Claims for Patent: 8,877,168

Summary for Patent: 8,877,168

Title:	Aqueous liquid preparations and light-stabilized aqueous liquid preparations
Abstract:	An aqueous liquid preparation containing (+)-(S)-4-[4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, which is stabilized with a water-soluble metal chloride, is provided.
Inventor(s):	Higashiyama; Masayo (Kobe, JP)
Assignee:	Senju Pharmaceuticals Co., Ltd. (Osaka, JP)
Application Number:	14/314,678
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,877,168
Patent Claims:	1. An aqueous liquid preparation consisting of, in an aqueous solution: (a) an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof; (b) a water-soluble metal chloride in a light-stabilizing effective amount; (c) water; and (d) at least one material selected from the group consisting of a buffer, a preservative, a chelating agent, sodium hydroxide, and a flavor; wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.1 w/v % and an upper limit concentration of 2.0 w/v %; and wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.15 w/v % and an upper limit concentration of 1.5 w/v %. 2. The aqueous liquid preparation according to claim 1, wherein the metal chloride is selected from the group consisting of sodium chloride, potassium chloride and calcium chloride. 3. The aqueous liquid preparation according to claim 1, wherein the acid addition salt is monobenzenesulfonate. 4. The aqueous liquid preparation according to claim 1, wherein the aqueous liquid preparation has a pH in the range of 4-8.5. 5. The aqueous liquid preparation according to claim 1, wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 1.2 w/v %. 6. The aqueous liquid preparation according to claim 1, wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.2 w/v %. 7. The aqueous liquid preparation according to claim 1, wherein the metal chloride is sodium chloride and has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.0 w/v %. 8. The aqueous liquid preparation according to claim 1, wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 2.0 w/v %. 9. The aqueous liquid preparation according to claim 1, wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.5 w/v %. 10. The aqueous liquid preparation according to claim 1, wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.5 w/v % and an upper limit concentration of 1.5 w/v %. 11. The aqueous liquid preparation according to claim 1, which is an eye drop. 12. The aqueous liquid preparation according to claim 1, which is a nasal drop. 13. The aqueous liquid preparation according to claim 1, wherein: (a) the acid addition salt of the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid is monobenzenesulfonate salt, and the acid addition salt has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.5 w/v %; (b) the water-soluble metal chloride is selected from the group consisting of sodium chloride, potassium chloride, and calcium chloride, and the metal chloride has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.0 w/v %; and the aqueous liquid preparation has a pH min the range of 5-8. 14. The aqueous liquid preparation according to claim 13, wherein the metal chloride is sodium chloride. 15. The aqueous liquid preparation according to claim 13, wherein the metal chloride is potassium chloride. 16. An aqueous eye drop consisting of: (a) an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof; (b) at least one water-soluble metal chloride selected from the group consisting of sodium chloride, potassium chloride, and calcium chloride; (c) sodium dihydrogenphosphate buffer; (d) a preservative; (e) water; and (f) sodium hydroxide; wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 1.2 w/v %; and wherein the pH is in the range of 5-8. 17. The aqueous liquid preparation according to claim 16, wherein the acid addition salt is monobenzenesulfonate. 18. The aqueous liquid preparation according to claim 16, wherein the metal chloride has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.2 w/v %. 19. The aqueous liquid preparation according to claim 16, wherein the metal chloride is sodium chloride and has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.0 w/v %. 20. The aqueous liquid preparation according to claim 16, wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 2.0 w/v %. 21. The aqueous liquid preparation according to claim 16, wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.5 w/v %. 22. The aqueous liquid preparation according to claim 16, wherein the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof has a concentration selected from the range of a lower limit concentration of 0.5 w/v % and an upper limit concentration of 1.5 w/v %. 23. An aqueous liquid preparation consisting of, in an aqueous solution: (a) an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof; (b) a water-soluble metal chloride; (c) benzalkonium chloride; (d) sodium dihydrogenphosphate dihydrate; (e) sodium hydroxide; and (f) water; wherein the metal chloride is sodium chloride and has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.0 w/v %; and wherein the pH is in the range of 6-8. 24. The aqueous liquid preparation according to claim 23, wherein the active ingredient consists of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid monobenzenesulfonate. 25. The aqueous liquid preparation according to claim 24, wherein the sodium chloride has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 0.8 w/v %. 26. The aqueous liquid preparation according to claim 25, wherein the active ingredient has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 2.0 w/v %. 27. The aqueous liquid preparation according to claim 26, wherein the active ingredient has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 1.5 w/v %. 28. The aqueous liquid preparation according to claim 26, wherein the active ingredient has a concentration selected from the range of a lower limit concentration of 0.5 w/v % and an upper limit concentration of 1.5 w/v %. 29. The aqueous liquid preparation according to claim 23, wherein (a) the acid addition salt of the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid is monobenzenesulfonate salt, and the monobenzenesulfonate salt has a concentration selected from the range of a lower limit concentration of 0.5 w/v % and an upper limit concentration of 1.5 w/v %; and (b) the water-soluble metal chloride is sodium chloride, and the sodium chloride has a concentration selected from the range of a lower limit concentration of 0.3 w/v % and an upper limit concentration of 0.8 w/v %. 30. The aqueous liquid preparation according to claim 29, wherein the monobenzenesulfonate salt has a concentration of 1.5 w/v %.