Clobazam Transdermal Patch Microemulsion Permeation
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Solution Overview
Problem
Clobazam poses challenges for transdermal delivery due to its poor permeation and water solubility, limiting its formulation as a transdermal drug delivery system, and existing solutions face issues like leaking pouch systems and inability to adjust doses.
Innovation Solution
A transdermal drug delivery system comprising a drug-containing layer with an oil-in-water microemulsion containing clobazam, a permeation enhancer, and a surfactant, combined with an adhesive component and an impermeable backing layer, forming a pressure-sensitive transdermal patch for improved bioavailability and dose flexibility.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of operation
If clobazam is formulated as a transdermal delivery system, then patient compliance and dosing flexibility are improved, but the formulation stability and permeation are worsened due to poor water solubility and permeation properties
Solution Approach 1:
The patent changes the physical-chemical parameters of clobazam by formulating it in an oil-in-water microemulsion system, transforming it from a poorly soluble compound into a stable transdermal delivery formulation. This parameter change enables both improved patient compliance through convenient patch application and maintained formulation stability through optimized emulsion composition.
Solution Approach 2:
The patent creates a composite material system combining clobazam with specific excipients in a microemulsion formulation. This composite approach allows the drug to achieve both good permeation properties and formulation stability simultaneously, while providing the convenience of transdermal delivery for improved patient compliance.
2Loss of time
If conventional transdermal systems are used, then dosing frequency is reduced, but dose flexibility and adaptability are worsened due to fixed dose formulations
Solution Approach 1:
The patent implements a dynamic dosing system where the transdermal patch can be adjusted based on patient needs. The formulation allows for flexible dose modification while maintaining the convenience of reduced dosing frequency through continuous transdermal delivery, resolving the contradiction between time loss and adaptability.
3Ease of operation
If oral formulation is used, then ease of administration is improved, but gastrointestinal side effects and dosing frequency are worsened
Solution Approach 1:
The patent uses the skin as an intermediary delivery route between the drug and the body's target sites. This intermediary approach eliminates direct gastrointestinal contact, reducing gastrointestinal side effects while maintaining ease of administration through simple patch application, thus resolving the contradiction between ease of operation and harmful factors.
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 system overcomes the barriers of clobazam's poor permeation and solubility, providing a stable and effective transdermal delivery with controlled release and improved patient compliance, reducing dosing frequency and gastrointestinal side effects.
Implementation Method 1
a drug-containing layer comprising (i) an oil-in-water microemulsion comprising: an oily phase comprising clobazam or a pharmaceutically acceptable salt thereof, an oily component and a solvent; and a hydrophilic phase comprising a surfactant
Implementation Method 2
The system overcomes the barriers of clobazam's poor permeation and solubility, providing a stable and effective transdermal delivery
Implementation Method 3
a hydrophilic phase comprising a surfactant, the microemulsion further comprising at least one of a permeation enhancer and/or a solubilizer
Data Source
AI summary
The present invention relates to transdermal drug delivery system of pharmaceutical compositions, which have a satisfactory in-vitro performance and good bioavailability. In particular, the transdermal pharmaceutical composition of clobazam in the present invention includes a micro-emulsion in liquid or semi solid form, in a dosage form adapted for transdermal delivery (e.g., transdermal patch) for treatment of certain types of epilepsy and anxiety for continues application.