Claims for Patent: 10,813,976

Summary for Patent: 10,813,976

Title:	Ophthalmic compositions comprising ciclosporin
Abstract:	The present invention relates to compositions in the form of a clear solution comprising ciclosporin with low residual water content and 1-perfluorobutylpentane. The compositions may be used for topical administration to the eye.
Inventor(s):	Frank LÖSCHER, Ralf GRILLENBERGER, Johan Engblom
Assignee:	Novaliq GmbH
Application Number:	US16/336,005
Patent Claims:	1. A composition comprising ciclosporin dissolved in 1-perfluorobutyl-pentane, wherein the ciclosporin has a water content of less than about 1.0 wt %, based on the total weight of the ciclosporin. 2. The composition according to claim 1, wherein the ciclosporin is dissolved in the absence of a co-solvent. 3. The composition according to claim 1, wherein the concentration of ciclosporin dissolved in the composition at 15-25° C. is greater than about 2.6 mg/mL. 4. The composition according to claim 1, wherein the concentration of ciclosporin dissolved in the composition at 15-25° C. is from 3.0 to 4.8 mg/mL. 5. The composition according to claim 4, wherein the concentration of ciclosporin dissolved in the composition at 15-25° C. is about 4.0 mg/mL. 6. The composition according to claim 1, wherein the 1-perfluorobutyl-pentane has a water content of less than 0.00016 mg/mL. 7. The composition according to claim 1, wherein the ciclosporin has a water content of less than 0.8 wt %, or less than 0.7 wt %, or less than 0.6 wt %, or less than 0.5 wt %, or less than 0.4 wt %, based on the total weight of the ciclosporin. 8. The composition according to claim 1, wherein the concentration of ciclosporin dissolved in the composition at 15-25° C. is from 3.0 to 4.8 mg/mL and wherein the composition has a total residual water content of less than 0.02 mg/mL. 9. The composition according to claim 1, wherein the composition is a pharmaceutical composition formulated for topical ophthalmic administration. 10. The composition according to claim 1, wherein the ciclosporin is amorphous or is not predominantly in any specific crystal form. 11. The composition according to claim 1, wherein the composition consists of the ciclosporin and the 1-perfluorobutyl-pentane and wherein the composition has a total residual water content of less than about 0.04 mg/mL. 12. A pharmaceutical kit, comprising: (i) a composition as defined in claim 1; (ii) a container adapted for holding the composition, wherein the container has a dispensing means adapted for topical administration of the composition to the eye or ophthalmic tissue; (iii) optionally, a water-desiccant; and (iv) optionally, instructions for use of the kit in the treatment of kerato-conjunctivitis sicca or a symptom thereof, or for use of the kit in the treatment of meibomian gland dysfunction or a symptom thereof. 13. A method for the preparation of a composition in the form of a clear solution comprising ciclosporin dissolved in 1-perfluorobutyl-pentane, and wherein the composition is essentially free of a co-solvent, the method comprising the steps of a) providing ciclosporin with a water content of less than about 1.0 wt % based on the total weight of the ciclosporin, and b) dissolving said ciclosporin in 1-perfluorobutyl-pentane. 14. The method according to claim 13, wherein step a) of providing ciclosporin with a water content of less than about 1.0 wt % based on the total weight of ciclosporin, comprises a step of drying ciclosporin with a water content of about 1.6 wt %, or greater than about 1.6 wt % based on the total weight of the ciclosporin. 15. The method according to claim 14, wherein step a) comprises drying ciclosporin under vacuum, optionally in the presence of a water-desiccant or drying agent.