CBD Compressed Tablets via Sucrose Fatty Acid Mono-Ester Granulate
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Solution Overview
Problem
Current pharmaceutical formulations of cannabidiol (CBD) for peroral administration suffer from low and unpredictable bioavailability due to its lipophilic nature and susceptibility to first-pass liver metabolization, as well as instability, making them unsuitable for effective treatment of psychosis and anxiety disorders.
Innovation Solution
Development of compressed tablets containing a CBD-containing granulate with lactose and sucrose fatty acid mono-ester, where the granulate is produced by combining CBD with lactose and sucrose fatty acid mono-ester in an organic solvent, followed by evaporation and mixing with additional lactose and excipients for compression, enhancing bioavailability and stability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If CBD is administered perorally in conventional formulations, then it can be taken orally, but bioavailability is low and unpredictable due to poor solubility and first-pass metabolism
Solution Approach 1:
The patent uses sucrose fatty acid mono-ester as an intermediary substance that forms a complex with CBD. This complex acts as a mediator that protects CBD from first-pass metabolism and enhances its solubility in the gastrointestinal environment, thereby improving bioavailability and reducing susceptibility to liver metabolization.
Solution Approach 2:
The invention creates a composite granulate consisting of CBD, sucrose fatty acid mono-ester, and lactose. This composite material combines the lipophilic CBD with hydrophilic excipients and solubility-enhancing agents, forming a formulation that overcomes the inherent solubility problems of pure CBD and improves its absorption profile.
2Ease of operation
If CBD is formulated for peroral administration, then oral treatment is possible, but stability is poor leading to degradation during storage
Solution Approach 1:
Sucrose fatty acid mono-ester serves as a protective intermediary that stabilizes CBD during storage. The complex formation between CBD and sucrose fatty acid mono-ester protects the cannabinoid from degradation, maintaining compositional stability while enabling peroral administration.
Solution Approach 2:
The composite granulate formulation with CBD, sucrose fatty acid mono-ester, and lactose creates a stable matrix that protects CBD from environmental factors during storage, preventing degradation while maintaining the desired oral dosage form.
3Ease of manufacture
If conventional CBD formulations are used, then they are simple to manufacture, but bioavailability remains low and unpredictable
Solution Approach 1:
The patent employs a composite granulate formulation that combines CBD with sucrose fatty acid mono-ester and lactose in specific proportions. This composite approach maintains manufacturing simplicity through conventional granulation and compression techniques while significantly improving bioavailability predictability through the solubility-enhancing and metabolism-protecting effects of the composite materials.
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 compressed tablets achieve high and predictable bioavailability of CBD, with minimal degradation during storage, allowing for effective treatment of psychosis and anxiety disorders with daily doses equivalent to 5-1000 mg of CBD.
Implementation Method 1
combining CBD with lactose and sucrose fatty acid mono-ester in an organic solvent
Implementation Method 2
followed by evaporation and mixing with additional lactose and excipients for compression
Data Source
AI summary
The present invention relates to compressed tablets for peroral delivery of the cannabinoid cannabidiol (CBD). More particularly, the invention provides a compressed tablet having a tablet weight of 60-1200 mg, said tablet being composed of:50-95 wt. % of a granulate;5-50 wt. % of lactose; and0-30 wt. % of other tablet excipients;wherein the granulate contains:a. 2-15 wt. % of cannabidiol;b. 2-30 wt. % of sucrose fatty acid mono-ester;c. 30-96 wt. % of lactose; andd. 0-25 wt. % of other granulate excipients.The compressed tablets according to the invention can conveniently be used in the treatment of psychosis disorders or anxiety disorders.The invention further provides a method for the manufacture of the compressed tablets.