Dexketoprofen Tramadol Injectable Composition Stabilization
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Solution Overview
Problem
The combination of dexketoprofen and tramadol in high concentrations is challenging to stabilize for injectable forms due to incompatibilities, making it difficult to prepare effective and stable pharmaceutical compositions for parenteral administration, especially for pain treatment of moderate to severe intensity.
Innovation Solution
A pharmaceutical composition comprising dexketoprofen tromethamine, tramadol hydrochloride, ethanol, and water for injection, with specific concentration ranges (15 mg to 75 mg/ml for dexketoprofen, 10 mg to 150 mg/ml for tramadol, and 5 mg to 200 mg/ml for ethanol) that is stable and suitable for direct injection or dilution, facilitating rapid and effective pain control with reduced side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If high concentrations of dexketoprofen and tramadol are combined for effective pain treatment, then the analgesic efficacy is improved, but the compositional stability deteriorates due to incompatibilities between the two active ingredients
Solution Approach 1:
The patent uses ethanol as an intermediary solvent to stabilize the combination of dexketoprofen and tramadol at high concentrations. The ethanol co-solvent system mediates between the two incompatible active ingredients, preventing precipitation and maintaining compositional stability while enabling effective therapeutic concentrations.
Solution Approach 2:
The patent changes the physical-chemical parameters of the pharmaceutical composition by adjusting the ethanol concentration (5-200 mg/ml) and pH levels. These parameter modifications enable the stable coexistence of high concentrations of both active ingredients by altering the solvent properties and solubility characteristics of the system.
2Quantity of substance
If typical opioids are used for pain treatment, then the analgesic effect is improved, but the harmful side effects increase (nausea, vomiting, respiratory depression, constipation, dependency)
Solution Approach 1:
The patent merges two different analgesic mechanisms by combining dexketoprofen (NSAID with COX inhibition) and tramadol (atypical opioid). This combination allows for synergistic pain relief while reducing the dosage of each individual agent, thereby minimizing the harmful side effects associated with typical opioids while maintaining effective analgesia.
3Quantity of substance
If dexketoprofen is administered to achieve strong anti-inflammatory and analgesic action, then the therapeutic effect is improved, but the gastrointestinal adverse effects increase due to COX-1 inhibition
Solution Approach 1:
The patent combines dexketoprofen with tramadol to achieve a multimodal analgesic effect. This combination allows for lower doses of dexketoprofen to be used while maintaining effective pain relief, thereby reducing the gastrointestinal adverse effects caused by COX-1 inhibition while preserving the therapeutic benefits through the complementary action of tramadol.
Data Source
AI summary
This invention refers to an injectable pharmaceutical composition of dexketoprofen and tramadol as active ingredients. In particular, this is a solution of dexketoprofen and tramadol in a mixture of water for injection and at least one cosolvent. This invention also refers to the process for preparing this composition, to a unit dosage pharmaceutical form that contains it and to its use for the treatment of moderate to severe pain, inflammation and/or fever.