Bilastine–β-Cyclodextrin Injection for Rapid Once-Daily Allergy Treatment
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Solution Overview
Problem
There is a lack of effective and well-tolerated parenteral antihistamine formulations suitable for immediate action in severe allergic reactions, with existing options causing sedation and other adverse effects, and current formulations are not suitable for once-daily administration.
Innovation Solution
Aqueous parenteral pharmaceutical compositions comprising 0.96-2.60% w/v bilastine and 10-30% w/v β-cyclodextrin, with a pH between 3.0 and 7.2, for intravenous or intramuscular administration, providing rapid onset, high efficacy, and minimal side effects, allowing once-daily treatment of severe allergic reactions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If parenteral formulations of first-generation antihistamines are used for immediate action in severe allergic reactions, then rapid onset of action is achieved, but sedation and cognitive impairment occur
Solution Approach 1:
The patent changes the chemical parameter by using second-generation antihistamines (bilastine, fexofenadine, cetirizine) instead of first-generation agents. These compounds have modified molecular structures that prevent central nervous system penetration, eliminating sedation while maintaining H1 receptor antagonism. The formulation enables parenteral administration of these previously oral-only agents, achieving rapid onset without harmful side effects.
2Speed
If topical antihistaminic agents are used for ocular allergic reactions, then faster onset of action is achieved, but the treatment is limited to ocular symptoms only
Solution Approach 1:
The patent creates a universal parenteral formulation that can treat multiple types of allergic reactions systemically (urticaria, rhinitis, conjunctivitis, anaphylaxis) rather than being limited to ocular symptoms. The injectable route delivers the drug systemically, making the same formulation applicable to diverse allergic conditions while maintaining rapid onset of action.
3Adaptability or versatility
If oral antihistaminic agents are used for allergy treatment, then broader spectrum of diseases is treated, but delayed onset of action occurs
Solution Approach 1:
The patent uses the hydraulic principle of parenteral injection to deliver the drug directly into the bloodstream, bypassing the gastrointestinal tract and first-pass metabolism. This eliminates the delay associated with oral absorption and achieves rapid therapeutic levels in the blood, while maintaining the ability to treat systemic allergic conditions.
4Speed
If existing parenteral antihistamine formulations are used for severe allergic reactions, then immediate action is achieved, but the formulations are not suitable for once-daily administration
Solution Approach 1:
The patent selects second-generation antihistamines with inherently long half-lives and prolonged duration of action. These compounds are designed to provide 24-hour coverage with once-daily dosing. The parenteral formulation delivers the full therapeutic dose immediately, achieving both rapid onset and extended duration of effectiveness in a single administration.
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 achieves fast drug onset, high efficacy, and minimal side effects, effectively reducing allergic symptoms within 15 minutes and maintaining effectiveness for up to 24 hours, suitable for once-daily administration.
Implementation Method 1
aqueous parenteral pharmaceutical compositions comprising 0.96-2.60% w/v bilastine and 10-30% w/v β-cyclodextrin
Data Source
AI summary
The invention relates to an aqueous parenteral pharmaceutical composition comprising:a) 0.96-2.60% w/v of bilastine, or a pharmaceutically acceptable salt or solvate thereof,b) 10-30% w/v of a β-cyclodextrin selected from unmodified β-cyclodextrin, C1-C6 alkyl-β-cyclodextrin, C1-C6 hydroxyalkyl β-cyclodextrin, C1-C6 carboxyalkyl-β-cyclodextrin, carbonyl-β-cyclodextrin, C1-C6 sulfoalkylether β-cyclodextrin and mixtures thereof,wherein the pH value of the composition is between 3.0 and 7.2, both lower and upper limits of the range included and wherein parenteral is selected from intravenous or intramuscular;and its use in the treatment and/or prevention of conditions mediated by H1 histamine receptor, such as allergic disorders or diseases and allergic symptoms; particularly when immediate action is required.