Emulsions or microemulsions for use in endoscopic mucosal resectioning and/or endoscopic submucosal dissection

Patent metadata

Field	Value
Publication number	US-9962445-B2
Application number	US-201615334496-A
Country	US
Kind code	B2
Filing date	Oct 26, 2016
Priority date	Nov 20, 2013
Publication date	May 8, 2018
Grant date	May 8, 2018

Abstract

The present invention relates to a pharmaceutical composition in form of emulsion or microemulsion and the use thereof as aid during endoscopic procedures in which it is injected in a target tissue in order to form a cushion. More in details, the invention relates to a method for performing an endoscopic procedure, which comprises injecting said pharmaceutical composition in form of emulsion or microemulsion in a target tissue of a patient, in order to form a cushion, which cushion is then optionally subjected to an endoscopic surgical procedure, such as a resection.

First claim

The invention claimed is:

1. A pharmaceutical composition in the form of an emulsion or a microemulsion comprising:
(a) an aqueous phase;
(b) an oily phase;
(c) at least one surfactant; and
(d) at least one inverse thermosensitive polymer selected from poloxamer 124, poloxamer 188, poloxamer 237, poloxamer 338, poloxamer 407 and mixtures thereof;
wherein said at least one inverse thermosensitive polymer is present in an amount below the critical gelation concentration (CGC), and wherein said composition remains in liquid phase up to a temperature of about 40° C. in vitro.

2. The pharmaceutical composition according to claim 1 , wherein said composition has a viscosity below about 150 cP (centipoises).

3. The pharmaceutical composition according to claim 1 , wherein said at least one inverse thermosensitive polymer is present in an amount below about 15% by weight, with respect to the weight of the composition.

4. The pharmaceutical composition according to claim 3 , wherein said at least one inverse thermosensitive polymer is present in an amount between about 2% and about 14.5% by weight, with respect to the weight of the composition.

5. The pharmaceutical composition according to claim 4 wherein said at least one inverse thermosensitive polymer is present in an amount between about 5% and about 11% by weight, with respect to the weight of the composition.

6. The pharmaceutical composition according to claim 1 , wherein said at least one poloxamer is poloxamer 188, poloxamer 407 or mixtures thereof.

7. The pharmaceutical composition according to claim 1 , wherein said oily phase comprises at least one lipophilic compound.

8. The pharmaceutical composition according to claim 7 , wherein said at least one lipophilic compound is a medium-chain triglycerides, soybean oil, sesame oil or almond oil.

9. The pharmaceutical composition according to claim 1 , wherein said at least one surfactant is at least one non-ionic surfactant.

10. The pharmaceutical composition according to claim 9 , wherein said at least one non-ionic surfactant is polysorbate 80 or polyoxyl-15-hydroxystearate.

11. The pharmaceutical composition according to claim 1 , wherein said at least one surfactant is at least one ionic surfactant.

12. The pharmaceutical composition according to claim 11 , wherein said at least one ionic surfactant is egg lecithin, hydrogenated phosphatidyl choline from egg lecithin, soybean lecithin or hydrogenated soybean lecithin.

13. The pharmaceutical composition according to claim 1 , further comprising at least one co-surfactant wherein said at least one co-surfactant is propylene glycol, glycerol or sodium oleate.

14. The pharmaceutical composition according to claim 1 , further comprising at least one dye wherein said at least one dye is a vital dye, a non-vital dye or a reactive dye.

15. The pharmaceutical composition according to claim 14 , wherein said at least one dye is Lugol's solution, methylene blue, toluidine blue, crystal violet, indigo carmine, Congo red or phenol red.

16. The pharmaceutical composition according to claim 15 , wherein said at least one dye is methylene blue.

17. A pharmaceutical composition in the form of an emulsion or a microemulsion comprising:
(a) an aqueous phase;
(b) an oily phase comprising medium-chain triglycerides;
(c) a surfactant comprising polyoxyl-15-hydroxystearate;
(d) an inverse thermosensitive polymer comprising poloxamer 188; and
(e) methylene blue;
wherein said poloxamer 188 is present in an amount below the critical gelation concentration (CGC), and wherein said composition remains in liquid phase up to a temperature of about 40° C. in vitro.

18. The pharmaceutical composition according to claim 17 , which further comprises sodium chloride.

19. The pharmaceutical composition according to claim 17 , wherein the composition comprises in w/v about 0.02% to about 1.0% of medium-chain triglycerides, about 0.08% to about 4% polyoxyl-15-hydroxystearate, about 5% to about 11% poloxamer 188, about 0.0005% to about 0.01% methylene blue and the remainder being water.

20. The pharmaceutical composition according to claim 18 , wherein the composition comprises in w/v about 0.02% to about 1.0% of medium-chain triglycerides, about 0.08% to about 4% polyoxyl-15-hydroxystearate, about 5% to about 11% poloxamer 188, about 0.0005% to about 0.01% methylene blue, about 0.44% to about 0.5% sodium chloride and the remainder being water.

Assignees

• Cosmo Technologies Ltd

Inventors

• Moro Luigi
• Longo Luigi Maria
• Frimonti Enrico
• Repici Alessandro

Classifications

• A61P41/00

  Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution · CPC title

• A61L31/06

  obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds {(A61L31/041 takes precedence)} · CPC title

• A61K9/0019 Primary

  Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00) · CPC title

• A61L24/0005

  Ingredients of undetermined constitution or reaction products thereof · CPC title

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title