Benzodiazepine Composition Inducing Opiate Effect
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Solution Overview
Problem
Current pharmaceutical compositions do not induce an opiate-analogous effect, despite containing benzodiazepines or their derivatives, which are used for anxiety and sedation but lack the morphine-like effects.
Innovation Solution
A pharmaceutical composition combining lormetazepam and/or its derivatives with macrogol 15 hydroxystearate as a non-ionic solubilizer, administered in specific concentrations to induce Straub's phenomenon, an opiate-analogous effect characterized by an S-shaped dorsiflexion of the tail and perineum protrusion in mice.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Adaptability or versatility
If benzodiazepines or their derivatives are used in pharmaceutical compositions, then anxiety and sedation effects are achieved, but opiate-analogous effects are not induced
Solution Approach 1:
The patent combines lormetazepam (a benzodiazepine derivative) with macrogol 15 hydroxystearate (a non-ionic solubilizer) in specific concentrations to create a composition that produces both benzodiazepine effects and opiate-analogous Straub's phenomenon, thereby expanding the pharmacological effect spectrum
Solution Approach 2:
The invention creates a composite pharmaceutical composition where lormetazepam and macrogol 15 hydroxystearate work synergistically. The specific combination ratio and formulation create a new therapeutic agent with dual mechanisms of action, producing both anxiety-sedation effects and morphine-like Straub's phenomenon
2Adaptability or versatility
If lormetazepam is combined with macrogol 15 hydroxystearate in specific concentrations, then Straub's phenomenon is induced, but the composition complexity increases
Solution Approach 1:
The patent specifies precise concentration ranges for lormetazepam (0.1-10 mg/ml) and macrogol 15 hydroxystearate (1-50% w/v) to optimize the induction of Straub's phenomenon while maintaining formulation feasibility. These parameter specifications balance effect induction with manufacturing practicality
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 composition effectively induces Straub's phenomenon, previously only observed with morphine or morphine analogues, demonstrating an opiate-analogous effect suitable for anesthesia, intensive care, pain therapy, and neurology/psychiatry applications.
Implementation Method 1
Lormetazepam has a very high affinity for specific binding sites in the central nervous system. These binding sites are in close functional connection with the receptors of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). After binding to the receptor, lormetazepam potentiates GABAergic inhibition of the activity of downstream neurons.
Implementation Method 2
The non-ionic solubilizer is macrogol 15 hydroxystearate. Macrogol 15 hydroxystearate dissolves in water, ethanol and 2-propanol to form a clear solution.
Data Source
AI summary
The invention relates to a pharmaceutical composition characterized in that it comprises a benzodiazapine and/or benzodiazapine derivative, and a non-ionic solubilizer, and induces in said combination an analogous effect to an opiate, described as a Straub phenomenon.