Ospemifene Granulate Formulation for Enhanced Dissolution

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Solution Overview

Problem

Current solid drug formulations of ospemifene exhibit poor dissolution, which hinders effective drug absorption and bioavailability.

Innovation Solution

A solid drug formulation comprising granulates of ospemifene combined with intra-granular excipients such as disintegrants, diluents, and binders, produced through either dry or wet granulation methods, to enhance the drug's dissolution properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If ospemifene is formulated as a simple solid dosage form, then manufacturing is simple, but dissolution is poor

Engineering Contradiction:

Improvemanufacturing simplicityVSAvoiddissolution performance

Core Design Contradiction:

Ease of manufactureVSReliability

Solution Approach 1:

The formulation divides the solid dosage form into granulates with specific size ranges (0.2-2.0 mm), segmenting the drug substance into controlled particle sizes that enhance dissolution while maintaining manufacturing feasibility through standard granulation techniques

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

The invention creates a composite granulate system combining ospemifene with excipients including disintegrants (croscarmellose sodium, sodium starch glycolate), binders (pregelatinized starch, microcrystalline cellulose), and lubricants (magnesium stearate), forming a composite material that simultaneously achieves good dissolution and manufacturability

Inventive Principle:

Principle #40Composite materials

2Reliability

If granulation process is used to improve dissolution, then dissolution is enhanced, but manufacturing complexity increases

Engineering Contradiction:

Improvedissolution performanceVSAvoidmanufacturing process complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The invention optimizes specific parameters including granulate size (0.2-2.0 mm), excipient ratios (disintegrant 5-20%, binder 5-20%, lubricant 0.5-2%), and granulation method conditions to achieve enhanced dissolution while keeping the manufacturing process within standard pharmaceutical operation ranges

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The granulation process acts as an intermediary step that transforms the drug substance and excipients into a optimized granulate form, serving as a bridge between simple mixing and final tablet/capsule formulation, thereby improving dissolution without requiring complex manufacturing equipment

Inventive Principle:

Principle #24Intermediary (Mediator)

Data Source

PatentUS8642079B2Solid formulations of ospemifene

Publication Date: 2014.02.04 QUATRX PHARMACEUTICALS CO

AI summary

This invention relates to a solid drug formulation comprising granulates containing a therapeutically active compound of the formula (I)or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof, in combination with one or more intra-granular excipients.