Protein-Based Excipient for Amorphous API Solubility

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Solution Overview

Problem

Existing APIs with low solubility and bioavailability face challenges in achieving effective delivery due to poor solubility and dissolution rates, leading to diminished bioavailability and potential chemical interactions with polymer excipients, which can cause structural degradation and genotoxic impurities.

Innovation Solution

A protein-based excipient, derived from proteins of at least 10 amino acids in length, is combined with APIs to form a substantially amorphous and homogenous mixture, enhancing solubility, dissolution, and bioavailability, while maintaining supersaturation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If polymer excipients are used to enhance solubility, then solubility is improved, but chemical interactions occur causing structural degradation and genotoxic impurities

Engineering Contradiction:

ImprovesolubilityVSAvoidchemical interactions and genotoxic impurities

Core Design Contradiction:

Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses hydrolyzed gelatin, a biodegradable and naturally occurring protein, as an excipient that enhances solubility without the harmful chemical interactions associated with synthetic polymers. The gelatin is hydrolyzed to reduce molecular weight and improve solubility, and is designed to be metabolized in the body, avoiding long-term accumulation and genotoxicity concerns

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent changes the physical and chemical parameters of gelatin through hydrolysis, reducing the molecular weight and altering the structure to enhance solubility. The hydrolyzed gelatin forms an amorphous solid dispersion with the API, preventing crystallization and maintaining high solubility without the need for synthetic polymer excipients that cause harmful interactions

Inventive Principle:

Principle #35Parameter changes

2Quantity of substance

If APIs are administered in higher dosages to overcome poor solubility, then bioavailability is improved, but the need for higher dosages increases treatment complexity and cost

Engineering Contradiction:

ImprovebioavailabilityVSAvoiddosage requirements

Core Design Contradiction:

Quantity of substanceVSDevice complexity

Solution Approach 1:

The patent changes the physical state of the API from crystalline to amorphous by forming an amorphous solid dispersion with hydrolyzed gelatin. This parameter change dramatically increases solubility and bioavailability, allowing effective dosing at lower amounts and eliminating the need for complex high-dose regimens

Inventive Principle:

Principle #35Parameter changes

3Stability of the object's composition

If crystalline API formulations are used, then stability is improved, but dissolution rates are slow leading to poor bioavailability

Engineering Contradiction:

Improveformulation stabilityVSAvoiddissolution rate

Core Design Contradiction:

Stability of the object's compositionVSSpeed

Solution Approach 1:

The patent utilizes phase transition by converting the API from a crystalline state to an amorphous state through formation of an amorphous solid dispersion with hydrolyzed gelatin. This phase transition eliminates the slow dissolution rates associated with crystalline structures while maintaining formulation stability through the amorphous matrix

Inventive Principle:

Principle #36Phase transitions

Solution Approach 2:

The patent creates a composite material system consisting of hydrolyzed gelatin and API in an amorphous solid dispersion. The gelatin matrix provides structural stability while the amorphous nature ensures rapid dissolution, combining both stability and fast dissolution rate in a single formulation

Inventive Principle:

Principle #40Composite materials

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 protein-based excipient improves the solubility, dissolution, and bioavailability of APIs, reducing the need for higher dosages and minimizing chemical interactions, thus enhancing the therapeutic efficacy and safety of pharmaceutical formulations.

Implementation Method 1

said formulation is substantially amorphous

Methodology Applied

Scientific EffectAmorphization:

Implementation Method 2

maintaining supersaturation

Methodology Applied

Scientific EffectSupersaturation: Supersaturation

Data Source

PatentUS12582717B2Protein based excipient for active pharmaceutical ingredients

Publication Date: 2026.03.24 DISPERSOME IP APS

AI summary

Provided herein is a pharmaceutical formulation comprising a protein based excipient in combination with an active pharmaceutical ingredient (API) wherein said formulation is substantially amorphous and form a substantially homogenous mixture; and further a method for producing said pharmaceutical formulation; and said pharmaceutical formulation for use as a medicament.