Coated Solid Dosage Form for Controlled Release of Lipophilic Substances
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Solution Overview
Problem
Developing effective solid oral dosage forms for highly lipophilic physiologically active substances like cannabinoids is challenging due to their low water solubility and high lipophilicity, which complicates controlled release and bioavailability.
Innovation Solution
A solid dosage form comprising a core coated with a combination of highly lipophilic physiologically active substances and water-soluble film formers, with limited additional excipients, allows for controlled release by adjusting the amount of film former relative to the active substance, facilitating the formation of a coating that promotes the release of sparingly water-soluble compounds.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Duration of action of moving object
If highly lipophilic physiologically active substances are formulated as solid oral dosage forms, then controlled release can be achieved, but water solubility is insufficient
Solution Approach 1:
The patent introduces water-soluble film formers as intermediary substances that form a coating matrix. This coating serves as a mediator between the lipophilic active substance and the aqueous gastrointestinal environment, enabling controlled release by adjusting the ratio and type of film formers used in the coating composition.
Solution Approach 2:
The patent employs parameter changes by adjusting the concentration, type, and molecular weight of water-soluble film formers in the coating. By varying these parameters, the release rate and duration of the lipophilic substance can be controlled while maintaining adequate water solubility through the hydrophilic properties of the film formers.
2Reliability
If highly lipophilic substances are used in solid dosage forms, then bioavailability can be improved, but release control becomes difficult
Solution Approach 1:
The patent applies local quality by creating a coating layer with specific properties (water-soluble film formers) that is different from the core containing the lipophilic substance. This localized modification enables controlled release at the interface between the coating and gastrointestinal fluids, simplifying the overall release control mechanism.
Solution Approach 2:
The patent uses composite materials by combining water-soluble film formers with lipophilic active substances in a coating formulation. This composite structure leverages the hydrophilic properties of the film formers to control the release of the lipophilic substance, achieving both bioavailability improvement and release control without complex mechanisms.
3Quantity of substance
If multiple excipients are added to improve solubility, then water solubility increases, but formulation simplicity is reduced
Solution Approach 1:
The patent applies universality by selecting water-soluble film formers that serve multiple functions: they form the coating matrix, provide water solubility, control release rate, and maintain structural integrity. This multi-functionality reduces the need for multiple separate excipients, simplifying the formulation while achieving adequate water solubility.
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
This approach enables controlled release of highly lipophilic substances, ensuring sufficient and timely release of the active ingredients during gastrointestinal passage, improving bioavailability and practical suitability of solid oral dosage forms.
Implementation Method 1
the coating comprises one or more highly lipophilic physiologically active substances, one or more water-soluble film formers
Data Source
AI summary
The invention relates to a product for the release of highly lipophilic physiologically active substances, comprising a core and a coating on top of the core, the coating comprising one or more highly lipophilic physiologically active substances, one or more water-soluble film-forming agents and, relative to the weight of all components, not more than 20 wt % of other auxiliary substances.