STABLE OXALIPLATIN-ENCAPSULATING LIPOSOME AQUEOUS DISPERSION AND METHOD FOR STABILIZING SAME

• US 20150216801A1
• Filed: 08/09/2013
• Published: 08/06/2015
• Est. Priority Date: 08/10/2012
• Status: Active Grant

• Current Assignee: Taiho Pharmaceutical Company Limited (Otsuka Holdings Company Limited), University of Tokushima
• Original Assignee: Taiho Pharmaceutical Company Limited (Otsuka Holdings Company Limited), University of Tokushima
• Inventors: Doi, Yusuke, Ishida, Tatshiro
• Granted Patent: US 10,383,822 B2
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/282 Platinum compounds
• CPC Class Codes: A61K 31/555 containing heavy metals, e.g. hemin, hematin, melarsoprol
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61P 35/00 Antineoplastic agents

Abstract

An object of the present invention is to provide an oxaliplatin-encapsulating liposome aqueous dispersion that has excellent long-term storage stability. The present invention provides an aqueous dispersion of liposomes encapsulating oxaliplatin, the oxaliplatin-encapsulating liposome aqueous dispersion containing 2-morpholinoethanesulfonic acid in an external aqueous phase.

Claims

1. An oxaliplatin-encapsulating liposome aqueous dispersion comprising an external aqueous phase that contains 2-morpholinoethanesulfonic acid.

2. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, wherein the dispersion comprises an internal aqueous phase that substantially contains no 2-morpholinoethanesulfonic acid.

3. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, wherein the dispersion has a pH of 5 to 8.

4. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, wherein liposomes comprise at least one saturated phospholipid as a liposome component.

5. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, wherein the liposomes comprise as a liposome component at least one saturated phospholipid selected from the group consisting of hydrogenated purified soybean phosphatidylcholines, distearoylphosphatidylcholines, dipalmitoylphosphatidylcholines, and hydrogenated purified egg yolk phosphatidylcholines.

6. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, wherein the amount of 2-morpholinoethanesulfonic acid is 0.00001 to 10 parts by mass per part by mass of liposome-forming phospholipid.

9. An antitumor agent comprising the oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1.

10. A method for treating a cancer, comprising administering the oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1 to a mammal.

11. Use of the oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1 in the preparation of an antitumor agent.

12. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, which is for use in the treatment of a cancer.

13. An antitumor effect potentiator for enhancing antitumor activity of an antitumor agent, the potentiator comprising the oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1.

14. The method for treating a cancer according to claim 10, further comprising administering an antitumor agent to a mammal.

15. Use of the oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1 in the preparation of a potentiator for enhancing an effect of an antitumor agent.

16. The oxaliplatin-encapsulating liposome aqueous dispersion according to claim 1, which is for enhancing an effect of an antitumor agent.

7. A stabilizer for an oxaliplatin-encapsulating liposome aqueous dispersion containing 2-morpholinoethanesulfonic acid or a salt thereof as an active ingredient.

8. A method for stabilizing an oxaliplatin-encapsulating liposome aqueous dispersion, comprising adding 2-morpholinoethanesulfonic acid or a salt thereof to the oxaliplatin-encapsulating liposome aqueous dispersion.