PRE-MIXED, READY-TO-USE IV BOLUS NICARDIPINE COMPOSITIONS AND METHODS OF USE
Provided herein are ready-to-use premixed bolus injection pharmaceutical compositions of nicardipine or a pharmaceutically acceptable salt and methods for use in treating cardiovascular and cerebrovascular conditions.
1 - 18 . (canceled)
19 . An inclusion complex of nicardipine or a pharmaceutically acceptable salt thereof and a sulfoalkylated β-cyclodextrin.
20 . The inclusion complex of claim 19 , wherein the sulfoalkylated β-cyclodextrin is sulfobutylated β-cyclodextrin.
21 . The inclusion complex of claim 20 , wherein the sulfobutylated β-cyclodextrin is sulfobutylether β-cyclodextrin.
22 . The inclusion complex of claim 20 , wherein the pharmaceutically acceptable salt of nicardipine is the nicardipine hydrochloride salt.
23 . A pharmaceutical composition comprising an inclusion complex of claim 19 , wherein the composition is formulated for parenteral bolus administration to a human subject.
24 . The pharmaceutical composition of claim 23 , wherein the sulfoalkylated β-cyclodextrin is a sulfobutylated β-cyclodextrin having an average of 5 to 8 degrees of sulfobutylation.
25 . (canceled)
26 . The pharmaceutical composition of claim 23 , comprising a pharmaceutically acceptable salt of nicardipine in an parenterally injectable aqueous carrier containing one or more buffering agents and having a pH within the range from about 3.5 to about 7.5, wherein the concentration of the nicardipine in the composition is from 0.25 mg/ml to 5 mg/ml, inclusive, the concentration of the sulfoalkylated β-cyclodextrin in the composition is from 0.1% to 25% (w/v) inclusive, the concentration of each buffering agent in the composition is 0.1 mM to 100 mM.
27 . The pharmaceutical composition of claim 26 , wherein the sulfoalkylated β-cyclodextrin is a sulfobutylated β-cyclodextrin having an average of 5 to 8 degrees of sulfobutylation.
28 . (canceled)
29 . The pharmaceutical composition of claim 26 , wherein the nicardipine is in a concentration of from 0.25 to 1 mg/ml.
30 . The pharmaceutical composition of claim 26 , wherein the nicardipine concentration is about 0.5 mg/ml.
31 . The pharmaceutical composition of claim 27 , wherein the sulfobutylated β-cyclodextrin concentration is from 0.5 to 10% (w/v).
32 . The pharmaceutical composition of claim 27 , wherein the sulfobutylated β-cyclodextrin concentration is from 0.1 to 0.5% (w/v).
33 . The pharmaceutical composition of claim 26 , wherein the composition is in unit dose format and the unit dose contains the formulation in a volume of from 0.5 to 20 ml, inclusive.
34 . The pharmaceutical composition of claim 26 , wherein the nicardipine concentration in the aqueous formulation is from 0.3 mg/ml to 0.7 mg/ml, inclusive.
35 . The pharmaceutical composition of claim 26 , wherein the nicardipine concentration of the aqueous formulation is about 0.5 mg/ml.
36 . The pharmaceutical composition of claim 26 , wherein the buffering agent is one or more agents selected from the group consisting of acetate, citrate, succinate, and phosphate buffering agents.
37 - 38 . (canceled)
39 . The pharmaceutical composition of claim 26 , further comprising a tonicity adjusting agent.
40 . (canceled)
41 . The pharmaceutical composition of claim 26 , wherein the composition further comprises at least one co-solvent in a concentration of 0.1 to 25% (w/v).
42 . The pharmaceutical composition of claim 41 , wherein concentration of at least one co-solvent is 0.1 to 10% (w/v).
43 . (canceled)
44 . The pharmaceutical composition of claim 26 , wherein the pH is above a pH of 3.5 and equal to or less than a pH of 5.5.
45 - 51 . (canceled)