Solid Preparation Segregating Tranexamic and Ascorbic Acid

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Solution Overview

Problem

Solid preparations containing tranexamic acid and ascorbic acid tend to undergo discoloration during long-term storage, which affects their stability and usability.

Innovation Solution

Separating tranexamic acid and ascorbic acid by a boundary within the preparation, and incorporating L-cysteine, pyridoxine, and pantothenic acid in specific configurations to prevent discoloration, either in separate granules or combined forms, ensures stability without mixing the active ingredients.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If tranexamic acid and ascorbic acid are mixed in the same granule, then the preparation shows superior pigmentation improvement effect, but the preparation undergoes discoloration (red discoloration) during long-term storage

Engineering Contradiction:
Improvepigmentation improvement effectVSAvoidcolor stability during storage
Core Design Contradiction:
ReliabilityVSStability of the object's composition

Solution Approach 1:

The invention divides the preparation into multiple granules, with tranexamic acid and ascorbic acid placed in separate granules. This segmentation prevents direct contact between the two active ingredients, thereby preventing discoloration while maintaining their individual therapeutic effects. The granules are formulated separately and can be administered together to achieve the synergistic pigmentation improvement effect.

Inventive Principle:
Principle #1Segmentation

2Reliability

If multiple active ingredients (tranexamic acid, ascorbic acid, L-cysteine, pyridoxine, pantothenic acid) are incorporated to enhance pigmentation suppression, then the therapeutic effect is improved, but the complexity of formulation and risk of interactions increases

Engineering Contradiction:
Improvepigmentation suppression effectVSAvoidformulation complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The invention segments multiple active ingredients into different granules based on their compatibility characteristics. Tranexamic acid and ascorbic acid are placed in separate granules to prevent discoloration. Additional ingredients like L-cysteine, pyridoxine, and pantothenic acid are incorporated into appropriate granules, creating a multi-component segmented system that manages complexity while maintaining enhanced therapeutic effects.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention uses granular structure as an intermediary barrier between incompatible active ingredients. By placing substances that may interact adversely into separate granular compartments, the formulation maintains the benefits of multiple active ingredients while preventing harmful interactions through the physical barrier of the granule structure.

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentEP2335698B8Pharmaceutical solid preparation having active ingredients separated by boundary therein
Publication Date: 2014.06.25 DAIICHI SANKYO HEALTHCARE

AI summary

[Object] An object of the present invention is to provide a solid preparation for oral administration containing tranexamic acid and ascorbic acid and satisfying the condition of stability without causing discoloration and the like. [Means for Resolution] The solid preparation for oral administration characterized by containing tranexamic acid and ascorbic acid as active ingredients, wherein these active ingredients exist in the preparation being separated by a boundary therebetween.