Bilastine β-Cyclodextrin Injection for Once-Daily Rapid Allergy Relief
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a lack of effective and well-tolerated parenteral antihistamine formulations for immediate treatment of severe allergic reactions, with existing options causing sedation and drowsiness, and existing bilastine compositions have low water solubility, making once-daily administration impractical.
Innovation Solution
Aqueous parenteral pharmaceutical compositions containing 0.96% to 2.60% w/v bilastine and 10% to 30% w/v β-cyclodextrin, with a pH between 3.0 and 7.2, for intravenous or intramuscular administration, providing fast onset, high efficacy, and reduced side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If parenteral antihistamine formulations are used for immediate treatment of severe allergic reactions, then rapid action is achieved, but existing options cause sedation and drowsiness
Solution Approach 1:
The patent changes the chemical parameters of the antihistamine molecule by developing bilastine, a second-generation H1 antagonist with modified molecular structure that selectively blocks H1 receptors without crossing the blood-brain barrier, thereby eliminating sedative effects while maintaining rapid parenteral action
2Reliability
If bilastine compositions are formulated for parenteral administration, then effective treatment is achieved, but low water solubility makes once-daily administration impractical
Solution Approach 1:
The patent changes the physical parameter of water solubility by formulating bilastine as a sodium salt (bilastine sodium) which has significantly higher aqueous solubility than the free base form, enabling formulation of stable once-daily parenteral injections
3Speed
If first-generation antihistamines are administered parenterally, then immediate action is achieved, but they cause extreme sleepiness and cognitive impairment
Solution Approach 1:
The patent changes the pharmacological parameters by developing second-generation H1 antagonists with selective peripheral action that do not cross the blood-brain barrier, eliminating CNS side effects while maintaining rapid parenteral efficacy through optimized molecular structure and salt form
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 rapid action within 15 minutes, maintains effectiveness for 24 hours, and allows once-daily administration without sedation or drowsiness, outperforming existing treatments in efficacy and side effect profile.
Implementation Method 1
aqueous parenteral pharmaceutical compositions containing 0.96% to 2.60% w/v bilastine and 10% to 30% w/v β-cyclodextrin
Data Source
Figure 1a~1d
Figure 2
Figure 3
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.