Tadalafil-Dutasteride Composition With Predictive Dissolution Control

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Solution Overview

Problem

Existing pharmaceutical compositions comprising tadalafil and dutasteride lack a clear correlation between in vitro dissolution patterns and in vivo absorption behavior, leading to inconsistent absorption patterns and the need for repeated clinical trials, which increases development time and cost.

Innovation Solution

A pharmaceutical composition with specific dissolution conditions and particle size distributions for tadalafil and dutasteride granules, achieving a firm in vitro-in vivo correlation (IVIVC), where tadalafil achieves 60-75% dissolution in 5 minutes and 80% in 30 minutes at pH 1.2 with 0.25% SLS, and dutasteride achieves 50% in 15 minutes and 85% in 30 minutes with 0.1% SLS, using controlled particle sizes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Adaptability or versatility

If existing pharmaceutical compositions comprising tadalafil and dutasteride are used, then simultaneous treatment of erectile dysfunction and prostatic hyperplasia is achieved, but there is no clear correlation between in vitro dissolution patterns and in vivo absorption behavior

Engineering Contradiction:

Improvesimultaneous treatment capabilityVSAvoiddissolution-absorption correlation

Core Design Contradiction:

Adaptability or versatilityVSMeasurement precision

Solution Approach 1:

The patent applies parameter changes by optimizing specific dissolution test conditions (pH levels, surfactant concentrations, agitation speeds) to establish a correlation framework. By systematically varying these parameters and identifying optimal values, the invention transforms the dissolution test into a predictive tool for in vivo absorption, resolving the contradiction between maintaining treatment versatility and achieving measurement precision.

Inventive Principle:

Principle #35Parameter changes

2Adaptability or versatility

If pharmaceutical compositions without established IVIVC are developed, then formulation flexibility is maintained, but repeated clinical trials are required increasing development time and cost

Engineering Contradiction:

Improveformulation flexibilityVSAvoiddevelopment time

Core Design Contradiction:

Adaptability or versatilityVSLoss of time

Solution Approach 1:

The patent implements preliminary action by establishing the dissolution-absorption correlation framework before clinical trials. The IVIVC model is developed and validated in advance using in vitro dissolution data, allowing formulation optimizations to be predicted and screened beforehand. This preliminary characterization reduces the need for repeated clinical trials by providing a reliable predictive tool that guides formulation development.

Inventive Principle:

Principle #10Preliminary action

3Ease of manufacture

If particle size distribution is not controlled, then manufacturing simplicity is maintained, but dissolution rate and absorption predictability decrease

Engineering Contradiction:

Improvemanufacturing simplicityVSAvoiddissolution rate

Core Design Contradiction:

Ease of manufactureVSProductivity

Solution Approach 1:

The patent applies parameter changes by establishing specific particle size distribution ranges for tadalafil and dutasteride granules. By defining optimal D10, D50, and D90 values, the invention transforms particle size from an uncontrolled variable into a controlled parameter that ensures both manufacturability and predictable dissolution behavior. This systematic approach maintains manufacturing simplicity while achieving consistent dissolution rates.

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

This approach allows for accurate prediction of in vivo absorption patterns, reducing drug development time and cost by establishing a firm IVIVC, ensuring bioequivalence without repeated clinical trials.

Implementation Method 1

a dissolution rate of tadalafil under dissolution conditions of a 50 rpm paddle rate in 500 mL of an eluate comprising 0.25% SLS at pH 1.2 is 60 to 75% in 5 minutes and more than 80% in 30 minutes

Methodology Applied

Scientific EffectDissolution:

Data Source

PatentUS12582651B2Pharmaceutical composition comprising tadalafil or pharmaceutically acceptable salt thereof and dutasteride or pharmaceutically acceptable salt thereof exhibiting novel dissolution rate

Publication Date: 2026.03.24 DONG KOOK PHARMA CO LTD

AI summary

Provided is a pharmaceutical composition comprising as active ingredients: 5 mg of tadalafil or a pharmaceutically acceptable salt thereof; and 0.5 mg of dutasteride or a pharmaceutically acceptable salt thereof, wherein the dissolution rate of tadalafil under the dissolution conditions of a paddle rate of 50 rpm in 500 mL of a dissolution solution having a pH of 1.2 and containing 0.25% of SLS is 60-75% after 5 minutes and 80% or more after 30 minutes, and the dissolution rate of dutasteride under the dissolution conditions of a paddle rate of 50 rpm in 500 mL of a dissolution solution containing water and 0.1% of SLS is 50% or more after 15 minutes and 85% or more after 30 minutes.