Ophthalmic emulsion
The present invention is directed to an ophthalmic emulsion. The emulsion has a unique combination of ingredients that promotes the stability of small oil droplets within the emulsion. The emulsion also includes a mucoadhesive polymer that aid in delivering a lipid to the ocular surface.
1. An ophthalmic emulsion, the emulsion comprising:
water forming an aqueous phase;
oil forming an oil phase, wherein the oil is at least 0.1 w/v % and not greater than 5 w/v % of the emulsion;
a hydrophilic surfactant having an HLB value of at least 8, wherein the hydrophilic surfactant is present in the emulsion in an amount that is at least 0.08 w/v % and no greater than 0.8 w/v %;
a hydrophobic surfactant having an HLB value of below 8, wherein the hydrophobic surfactant is present in the emulsion in an amount that is at least 0.11 w/v % and no greater than 2.0 w/v %;
an anionic phospholipid;
borate;
a mucoadhesive galactomannan polymer, wherein the mucoadhesive galactomannan polymer is present in the emulsion in a concentration of at least 0.01 w/v %, but no greater than 1.0 w/v %;
wherein the emulsion is free of a benzalkonium chloride,
wherein:
i. the oil phase is in droplets within the aqueous phase and the droplets have an average diameter that is no greater than about 1000 nm, but is at least 10 nm, wherein the average diameter is corresponding to 90% of the cumulative undersize distribution by volume measured using a Microtrac S3500 Particle Size Analyzer (Software Version 10.3.1); and
ii. the borate and galactomannan polymer cooperatively act to form a gel upon instillation of the emulsion in an eye of an individual.
2. The emulsion according to claim 1 wherein the oil is a hydrocarbon selected from mineral oil, paraffin oil and petrolatum.
3. The emulsion according to claim 1 wherein the hydrophilic surfactant is polyoxyethylene-40-stearate.
4. The emulsion according to claim 1 wherein the hydrophobic surfactant is a sorbitan tristearate.
5. The emulsion according to claim 1 wherein the mucoadhesive galactomannan polymer is selected from the group consisting of guar and hydroxypropyl guar.
6. The emulsion according to claim 1 wherein the anionic phospholipid is dimyristoyl phosphatidylglycerol.
7. The emulsion according to claim 1 wherein the phospholipid is present in the emulsion in a concentration from 0.05 to 7.0 percent by weight.
8. The emulsion according to claim 1 further comprising a borate/polyol buffer system.
9. The emulsion according to claim 1 wherein the oil phase is in droplets within the aqueous phase and the droplets have an average diameter that is no greater than 500 nm but is at least 100 nm, wherein the average diameter is corresponding to 90% of the cumulative undersize distribution by volume measured using a Microtrac S3500 Particle Size Analyzer (Software Version 10.3.1).