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Last Updated: April 24, 2024

Details for Patent: 8,784,789


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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 Pharmaceutical Co., Ltd. (Osaka, JP)
Filing Date:Jul 30, 2003
Application Number:10/500,354
Claims:1. An aqueous liquid preparation consisting of, in an aqueous solution, an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof; a water-soluble metal chloride in a light-stabilizing effective amount; water; and optionally at least one material selected from the group consisting of a buffer, a preservative, a chelating agent, and a flavor; 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 %.

2. The aqueous liquid preparation of claim 1, wherein the metal chloride is at least one kind selected from sodium chloride, potassium chloride and calcium chloride.

3. The aqueous liquid preparation of claim 1, which is an acid addition salt of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyr- ic acid.

4. The aqueous liquid preparation of claim 3, wherein the acid addition salt is monobenzenesulfonate.

5. The aqueous liquid preparation of claim 1, wherein the aqueous liquid preparation has a pH in the range of 4-8.5.

6. The aqueous liquid preparation of claim 1, which is an eye drop.

7. The aqueous liquid preparation of claim 1, which is a nasal drop.

8. The aqueous liquid preparation of claim 1, wherein the metal chloride is at least one kind selected from alkali metal chlorides and alkaline earth metal chlorides.

9. 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) a water-soluble metal chloride; (c) sodium dihydrogen phosphate buffer; (d) a preservative; (e) water; and optionally (f) disodium edetate; 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 %.

10. An aqueous liquid preparation consisting of, in an aqueous solution, an active ingredient consisting of (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or a pharmacologically acceptable acid addition salt thereof, a water-soluble metal chloride in a light-stabilizing effective amount, 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 %, benzalkonium chloride, sodium dihydrogenphosphate dihydrate, sodium hydroxide and water.

11. The aqueous eye drop of claim 9, wherein: (i) the (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid or the pharmacologically acceptable acid addition salt thereof is (+)-(S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butyric acid monobenzenesufonate; (ii) the water-soluble metal chloride is sodium chloride; and (iii) the sodium chloride has a concentration selected from the range of a lower limit concentration of 0.2 w/v % and an upper limit concentration of 0.8 w/v %.

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