Thiocolchicoside Analgesic Formulation for Stable Plasma Release
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Solution Overview
Problem
Conventional pharmaceutical formulations of thiocolchicoside and analgesics often result in incompatible drug combinations due to chemico-physical and therapeutic incompatibilities, leading to increased side effects, undesirable interactions, and complex dosage schedules, which compromise safety and patient compliance.
Innovation Solution
A novel pharmaceutical formulation featuring an immediate release phase of thiocolchicoside, a first sustained release phase with glyceryl behenate as a release rate controlling agent, and a second sustained release phase of an analgesic, designed to provide a simplified dosage regimen and stable plasma concentrations for effective management of pain, spasticity, and inflammatory symptoms.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional pharmaceutical formulations combine thiocolchicoside and analgesics in the same dosage form, then therapeutic effects are enhanced, but chemico-physical incompatibility and undesirable drug interactions occur
Solution Approach 1:
The patent divides the pharmaceutical formulation into three distinct phases: an immediate release phase containing thiocolchicoside, a first sustained release phase containing thiocolchicoside and glyceryl behenate, and a second sustained release phase containing the analgesic. This segmentation physically separates the two active ingredients into different release compartments, preventing direct chemico-physical interactions while allowing both drugs to be administered together for synergistic therapeutic effect.
Solution Approach 2:
The patent introduces glyceryl behenate as a release rate controlling agent that acts as an intermediary substance. This excipient controls the sustained release of both thiocolchicoside and the analgesic, mediating their release kinetics to maintain stable plasma concentrations without direct drug-drug interaction. The intermediary mechanism allows compatible co-administration of otherwise incompatible drugs.
2Stability of the object's composition
If conventional formulations use multiple administration times for thiocolchicoside and analgesic, then plasma concentration stability is improved, but dosage schedule complexity increases
Solution Approach 1:
The patent merges multiple dosing regimens into a single combined pharmaceutical formulation. By incorporating both thiocolchicoside (immediate and sustained release) and the analgesic (sustained release) into one tablet or capsule, the invention eliminates the need for separate administrations while maintaining stable plasma concentrations of both drugs through coordinated release mechanisms.
Solution Approach 2:
The patent implements continuous therapeutic action through a combination of immediate release and sustained release phases. The immediate release phase provides rapid initial therapeutic effect, while the sustained release phases maintain continuous drug delivery over extended periods, ensuring continuous useful action without requiring multiple discrete dosing events.
3Object-affected harmful factors
If conventional formulations administer drugs at different times, then side effects are reduced, but patient compliance decreases
Solution Approach 1:
By segmenting the formulation into controlled release phases, the patent reduces peak plasma concentrations that cause side effects while maintaining therapeutic efficacy. The sustained release mechanism spreads drug delivery over time, avoiding sudden high concentrations that would trigger adverse reactions, thereby reducing side effects without requiring complex multiple dosing schedules.
Solution Approach 2:
The patent changes the release rate parameter of the drugs by incorporating glyceryl behenate as a release rate controlling agent. This parameter modification transforms rapid drug release into controlled sustained release, altering the pharmacokinetic profile to reduce side effects while simplifying the dosing regimen to once or twice daily administration, thereby improving patient compliance.
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 formulation achieves a synergistic effect with improved compatibility and patient compliance by maintaining stable plasma levels of both thiocolchicoside and analgesic over an extended period, allowing for once or twice daily dosing and reducing fluctuations that can cause chemical imbalances.
Implementation Method 1
first sustained release phase comprising an effective amount of thiocolchicoside or a pharmaceutically acceptable salt thereof and glyceryl behenate as release rate controlling agent
Data Source
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AI summary
This invention is a novel pharmaceutical formulations comprising a thiocolchicoside and an analgesic combination for oral administration with anti-inflammatory, analgesic, myorelaxant activity and methods of its manufacture. The pharmaceutical composition of the present invention is administered orally in tablet, multilayer tablet, multicoated tablet and capsule form.