Cyclobenzaprine Extended Release Beads Using Composite Coatings
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Solution Overview
Problem
Current cyclobenzaprine hydrochloride formulations require multiple daily administrations, which is a compliance challenge, especially for elderly patients, and existing extended release forms do not consistently maintain drug release for 8 to 12 hours, leading to potential dose dumping issues.
Innovation Solution
Development of extended release pharmaceutical compositions comprising a core coated with a matrix containing cyclobenzaprine hydrochloride and extended release agents, with optional plasticizers, structured to provide a controlled release profile of at least 8 to 12 hours, minimizing dose dumping by using a combination of inert cores, layers, and specific additives like ethylcellulose and Eudragit.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If immediate release tablets are administered three times a day to achieve relief from muscle spasm, then therapeutic effect is maintained, but patient compliance deteriorates
Solution Approach 1:
The patent divides the dosage form into multiple particles or beads, each containing the active ingredient cyclobenzaprine hydrochloride. This segmentation allows the drug to be released in a controlled manner over an extended period, providing sustained therapeutic effect while requiring only once-daily administration, thereby improving patient compliance.
2Ease of operation
If extended release capsules are designed for once a day administration, then patient compliance is improved, but drug release duration is insufficient (not consistently maintained for 8 to 12 hours)
Solution Approach 1:
The patent employs composite materials consisting of cyclobenzaprine hydrochloride combined with specific excipients and polymers that provide extended release properties. This composite formulation ensures consistent drug release over the required 8 to 12 hour period while maintaining once-daily dosing, thus achieving both improved compliance and adequate duration of action.
3Duration of action of moving object
If extended release coating is applied to core particles, then drug release is extended, but dose dumping may occur
Solution Approach 1:
The patent carefully controls the parameters of the extended release coating, including polymer type, coating thickness, and composition ratios. By optimizing these parameters, the formulation achieves sustained drug release over 8 to 12 hours while preventing dose dumping, ensuring reliable and predictable pharmacokinetic profiles.
Data Source
AI summary
The present invention provides extended release pharmaceutical compositions structured for once a day administration comprising skeletal muscle relaxant such as cyclobenzaprine or its pharmaceutically acceptable salt thereof that extends the release of the drug under in-vitro conditions for at least 8 to 12 hours. The invention also provides process for the preparation of such structured compositions.