Solid Preparation Uniform Dispersion for Diabetes Therapy

Resolve Bottlenecks,
Find Innovative Solutions
Generate Solutions

Solution Overview

Problem

Existing solid preparations containing insulin sensitizers and active ingredients face challenges in achieving uniform content distribution, adequate hardness, and optimal dissolution properties, which are crucial for effective therapeutic delivery in diabetes management.

Innovation Solution

A solid preparation is developed where an insulin sensitizer and a biguanide, such as metformin hydrochloride, are uniformly dispersed with a median size ratio of 0.5 to 15, ensuring uniform content distribution and enhanced dissolution properties, achieved through fluidized bed granulation and compression-molding, with optional film-coating for improved hardness and stability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If insulin sensitizer and active ingredient are simply mixed in a solid preparation, then the preparation can be manufactured, but content uniformity and dissolution properties are insufficient

Engineering Contradiction:
Improvecontent uniformityVSAvoidpreparation complexity
Core Design Contradiction:
Manufacturing precisionVSEase of manufacture

Solution Approach 1:

The patent divides the solid preparation into distinct phases: a first phase containing insulin sensitizer particles and a second phase containing active ingredient particles. This segmentation allows each component to be uniformly distributed within its respective phase while maintaining overall content uniformity throughout the preparation.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent applies local quality by creating specific phase regions with different compositions. The first phase is localized to contain insulin sensitizer, while the second phase is localized to contain active ingredient. This local differentiation ensures uniform distribution of each component within its phase while achieving overall content uniformity.

Inventive Principle:
Principle #3Local quality

2Strength

If the solid preparation is made harder to improve stability, then storage stability improves, but dissolution properties may be compromised

Engineering Contradiction:
Improvepreparation hardnessVSAvoiddissolution properties
Core Design Contradiction:
StrengthVSManufacturing precision

Solution Approach 1:

By segmenting the preparation into distinct phases with different compositions, the patent achieves both hardness and dissolution properties. The first phase (insulin sensitizer) and second phase (active ingredient) can be optimized independently for their respective requirements while contributing to overall preparation hardness.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent creates a composite solid preparation with multiple phases having different properties. The composite structure allows the preparation to exhibit both hardness (from the overall matrix) and improved dissolution properties (from the specifically designed phases with appropriate particle sizes and distributions).

Inventive Principle:
Principle #40Composite materials

3Manufacturing precision

If additional additives are used to improve content uniformity and hardness, then preparation quality improves, but the formulation complexity and cost increase

Engineering Contradiction:
Improvecontent uniformityVSAvoidformulation complexity
Core Design Contradiction:
Manufacturing precisionVSDevice complexity

Solution Approach 1:

The patent achieves content uniformity through segmentation into phases rather than relying on multiple additives. The first phase contains insulin sensitizer and the second phase contains active ingredient, with each phase having controlled composition and distribution. This reduces formulation complexity compared to using multiple additives to achieve the same uniformity.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent optimizes parameters such as particle size ratios (0.5 to 15 times), phase compositions, and distribution characteristics to achieve content uniformity and hardness. By adjusting these parameters within specific ranges, the patent achieves desired preparation quality without requiring excessive additives.

Inventive Principle:
Principle #35Parameter changes

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 preparation exhibits superior content uniformity, hardness, and dissolution properties, ensuring effective therapeutic delivery and improved patient outcomes for diabetes management, with enhanced bioavailability and reduced need for additional additives.

Implementation Method 1

achieved through fluidized bed granulation and compression-molding

Methodology Applied
Scientific EffectFluidized bed granulation:

Implementation Method 2

achieved through fluidized bed granulation and compression-molding

Methodology Applied
Scientific EffectCompression-molding: Compression

Implementation Method 3

with optional film-coating for improved hardness and stability

Methodology Applied
Scientific EffectFilm-coating: Coatings

Data Source

PatentUS9101660B2Solid preparation
Publication Date: 2015.08.11 TAKEDA PHARMA CO LTD

AI summary

The present invention provides a solid preparation containing an insulin sensitizer and an active ingredient (except insulin sensitizers), which is useful as a therapeutic drug for diabetes and the like, and which is superior in preparation characteristics such as content uniformity and dissolution property of the insulin sensitizer and the active ingredient (except insulin sensitizers), preparation hardness and the like.