pH-Dependent Release Polymers for Cannabinoid Microparticles
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Solution Overview
Problem
Cannabinoids, such as cannabidiol, have poor aqueous solubility and bioavailability, leading to challenges in high-dose administration, particularly in pediatric patients, where alcohol-based formulations can cause gastrointestinal side effects and rapid metabolism results in reduced efficacy.
Innovation Solution
Development of microparticulate formulations containing pH-dependent release polymers like HPMCAS or Eudragit, which enable targeted delivery to the colon or intestines, avoiding stomach digestion and degradation, thereby enhancing bioavailability and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If alcohol-based formulations are used to solubilize cannabinoids, then solubility is improved, but gastrointestinal side effects and rapid metabolism occur
Solution Approach 1:
The patent introduces pH-dependent release polymers as intermediary materials that mediate between the lipophilic cannabinoid and the aqueous gastrointestinal environment. These polymers form microparticulate carriers that protect the cannabinoid from rapid metabolism while enabling controlled release, thus resolving the contradiction between solubility enhancement and avoidance of harmful effects
Solution Approach 2:
The invention changes the physical and chemical parameters of the formulation by using pH-dependent release polymers that respond to changes in gastrointestinal pH. The polymers remain intact in acidic stomach conditions but dissolve at higher pH in the intestines, transforming the release profile from immediate (harmful) to controlled (beneficial)
2Reliability
If oil-based excipients are used to deliver cannabinoids, then bioavailability is improved, but severe gastrointestinal side effects occur
Solution Approach 1:
The patent creates composite microparticulate formulations combining lipophilic cannabinoids with pH-dependent release polymers. This composite structure maintains the bioavailability benefits of lipid-based delivery while eliminating the harmful gastrointestinal effects through controlled release mechanisms that prevent rapid degradation
3Reliability
If high doses of cannabinoids are administered to overcome poor bioavailability, then therapeutic efficacy is improved, but formulation challenges in pediatric patients increase
Solution Approach 1:
The invention changes the formulation parameters by using pH-dependent release polymers that enable lower doses of cannabinoids to achieve therapeutic efficacy. The controlled release mechanism improves bioavailability, allowing pediatric patients to receive effective doses without the complexity and side effects associated with high-dose alcohol or oil-based formulations
4Ease of operation
If cannabinoids are delivered as oral solution, then administration is simplified, but rapid metabolism reduces efficacy
Solution Approach 1:
The patent introduces microparticulate carriers as intermediary structures that maintain the simplicity of oral administration while protecting the cannabinoid from rapid metabolism. The pH-dependent release polymers serve as mediators that control the release rate, ensuring therapeutic efficacy is maintained despite the convenience of oral dosing
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 microparticulate formulations improve bioavailability and stability of cannabinoids, allowing for lower doses and reduced gastrointestinal side effects, while ensuring effective delivery to the intended site, enhancing treatment efficacy.
Implementation Method 1
a pH dependent release polymer (also referred to herein as a 'enteric polymer')
Data Source
AI summary
The present disclosure provides a microparticulate comprising one or more cannabinoids and a pH dependent release polymer. In embodiments, the one or more cannabinoids are present in an amount ranging from 10% w/w to about 50% w/w. In embodiments, the pH dependent release polymer is present in an amount ranging from ranging from about 5% w/w to about 85% w/w.