Soft Gel Nintedanib Formulation With Lipid Carrier Solubilization

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Solution Overview

Problem

Nintedanib, a triple tyrosine kinase inhibitor, has poor solubility and bioavailability, limiting its clinical application due to low water solubility and requiring complex and costly manufacturing processes in existing formulations.

Innovation Solution

A soft gel capsule formulation comprising a suspension of nintedanib with a carrier system of medium chain triglycerides, phospholipids, and excipients like lecithin and solubilizing agents, enhancing solubility and bioavailability through a non-aqueous carrier system.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If nintedanib is formulated with conventional aqueous carriers, then manufacturing is simpler, but solubility and bioavailability remain poor

Engineering Contradiction:

ImprovebioavailabilityVSAvoidmanufacturing complexity

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent changes the fundamental parameter of the carrier system from aqueous to non-aqueous (lipid-based). This parameter change transforms the formulation approach, enabling nintedanib to achieve adequate solubility and bioavailability by matching the lipophilic nature of the drug with a lipid-based carrier system containing medium chain triglycerides, phospholipids, and surfactants.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The formulation employs a composite lipid-based carrier system combining multiple components: medium chain triglycerides (solvent), phospholipids (emulsifying agents), and surfactants. This composite material approach creates a synergistic system that effectively solubilizes nintedanib while maintaining stability and enhancing bioavailability.

Inventive Principle:

Principle #40Composite materials

2Reliability

If nintedanib is formulated with lipid-based carriers, then solubility and bioavailability improve, but manufacturing complexity and cost increase

Engineering Contradiction:

ImprovesolubilityVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent optimizes specific parameters within the lipid-based formulation, including the ratio of medium chain triglycerides to phospholipids, the selection of specific surfactants, and the concentration ranges of each component. These parameter optimizations simplify the formulation while maintaining enhanced solubility and bioavailability.

Inventive Principle:

Principle #35Parameter changes

3Reliability

If complex manufacturing processes are used for nintedanib formulation, then formulation performance improves, but manufacturing cost increases

Engineering Contradiction:

Improveformulation performanceVSAvoidmanufacturing cost

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent employs conventional, readily available pharmaceutical excipients and standard formulation techniques rather than requiring specialized or expensive materials. The lipid-based carrier system uses common ingredients like medium chain triglycerides and phospholipids that can be sourced from standard pharmaceutical suppliers, reducing material costs.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

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 formulation improves solubility and bioavailability of nintedanib, providing a cost-effective and stable dosage form with improved dissolution profiles compared to marketed formulations.

Implementation Method 1

Methodology Applied

Scientific EffectSolubilization: Solvation

Implementation Method 2

A soft gel capsule formulation comprising a suspension of nintedanib with a carrier system of medium chain triglycerides, phospholipids, and excipients like lecithin and solubilizing agents

Methodology Applied

Scientific EffectEmulsion: Emulsion

Data Source

PatentUS12558321B2Pharmaceutical formulation

Publication Date: 2026.02.24 CIPLA LTD

AI summary

Soft gelatin capsules comprising a suspension composition of nintedanib or a pharmaceutically acceptable salt thereof in medium chain triglycerides and carrier system, wherein the carrier system comprises solubilizers, phospholipids, thickeners and mixtures thereof.