Cyclic Oligomer Inclusion Complexes for Poorly Soluble APIs

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Solution Overview

Problem

Many active pharmaceutical ingredients (APIs) have poor solubility in aqueous solutions and bioavailability, and existing formulation methods fail to adequately address these issues, making it challenging to develop effective pharmaceutical formulations.

Innovation Solution

A pharmaceutical formulation comprising an inclusion complex of an API with a cyclic oligomer, formed through thermokinetic processing, where at least a portion of the API is present within the cyclic oligomer, enhancing solubility and bioavailability.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If existing formulation methods are used for APIs, then the formulation process is simple, but the solubility and bioavailability of the API remain poor

Engineering Contradiction:

Improvesolubility and bioavailabilityVSAvoidformulation process complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent uses cyclodextrin, a cyclic oligomer with a hydrophilic outer surface and hydrophobic inner cavity, to form inclusion complexes with poorly soluble APIs. This composite structure allows the hydrophobic API to be incorporated within the hydrophilic cyclodextrin cavity, thereby improving solubility and bioavailability while maintaining a relatively simple formulation process.

Inventive Principle:

Principle #40Composite materials

Solution Approach 2:

The patent applies the nesting principle by placing the API molecule inside the central cavity of the cyclodextrin oligomer. The API is encapsulated within the hydrophobic interior of the cyclodextrin ring structure, forming an inclusion complex where the guest molecule (API) is nested within the host molecule (cyclodextrin), thereby enhancing solubility without complex processing.

Inventive Principle:

Principle #7Nested doll (Nesting)

2Reliability

If thermokinetic processing is used to form inclusion complexes, then solubility and bioavailability increase, but processing time must be precisely controlled

Engineering Contradiction:

Improvesolubility and bioavailabilityVSAvoidprocessing time control

Core Design Contradiction:

ReliabilityVSManufacturing precision

Solution Approach 1:

The patent utilizes thermokinetic processing that involves controlled heating to facilitate the formation of inclusion complexes. By changing the temperature parameter during processing, the patent achieves enhanced complex formation efficiency and solubility improvement while maintaining precise control over the processing time (less than 300 seconds), thereby balancing performance enhancement with manufacturing precision.

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

The inclusion complex significantly increases the solubility and bioavailability of the API, improving therapeutic properties and stability, allowing for more efficient drug delivery.

Implementation Method 1

an inclusion complex of an active pharmaceutical ingredient (API) with a cyclic oligomer

Methodology Applied

Scientific EffectInclusion complex formation: Absorption (physical)

Implementation Method 2

thermokinetic processing, where at least a portion of the API is present within the cyclic oligomer, enhancing solubility and bioavailability

Methodology Applied

Scientific EffectThermokinetic processing: Heating

Data Source

PatentUS20220401579A1Inclusion complexes of pharmaceuticals and cyclic oligomers

Publication Date: 2022.12.22 AUSTINPX LLC

AI summary

Pharmaceutical formulations including an inclusion complex of an API with a cyclic oligomer, and methods of forming such pharmaceutical formulations are described.