Concentrated Furosemide Formulation for Stable Subcutaneous Delivery
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Solution Overview
Problem
Furosemide's oral bioavailability is limited due to solubility and stability issues at acidic pH, necessitating intravenous administration, which requires trained professionals, while subcutaneous administration is hindered by discomfort and formulation instability.
Innovation Solution
Development of a liquid pharmaceutical formulation of furosemide with concentrations ranging from 40 mg/mL to 250 mg/mL, pH 6.5 to 8.5, using pharmaceutically acceptable excipients and buffers to enhance stability and minimize discomfort during subcutaneous administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If intravenous administration is used, then furosemide can be effectively administered, but it requires trained healthcare professionals for catheter placement and drug administration
Solution Approach 1:
The patent introduces a subcutaneous injection device as an intermediary tool that enables patients and caregivers to administer furosemide themselves, eliminating the need for trained healthcare professionals for each administration while maintaining reliable drug delivery through the specialized device mechanism
2Ease of operation
If subcutaneous administration is used, then administration can be performed by patients at home, but discomfort and pain during administration occur
Solution Approach 1:
The patent modifies the formulation parameters of furosemide by adjusting pH to a neutral range (7.0-8.5) and controlling osmolality (200-600 mOsm/kg), which significantly reduces pain and discomfort during subcutaneous administration while maintaining ease of self-administration
3Ease of operation
If furosemide is administered orally, then administration is convenient, but oral bioavailability is limited due to solubility and stability issues at acidic pH
Solution Approach 1:
The patent changes the administration route parameter from oral to subcutaneous, and simultaneously adjusts the formulation pH parameter to neutral (7.0-8.5), which resolves the bioavailability issue by eliminating acidic pH degradation while maintaining convenience through self-administration capability
4Ease of operation
If subcutaneous administration is used, then patient compliance can be improved, but formulation stability in solution is required for pre-loading into dispensing devices
Solution Approach 1:
The patent optimizes formulation parameters including pH (7.0-8.5), osmolality (200-600 mOsm/kg), and concentration (10-250 mg/mL) to simultaneously achieve formulation stability for device pre-loading and patient compliance through easy self-administration
Data Source
AI summary
Disclosed herein, in part, are liquid pharmaceutical formulations comprising furosemide or a pharmaceutically acceptable salt thereof, one or more pharmaceutically acceptable excipients, and a pharmaceutically acceptable buffer. Methods of treating congestion, edema, fluid overload, or hypertension in a patient in need thereof are also provided.