Pre-mixed, ready-to-use pharmaceutical compositions
Inventors
Duncan, Michelle Renee • Gupta, Supriya • Haas, David Hartley • Stephens, Norma V. • Zamiri, Camellia
Assignees
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Publication Number
US-9364564-B2
Publication Date
2016-06-14
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 relates to a pharmaceutical composition for parenteral administration that is a pre-mixed aqueous solution containing nicardipine or a pharmaceutically acceptable salt thereof, a tonicity agent, and a buffer. The composition requires no dilution before administration and has a pH from about 3.6 to about 4.4.
A central feature is container-based stability: when stored in a pharmaceutically acceptable container in contact with non-polar polymers for at least three months at room temperature, the solution exhibits less than a 10% decrease in the concentration of nicardipine or pharmaceutically acceptable salt thereof and a total impurity formulation of less than about 3%.
The disclosure further defines particular formulation and container-contact aspects. In one aspect, the tonicity agent is selected from sodium chloride or dextrose, the solution includes from 0 mg/mL to about 4 mg/mL sorbitol, and the container comprises copolyester, polyethylene, or polyolefin.
Claims Coverage
The provided document content includes two independent claims that cover pre-mixed, ready-to-use aqueous nicardipine solutions for parenteral administration with defined composition parameters, defined container contact with non-polar polymers, and container-based room-temperature stability for at least three months under impurity and concentration-loss limits.
Dilution-free pre-mixed aqueous nicardipine composition for parenteral administration
A pharmaceutical composition for parenteral administration comprising a pre-mixed aqueous solution comprising nicardipine or a pharmaceutically acceptable salt thereof, a tonicity agent, and a buffer, wherein the composition requires no dilution before administration and has a pH from about 3.6 to about 4.4.
Container 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 container stability for at least three months
The aqueous solution when stored in the container for at least three months at room temperature exhibits less than a 10% decrease in the concentration of nicardipine or pharmaceutically acceptable salt thereof and a total impurity formulation of less than about 3%.
Tonicity agent selected from sodium chloride or dextrose with sorbitol inclusion
The tonicity agent is selected from sodium chloride or dextrose, and the solution includes from 0 mg/mL to about 4 mg/mL sorbitol.
Container comprising copolyester, polyethylene or polyolefin
The aqueous solution is contained in a pharmaceutically acceptable container comprising copolyester, polyethylene or polyolefin.
Across the independent claims, the inventive subject matter is anchored by a dilution-free, pre-mixed aqueous nicardipine composition for parenteral administration with defined pH, defined container contact with non-polar polymers, and demonstrated room-temperature stability for at least three months with limits on nicardipine concentration decrease and total impurities.
Stated Advantages
Exhibiting less than a 10% decrease in the concentration of nicardipine or pharmaceutically acceptable salt thereof when stored in the container for at least three months at room temperature.
Having a total impurity formulation of less than about 3% when stored in the container for at least three months at room temperature.
Extending the required room-temperature stability duration to at least one year while maintaining less than a 10% concentration decrease and total impurities of less than about 3%.
Documented Applications
Parenteral administration using a pre-mixed aqueous nicardipine composition that requires no dilution before administration.
Use in continuous intravenous infusion is described in the provided content as a context for the ready-to-use formulation.
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