Calcium Compound Coating for Poorly Soluble Substance Particles

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Solution Overview

Problem

Poorly soluble substances in pharmaceutical, veterinary, cosmetic, and agricultural products face challenges in solubility, leading to reduced bioavailability and effectiveness due to existing methods' limitations, such as high additive requirements, instability, and safety concerns with organic solvents.

Innovation Solution

Coating poorly soluble substance particles with calcium compound microparticles, specifically calcium phosphate or calcium carbonate, to enhance solubility through improved wetting and dispersibility, without the need for large amounts of additives.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If mechanical microparticulation is used to increase solubility, then dissolution rate is improved, but particle size reduction requires excessive energy input and equipment complexity

Engineering Contradiction:
ImprovesolubilityVSAvoidenergy input
Core Design Contradiction:
ReliabilityVSUse of energy by moving object

Solution Approach 1:

The invention changes the chemical composition parameter of the coating material from conventional options to calcium compounds (calcium phosphate, calcium carbonate). This parameter change achieves the solubility enhancement goal without requiring excessive mechanical energy input for particle size reduction, as the calcium compound coating provides a chemical mechanism for improved dissolution rather than relying solely on physical size reduction

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates a composite structure consisting of the poorly-soluble substance core coated with calcium compound microparticles. This composite material approach combines the properties of both components: the active pharmaceutical ingredient and the calcium compound coating, achieving enhanced solubility and dissolution rate without the need for extreme mechanical microparticulation

Inventive Principle:
Principle #40Composite materials

2Reliability

If cyclodextrin inclusion is used to improve solubility, then dissolution rate increases, but the amount of additive required becomes excessively large

Engineering Contradiction:
ImprovesolubilityVSAvoidadditive amount
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention changes the type of coating material from cyclodextrin to calcium compounds (calcium phosphate, calcium carbonate). This parameter change achieves solubility enhancement while using much smaller amounts of additive, as the calcium compound coating forms a thin layer on the particle surface rather than requiring large quantities of inclusion complexing agents

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention applies the calcium compound coating locally on the surface of the poorly-soluble substance particles. This localized application provides the solubility enhancement function where needed (at the particle surface interface with aqueous medium) without requiring bulk modification of the entire substance, thereby minimizing additive quantity

Inventive Principle:
Principle #3Local quality

3Reliability

If organic solvents are used to increase solubility, then dissolution rate improves, but toxicity and safety hazards increase

Engineering Contradiction:
ImprovesolubilityVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention changes the chemical nature of the coating material from organic solvents to inorganic calcium compounds (calcium phosphate, calcium carbonate). This parameter change maintains solubility enhancement functionality while eliminating the toxicity and safety hazards associated with organic solvents, as calcium compounds are generally recognized as safe and biocompatible

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The calcium compound coating acts as a temporary, sacrificial layer that enhances solubility during the dissolution process. These inorganic coating materials are safe even if residual amounts remain in the final product, eliminating the need for strict solvent residue control required with toxic organic solvents

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

Significantly increases the solubility of poorly soluble substances in water, improving bioavailability and product effectiveness while being cost-effective and safer for workers and the environment.

Implementation Method 1

coating the surface of a poorly-soluble substance particle with microparticles of a calcium compound

Methodology Applied
Scientific EffectSurface coating: Coatings

Implementation Method 2

improve the solubility of the poorly-soluble substance by coating the surface of the poorly-soluble substance particle with the microparticles of a calcium compound

Methodology Applied
Scientific EffectWetting: Wetting

Data Source

PatentUS9023398B2Method for improving the aqueous solubility of poorly-soluble substances
Publication Date: 2015.05.05 SANGI CO LTD
  • US9023398B2 patent drawing
  • US9023398B2 patent drawing
  • US9023398B2 patent drawing

AI summary

Provided is a method for increasing the solubility of a poorly-soluble substance used in pharmaceutical products, veterinary pharmaceutical products, quasi-drugs, cosmetic products, food products, agricultural chemicals, and the like, without using large amounts of additives. This is a method for improving aqueous solubility, which comprises coating the surface of the particle of a poorly-soluble substance used in pharmaceutical products, veterinary pharmaceutical products, quasi-drugs, cosmetic products, food products, agricultural chemicals, and the like, with microparticles of a calcium compound such as calcium phosphate or calcium carbonate.