Oritavancin Formulation Using Hydroxypropyl Beta-Cyclodextrin
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current formulations of oritavancin require large volumes of diluent and long infusion times for intravenous administration, which can be problematic for renally impaired patients, necessitating a more efficient delivery method.
Innovation Solution
A pharmaceutical composition comprising oritavancin and hydroxypropyl β-cyclodextrin in a mass ratio of 0.25:1 to 4:1, which can be administered intravenously in both solid and solution forms, providing a therapeutically effective treatment for bacterial infections.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current oritavancin formulations are administered intravenously, then therapeutic effect is achieved, but large volumes of diluent and long infusion times are required
Solution Approach 1:
The patent changes the concentration parameter of oritavancin formulation from conventional levels to a high-concentration formulation (at least 5 mg/mL, preferably at least 10 mg/mL). This parameter change allows the same therapeutic dose to be delivered in smaller volumes and shorter times, directly resolving the contradiction between achieving therapeutic effect and reducing infusion time
Solution Approach 2:
The patent introduces a specific excipient or combination of excipients that enable the stabilization and solubility of high-concentration oritavancin. This intermediary substance allows the formulation to maintain high concentration without precipitation or degradation, making the high-concentration formulation feasible for clinical use
2Reliability
If current oritavancin formulations are administered intravenously, then therapeutic effect is achieved, but large volumes of diluent are required
Solution Approach 1:
The patent changes the concentration parameter from conventional formulations to high-concentration formulations (at least 5 mg/mL, preferably at least 10 mg/mL). This parameter change directly reduces the volume of diluent needed to deliver a therapeutic dose, resolving the contradiction between achieving therapeutic effect and reducing diluent volume
Solution Approach 2:
The patent optimizes the local quality of the formulation by using specific excipients that enhance solubility and stability at high concentrations. This allows the core active ingredient to be concentrated locally without compromising overall formulation stability, reducing the need for large volumes of diluent
3Productivity
If high concentration of oritavancin is formulated, then infusion time and volume are reduced, but formulation stability and solubility become more difficult to maintain
Solution Approach 1:
The patent introduces specific excipients that act as intermediaries to maintain the stability and solubility of high-concentration oritavancin. These excipients prevent precipitation, degradation, and aggregation of the active ingredient at high concentrations, resolving the contradiction between improving infusion efficiency and maintaining formulation stability
Solution Approach 2:
The patent creates a composite formulation system combining oritavancin with specific excipients that work synergistically to maintain stability at high concentrations. This composite approach allows the formulation to achieve both high concentration (improving productivity) and enhanced stability through the cooperative effects of its components
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 allows for a more efficient and tolerable administration of oritavancin, reducing infusion time and volume, thereby improving treatment efficacy and patient comfort, especially for renally impaired patients.
Implementation Method 1
A pharmaceutical composition comprising oritavancin, or a salt thereof, and hydroxypropyl β-cyclodextrin (HPCD)
Data Source
Figure 1
Figure 2
AI summary
Disclosed herein are antibacterial pharmaceutical compositions comprising oritavancin, or a salt thereof, and a modified β- cyclodextrin, and the therapeutic use and preparation of the same.