DRUG VEHICLE COMPOSITIONS AND METHODS OF USE THEREOF
The invention is directed to a topical lidocaine gel composition comprising lidocaine or a salt thereof and magnesium chloride. The invention is further directed to a method of inducing local anesthesia in an eye of a patient comprising topically applying compositions of the present invention to the eye of the patient.
1 . A topical ophthalmological lidocaine gel composition comprising lidocaine or a salt thereof and magnesium chloride.
2 . The composition of claim 1 , wherein the lidocaine or a salt thereof is lidocaine hydrochloride.
3 . The composition of claim 1 , further comprising one or more excipients selected from the group consisting of a nonionic surfactant, a polyethylene glycol, mannitol, carboxymethyl cellulose and sodium chloride.
4 . The composition of claim 1 , wherein the lidocaine or a salt thereof is at a concentration from about 1% to about 5% w/v and the concentration of magnesium chloride is from about 0.01% to about 0.5% w/v, wherein w/v denotes weight by total volume of the composition.
5 . The composition of claim 3 , wherein the nonionic surfactant is polysorbate 80.
6 . The composition of claim 5 , wherein the polyethylene glycol is a polyethylene glycol having a molecular weight of from about 400 to about 20,000 Daltons.
7 . The composition of claim 6 , wherein polysorbate 80 is at a concentration from about 1.5% to about 5.9% w/v, the polyethylene glycol is at a concentration from about 0.1% to about 5% w/v, mannitol is at a concentration from about 0.1% to about 5% w/v, carboxymethyl cellulose is at a concentration from about 1% to about 5% w/v and the sodium chloride is at a concentration from about 0.1% to about 2% w/v, wherein w/v denotes weight by total volume of the composition.
8 . A method of inducing local anesthesia in an eye of a patient comprising topically applying the composition of claim 1 to the eye of the patient.
9 . A topical ophthalmological lidocaine gel composition comprising lidocaine or a salt thereof, magnesium chloride, a nonionic surfactant, a polyethylene glycol, mannitol, a viscosity enhancer and sodium chloride.
10 . A topical ophthalmological lidocaine gel composition comprising:
from about 3% to about 4% w/v lidocaine hydrochloride;
from about 3% to about 4% w/v polysorbate 80;
from about 0.25% to about 2.5% w/v of a polyethylene glycol having a molecular weight of from about 400 to about 20,000 Daltons;
from about 0.25% to about 1.5% w/v mannitol; and
from about 0.05% to about 0.2% w/v magnesium chloride,
wherein w/v denotes weight by total volume of the composition.
11 . The composition of claim 10 , further comprising:
from about 0.5% to about 1.5% w/v sodium chloride;
from about 1 millimolar to about 3 millimolar citrate buffer; and
from about 0.05% to about 0.2% w/v sorbate.
12 . A method of inducing local anesthesia in an eye of a patient comprising topically applying the composition of claim 10 to the eye of the patient.
13 . A topical ophthalmological lidocaine gel composition comprising:
about 3.5% w/v lidocaine hydrochloride;
about 3.5% w/v polysorbate 80;
from about 0.75% to about 1.50% w/v of a polyethylene glycol having a molecular weight of from about 400 to about 20,000 Daltons;
about 0.75% w/v mannitol;
about 0.1% w/v magnesium chloride;
from about 0.9% to about 1.25% w/v sodium chloride;
about 3 millimolar citrate buffer;
from about 1.25% to about 1.50% w/v carboxymethyl cellulose; and
about 0.1% w/v sorbate;
wherein w/v denotes weight by total volume of the composition.
14 . The composition of claim 13 , wherein:
the polyethylene glycol is polyethylene glycol 400 at a concentration of about 0.75% w/v;
sodium chloride is at a concentration of about 0.9% w/v; and
carboxymethyl cellulose is at a concentration of about 1.25% w/v.
15 . The composition of claim 13 , wherein:
the polyethylene glycol is polyethylene glycol 400 at a concentration of about 1.50% w/v;
sodium chloride is at a concentration of about 1.25% w/v; and
carboxymethyl cellulose is at a concentration of about 1.40% w/v.
16 . The composition of claim 13 , wherein:
the polyethylene glycol is polyethylene glycol 20000 at a concentration of about 1.50% w/v;
sodium chloride is at a concentration of about 1.25% w/v; and
carboxymethyl cellulose is at a concentration of about 1.50% w/v.
17 . A method of inducing local anesthesia in an eye of a patient comprising topically applying the composition of claim 13 to the eye of the patient.