Nasal calcitonin formulations containing chlorobutanol
View Patent ↗An aqueous solution of calcitonin suitable for intranasal administration comprised of calcitonin, chlorobutanol at a concentration of less than 0.4% weight/weight, and water and having a pH of less than 4 with the proviso that benzalkonium chloride is not present in the solution. The aqueous solution of calcitonin can be used to treat osteoporosis, Paget's bone disease and hypercalcemia.
1. A method for intranasal administration of calcitonin which comprises administering intranasally to an individual a solution of calcitonin comprising calcitonin, water, sodium chloride and only one preservative, wherein the preservative is chlorobutanol at a concentration equal to or greater than about 0.25% and less than about 0.4% weight/weight.
2. The method of claim 1 , wherein the calcitonin is present in the solution at a concentration of about 0.0355 weight/weight, the sodium chloride is present in the solution at a concentration of about 0.85%, and the solution has a pH of less than 4 and an oxygen at a content of less than about 5%.
3. The method of claim 1 , wherein the solution of calcitonin is administered into a nose of an individual through an actuator tip as a spray, wherein the spray has a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip.
4. The method of claim 3 , wherein the spray produces droplets, wherein less that 5% of the droplets are less than 10 microns in size.
5. The method of claim 3 , wherein the spray has a spray pattern major axis of about 31.2 mm and a minor axis of about 27.4 mm.
6. A composition comprising calcitonin, water, sodium chloride and only one preservative, wherein the preservative is chlorobutanol at a concentration equal to or greater than about 0.25% and less than about 0.4% weight/weight, and wherein the composition is suitable for intranasal administration in humans.
7. A composition consisting essentially of calcitonin, water, sodium chloride, a single preservative and optionally hydrochloric acid, wherein the single preservative is chlorobutanol at a concentration equal to or greater than about 0.25% and less than about 0.4% weight/weight, and wherein the composition is suitable for intranasal administration in humans.
8. A composition consisting essentially of a solution of (i) calcitonin, (ii) chlorobutanol at a concentration equal to or greater than about 0.25% and less than about 0.4% weight/weight, (iii) water, (iv) sodium chloride, and optionally (v) hydrochloric acid, wherein the composition has a pH of 4 or less, and wherein the composition is suitable for intranasal administration in humans.
9. A pharmaceutical device comprising a composition according to claim 6 and an actuator to produce an aerosol spray of the composition, the spray having a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip.
10. A pharmaceutical device comprising a composition according to claim 6 and an actuator to produce an aerosol spray of the composition, wherein the spray has a spray pattern major axis of about 31.2 mm and a minor axis of about 27.4 mm.
11. A pharmaceutical device comprising a composition according to claim 6 and an actuator to produce an aerosol spray of the composition, the spray having a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip, wherein less than 5% of the droplets are smaller than 10 microns in size.
12. A pharmaceutical device comprising a composition according to claim 7 and an actuator to produce an aerosol spray of the composition, the spray having a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip.
13. A pharmaceutical device comprising a composition according to claim 7 and an actuator to produce an aerosol spray of the composition, wherein the spray has a spray pattern major axis of about 31.2 mm and a minor axis of about 27.4 mm.
14. A pharmaceutical device comprising a composition according to claim 7 and an actuator to produce an aerosol spray of the composition, the spray having a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip, wherein less than 5% of the droplets are smaller than 10 microns in size.
15. A pharmaceutical device comprising a composition according to claim 8 and an actuator to produce an aerosol spray of the composition, the spray having a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip.
16. A pharmaceutical device comprising a composition according to claim 8 and an actuator to produce an aerosol spray of the composition, wherein the spray has a spray pattern major axis of about 31.2 mm and a minor axis of about 27.4 mm.
17. A pharmaceutical device comprising a composition according to claim 8 and an actuator to produce an aerosol spray of the composition, the spray having a spray pattern ellipticity ratio of from about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip, wherein less than 5% of the droplets are smaller than 10 microns in size.