Pharmaceutical compositions containing a fluoroquinolone antibiotic drug
View Patent ↗Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions.
1. An aqueous pharmaceutical composition, comprising:
a fluoroquinolone drug consisting of moxifloxacin in the composition at a concentration that is at least 0.4 w/v % but less than 1.0 w/v %; and
a pharmaceutical vehicle for the fluoroquinolone drug, the pharmaceutical vehicle consisting essentially of:
i. sodium chloride in an amount that provides a weight/volume ratio of sodium chloride to the fluoroquinolone drug in the composition that is between 1.0 and 1.7;
ii. a surfactant that assists in evenly distributing the fluoroquinolone drug throughout the pharmaceutical vehicle wherein the surfactant is a polyether alcohol;
iii. a borate and a polyol;
iv. a polysaccharide viscosity enhancing agent comprised of xanthan gum in an amount such that the concentration of the xanthan gum in the composition is at least 0.3 w/v % but less than 1.2 w/v % wherein the xanthan gum is at least 90% by weight of the viscosity enhancing agent;
v. a pH adjusting agent; and
vi. water;
wherein the composition is an aqueous ophthalmic solution and wherein the composition exhibits turbidity that is less than 13 NTU.
2. A composition as in claim 1 wherein the composition is located within a container that dispenses the composition as drops.
3. A composition as in claim 1 wherein the sodium chloride is in the composition at a concentration such that the weight/volume ratio of sodium chloride to the fluoroquinolone drug that is between 1.1 and 1.4.
4. A composition as in claim 1 wherein the polyol comprises sorbitol.
5. A composition as in claim 1 wherein the viscosity enhancing agent consists of xanthan gum.
6. A composition as in claim 1 wherein the pharmaceutical vehicle consists essentially of sodium chloride, a surfactant, a borate, a polyol, xanthan gum, sodium hydroxide and water.
7. A composition as in claim 1 wherein the composition has a pH of 6.8 to 7.4 and the turbidity is less than 10 NTU.
8. An aqueous pharmaceutical composition, comprising:
a fluoroquinolone drug wherein the fluoroquinolone drug is moxifloxacin at a concentration that is at least 0.4 w/v % but less than 1.0 w/v %; and
a pharmaceutical vehicle for the fluoroquinolone drug, the pharmaceutical vehicle consisting essentially of:
i. sodium chloride in an amount that provides a weight/volume ratio of sodium chloride to the fluoroquinolone drug in the composition that is between 1.1 and 1.4;
ii. a surfactant that assists in evenly distributing the fluoroquinolone drug throughout the pharmaceutical vehicle;
iii. a borate and a polyol; and
iv. a polysaccharide viscosity enhancing agent comprised of xanthan gum in an amount such that the concentration of the xanthan gum in the composition is at least 0.3 w/v % but is less than 1.2 w/v % wherein the xanthan gum is at least 90% by weight of the viscosity enhancing agent;
v, a pH adjusting agent; and
vi, water;
wherein the composition is an aqueous ophthalmic solution and wherein the composition is located within a container that dispenses the composition as drops and wherein the composition exhibits turbidity that is less than 10 NTU.
9. A composition as in claim 8 wherein the composition has a pH of 6.8 to 7.4.
10. A composition as in claim 8 wherein the polysaccharide viscosity enhancing agent consists of xanthan gum.
11. A composition as in claim 8 wherein the surfactant is a polyether alcohol.
12. A composition as in claim 8 wherein the surfactant is an alkyl aryl polyether alcohol.
13. A composition as in claim 12 wherein the polysaccharide viscosity enhancing agent consists of xanthan gum.
14. A composition as in claim 12 wherein the composition has a pH of 6.8 to 7.4.
15. A composition as in claim 1 wherein the surfactant is an alkyl aryl polyether alcohol.
16. An aqueous pharmaceutical composition, comprising:
a fluoroquinolone drug comprised of moxifloxacin in the composition at a concentration that is at least 0.4 w/v % but less than 0.7 w/v %; and
a pharmaceutical vehicle for the fluoroquinolone drug, the pharmaceutical vehicle including the following:
i. sodium chloride in an amount that provides a weight/volume ratio of sodium chloride to the fluoroquinolone drug in the composition that is between 1.1 and 1.4;
ii. a surfactant that assists in evenly distributing the fluoroquinolone drug throughout the pharmaceutical vehicle wherein the surfactant is a polyether alcohol;
iii. a borate and a polyol;
iv. a polysaccharide viscosity enhancing agent comprised of xanthan gum in an amount such that the concentration of the xanthan gum in the composition is at least 0.6 w/v % but is less than 0.75 w/v % wherein the xanthan gum is at least 90% by weight of the viscosity enhancing agent;
v. a pH adjusting agent; and
vi. water;
wherein the composition is an aqueous ophthalmic solution and wherein the composition exhibits turbidity that is less than 13 NTU.
17. A composition as in claim 16 wherein the composition has a pH of 6.8 to 7.4 and the turbidity is less than 10 NTU.