Pre-mixed, ready-to-use pharmaceutical compositions
Inventors
Duncan, Michelle Renee • Gupta, Supriya • Haas, David Hartley • Nenonene, Norma V. • Zamiri, Camellia
Assignees
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Publication Number
US-11547758-B2
Publication Date
2023-01-10
Expiration Date
Abstract
Provided herein are ready-to-use premixed pharmaceutical compositions of nicardipine or a pharmaceutically acceptable salt and methods for use in treating cardiovascular and cerebrovascular conditions.
Core Innovation
The invention provides a method for preventing acute elevations of blood pressure in a human subject in need thereof by parenterally administering a pharmaceutical composition comprising a pre-mixed aqueous solution of nicardipine or a pharmaceutically acceptable salt thereof and a tonicity agent. The composition is contained in a pharmaceutically acceptable container such that the solution is in contact with non-polar polymers, requires no dilution before administration, and has a pH from about 3.6 to about 4.4.
The pre-mixed aqueous solution demonstrates storage stability in the container at room temperature for at least three months, exhibiting less than a 10% decrease in the concentration of nicardipine or pharmaceutically acceptable salt thereof and a total impurity formation of less than about 3%. The disclosed ready-to-use formulations are described as premixed aqueous nicardipine injectable compositions with buffered pH and tonicity agents.
The document additionally describes optional cosolvents and complexing agents such as sorbitol, propylene glycol, and cyclodextrin complexing agents. It further describes compatibility of the pharmaceutical composition with containers and packaging materials, including contact with non-polar polymers and comparisons of plastic contact compatibility across packaging systems.
Claims Coverage
The disclosed claims include one independent claim directed to preventing acute elevations of blood pressure using a specific ready-to-use pre-mixed aqueous nicardipine pharmaceutical composition. The independent claim centers on three inventive features combining formulation composition, container contact with non-polar polymers, and demonstrated room-temperature stability for at least three months, defined by concentration decrease and total impurity formation limits.
Dilution-free pre-mixed aqueous nicardipine solution with defined tonicity agent
A parenterally administered pharmaceutical composition comprising a pre-mixed aqueous solution containing from about 0.1 to 0.4 mg/mL nicardipine or a pharmaceutically acceptable salt thereof and a tonicity agent, where the composition requires no dilution before administration and has a pH from about 3.6 to about 4.4.
Container in contact with non-polar polymers
The aqueous solution is contained in a pharmaceutically acceptable container such that the solution is in contact with non-polar polymers.
Room-temperature stability in-container for at least three months
When stored in the container for at least three months at room temperature, the composition exhibits less than a 10% decrease in the concentration of nicardipine or pharmaceutically acceptable salt thereof and a total impurity formation of less than about 3%.
Overall, the claim coverage is focused on a ready-to-use, dilution-free pre-mixed aqueous nicardipine composition with a defined concentration and tonicity agent, a pH between about 3.6 and about 4.4, and demonstrated chemical stability after at least three months at room temperature while the solution is in contact with non-polar polymer containers.
Stated Advantages
Less than a 10% decrease in the concentration of nicardipine or pharmaceutically acceptable salt thereof after at least three months at room temperature.
Total impurity formation of less than about 3% after at least three months at room temperature.
Documented Applications
Preventing acute elevations of blood pressure in a human subject in need thereof by parenterally administering the described pharmaceutical composition.
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