secretagogue particles, increasing their wettability and dissolution rate while maintaining the stability and efficacy of both active ingredients

Inventive Principle:
Principle #35Parameter changes

2Reliability

If an insulin sensitizer and an insulin secretagogue are combined in a solid preparation, then the therapeutic effect is enhanced, but the content uniformity decreases

Engineering Contradiction:
Improvetherapeutic effectVSAvoidcontent uniformity
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The water-soluble polymer serves as a binding intermediary that facilitates uniform distribution of both insulin sensitizer and insulin secretagogue throughout the formulation. This intermediary substance improves the mixing characteristics and prevents segregation, ensuring consistent content uniformity across dosage units

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation is designed as a composite material system where the water-soluble polymer creates a matrix that uniformly incorporates both active ingredients. This composite structure ensures that each dosage unit contains the intended proportion of insulin sensitizer and insulin secretagogue, improving content uniformity

Inventive Principle:
Principle #40Composite materials

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 incorporation of Polysorbate 80 in the solid preparation results in a dissolution rate of the insulin secretagogue equivalent to that of a single active ingredient, ensuring effective and stable medical efficacy with improved content uniformity and storage stability.

Implementation Method 1

a solid preparation comprising an insulin sensitizer, an insulin secretagogue and a polyoxyethylene sorbitan fatty acid ester

Methodology Applied
Scientific EffectSurfactant: Surfactant

Data Source

PatentUS7700128B2Solid preparation comprising an insulin sensitizer, an insulin secretagogue and a polyoxyethylene sorbitan fatty acid ester
Publication Date: 2010.04.20 TAKEDA PHARMA CO LTD

AI summary

A solid preparation useful as a diabetes-treating agent or the like and excellent in the dissolution properties of an insulin sensitizer and an insulin secretagogue, which comprises an insulin sensitizer, an insulin secretagogue and a polyoxyethylene sorbitan fatty acid ester is provided.