Self-Emulsifying Solid Dispersion With Silicate Carrier for Oral Absorption
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Solution Overview
Problem
Poorly soluble drugs and nutraceuticals, such as tocotrienols, face challenges with low bioavailability, solubility, and absorption, limiting their therapeutic efficacy.
Innovation Solution
A self-emulsifying solid dispersion (SESD) composition comprising a drug or nutraceutical, a surfactant, a carrier (silicic acid or silicate), and a carbohydrate filler, which enhances solubility and absorption by forming a self-emulsifying solid dispersion.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If poorly soluble drugs or nutraceuticals are administered orally, then they can be delivered to the target site, but their solubility and bioavailability are low, limiting therapeutic efficacy
Solution Approach 1:
The patent employs a composite material system consisting of silicic acid/silicate carrier, surfactant, and carbohydrate filler to create a self-emulsifying solid dispersion. This composite structure combines the hydrophobic drug with hydrophilic excipients to achieve both solubility enhancement and maintained therapeutic activity, directly resolving the contradiction between poor solubility and therapeutic efficacy
Solution Approach 2:
The invention changes the physical and chemical parameters of the drug delivery system by transforming the solid drug into a self-emulsifying solid dispersion with specific surface area, porosity, and emulsification properties. This parameter transformation enables the drug to transition from poor solubility state to enhanced bioavailability state while maintaining therapeutic efficacy
2Quantity of substance
If the drug is formulated to improve solubility, then bioavailability increases, but the formulation complexity increases
Solution Approach 1:
The formulation utilizes self-emulsifying properties where the combination of silicic acid/silicate, surfactant, and carbohydrate filler automatically forms emulsions upon contact with aqueous fluids in the body. This self-service mechanism eliminates the need for complex external emulsification equipment or complex multi-step formulation processes, achieving enhanced bioavailability with relatively simple formulation
Solution Approach 2:
The silicic acid/silicate acts as an intermediary carrier that facilitates the interaction between the hydrophobic drug and hydrophilic environment. This intermediary enables solubility enhancement through a straightforward solid dispersion approach rather than requiring complex formulation systems, thus improving bioavailability while controlling formulation complexity
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 SESD composition significantly increases solubility, bioaccessibility, and absorption of poorly soluble drugs and nutraceuticals, improving their therapeutic efficacy.
Implementation Method 1
at least one surfactant
Implementation Method 2
self-emulsifying solid dispersion (SESD) composition
Data Source
AI summary
The present invention pertains to a pharmaceutical, or nutraceutical, “self-emulsifying solid dispersion” composition for oral administration which contains (a) a drug or a nutraceutical that is water-insoluble or poorly water-soluble; (b) at least one surfactant; (c) one carrier selected from the group consisting of silicic acid, a silicate, or any combination thereof; and (d) at least one carbohydrate filler.