Low-Substituted Hydroxypropyl Cellulose Dissolvability

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Solution Overview

Problem

Pharmaceutical compositions containing a compound with platelet aggregation inhibition activity have poor dissolvability, which is not effectively improved by existing additives like low-substituted hydroxypropyl cellulose, as described in prior patent documents.

Innovation Solution

Incorporating low-substituted hydroxypropyl cellulose in a specific range (2.5 to 40.0% by weight) with the compound represented by general formula (I) or its pharmacologically acceptable salt, particularly using a direct compression method to formulate the composition into powders, granules, capsules, or tablets, enhances dissolvability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional additives are used in pharmaceutical compositions containing the compound of formula (I), then the composition can be formulated, but the dissolvability remains poor

Engineering Contradiction:
ImprovedissolvabilityVSAvoidformulation effectiveness
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent applies parameter changes by specifying a particular concentration range of low-substituted hydroxypropyl cellulose (2.5-40.0% by weight) in the pharmaceutical composition. This quantitative parameter optimization transforms the formulation from ineffective to highly effective in improving dissolvability, directly resolving the technical contradiction between poor dissolvability and formulation effectiveness

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite pharmaceutical composition by combining the compound of formula (I) with low-substituted hydroxypropyl cellulose as a specific excipient. This composite material approach leverages the synergistic interaction between the active compound and the cellulose derivative to achieve improved dissolvability that neither component could achieve alone

Inventive Principle:
Principle #40Composite materials

2Reliability

If low-substituted hydroxypropyl cellulose is used as an additive, then dissolvability can be improved, but the formulation requires specific concentration control

Engineering Contradiction:
ImprovedissolvabilityVSAvoidconcentration control
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent defines a specific concentration range (2.5-40.0% by weight) for low-substituted hydroxypropyl cellulose to optimize dissolvability while providing clear manufacturing guidelines. This parameter specification balances the need for improved dissolvability with practical manufacturing considerations, establishing an optimal window that achieves therapeutic effect without requiring excessive precision

Inventive Principle:
Principle #35Parameter changes

Data Source

PatentUS9034860B2Pharmaceutical composition containing low-substituted hydroxypropyl cellulose
Publication Date: 2015.05.19 DAIICHI SANKYO CO LTD
  • US9034860B2 patent drawing
  • US9034860B2 patent drawing
  • US9034860B2 patent drawing

AI summary

Disclosed is a pharmaceutical composition containing a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, while having improved dissolvability. Specifically disclosed is a pharmaceutical composition containing (A) a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, and (B) a low-substituted hydroxypropyl cellulose.