Self-Emulsifying Drug Delivery System for Oral THC

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Solution Overview

Problem

Current delivery systems for Δ9-THC face challenges such as low bioavailability due to hepatic first-pass metabolism, rapid absorption, and gastrointestinal irritation, which limits the effectiveness of cannabinoids in treating conditions like brain damage and pain management.

Innovation Solution

A self-emulsifying drug delivery system (SEDDS) is developed, using an oily medium with surfactants to promote self-emulsification, allowing targeted chylomicron/lipoprotein delivery and avoiding hepatic first-pass metabolism, thereby enhancing bioavailability and stability of Δ9-THC.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If oral administration of Δ9-THC is used, then ease of administration is improved, but bioavailability is reduced due to hepatic first-pass metabolism

Engineering Contradiction:

Improveease of administrationVSAvoidbioavailability

Core Design Contradiction:

Ease of operationVSReliability

Solution Approach 1:

The patent introduces chylomicron/lipoprotein particles as intermediary carriers that transport Δ9-THC through the lymphatic system instead of the hepatic portal system. This intermediary delivery mechanism bypasses the liver's first-pass metabolism while maintaining oral administration convenience, thereby resolving the contradiction between ease of administration and bioavailability.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent segments the delivery pathway by utilizing different anatomical routes: oral administration for convenience, lymphatic transport for bypassing the liver, and targeted delivery to the brain. This segmentation allows the system to maintain the benefits of oral administration while avoiding the harmful first-pass metabolism through alternative transport channels.

Inventive Principle:

Principle #1Segmentation

2Ease of operation

If conventional oral delivery systems are used, then ease of administration is improved, but absorption rate is too rapid causing gastrointestinal irritation

Engineering Contradiction:

Improveease of administrationVSAvoidgastrointestinal irritation

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The patent applies dynamics by controlling the release rate of Δ9-THC through lipoprotein particle formation and lymphatic transport mechanisms. This dynamic control allows the system to maintain ease of oral administration while regulating absorption speed to prevent gastrointestinal irritation, achieving both convenience and comfort.

Inventive Principle:

Principle #15Dynamics

3Ease of operation

If Δ9-THC is administered orally in conventional formulations, then ease of administration is improved, but stability is reduced due to oxidation and degradation

Engineering Contradiction:

Improveease of administrationVSAvoidstability

Core Design Contradiction:

Ease of operationVSStability of the object's composition

Solution Approach 1:

The patent uses lipoprotein particles as protective intermediaries that encapsulate Δ9-THC, shielding it from oxidation and degradation in the gastrointestinal tract. This intermediary protection maintains the stability of the cannabinoid while preserving the ease of oral administration, resolving the contradiction between convenience and compositional stability.

Inventive Principle:

Principle #24Intermediary (Mediator)

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 SEDDS system significantly improves the bioavailability and stability of Δ9-THC, providing sustained release and reducing gastrointestinal irritation, enabling more effective therapeutic outcomes for conditions like brain damage and pain management.

Implementation Method 1

A self-emulsifying drug delivery system (SEDDS) is developed, using an oily medium with surfactants to promote self-emulsification

Methodology Applied

Scientific EffectSelf-emulsification: Emulsion

Implementation Method 2

using an oily medium with surfactants to promote self-emulsification

Methodology Applied

Scientific EffectSurfactant action: Surfactant

Implementation Method 3

targeted chylomicron/lipoprotein delivery and avoiding hepatic first-pass metabolism

Methodology Applied

Scientific EffectLipoprotein transport:

Data Source

PatentUS9265724B2Oral dosage form of tetrahydrocannabinol and a method of avoiding and/or suppressing hepatic first pass metabolism via targeted chylomicron/lipoprotein delivery

Publication Date: 2016.02.23 MURTY RAM B

AI summary

Self-emulsifying drug delivery systems are provided to improve dissolution, stability, and bioavailability of drug compounds of dronabinol or other cannabinoids. The drug compound(s) are dissolved in an oily medium (e.g. triglycerides and/or mixed glycerides and/or free fatty acids containing medium and/or long chain saturated, mono-unsaturated, and/or poly-unsaturated free fatty acids) together with at least one surfactant. The surfactant promotes self-emulsification, thereby promoting targeted chylomicron/lipoprotein delivery and optimal bioavailability through the mammalian intestinal tract. A dosage form can optionally include co-solvents, anti-oxidants, viscosity modifying agents, cytochrome P450 metabolic inhibitors, P-GP efflux inhibitors, and amphiphilic/non-amphiphilic solutes to induce semi-solid formation for targeted release rates.