Composition comprising EPA and DHA ethylester for parenteral administration

Patent metadata

Field	Value
Publication number	US-9801846-B2
Application number	US-201515114937-A
Country	US
Kind code	B2
Filing date	Jan 28, 2015
Priority date	Jan 28, 2014
Publication date	Oct 31, 2017
Grant date	Oct 31, 2017

Abstract

Described herein are compositions for parenteral administration that include an aqueous phase and 5 to 30%, by weight, of an oil phase, based on the total weight of the composition. The oil phase comprises the omega-3 fatty acid ethylesters eicosapentaenoic acid ethylester, docosahexaenoic acid ethylester, and mixtures thereof. The composition further comprises at least one anionic surfactant and at least one amphoteric surfactant, and less than 0.05% by weight of oleic acid, based on the total weight of the composition. Also described is a method for preparing such a composition as well as such compositions for use as a medicament, in particular for use in treating stroke, sepsis, Alzheimer's disease or cancer. Also featured are methods of treating these conditions by parenterally administering a composition to a patient in need thereof and methods of providing parenteral nutrition to such patients by administering to them a composition as described herein.

First claim

The invention claimed is:

1. A composition comprising
an aqueous phase and 5 to 30% by weight of an oil phase, based on the total weight of the composition, wherein the oil phase comprises eicosapentaenoic acid ethylester, docosahexaenoic acid ethylester or mixtures thereof and less than 1% by weight medium chain triglycerides, based on the total weight of the composition;
an anionic surfactant; and
an amphoteric surfactant, wherein the composition is formulated for parenteral administration and comprises less than 0.05% by weight of oleic acid, based on the total weight of the composition.

2. The composition of claim 1 , wherein at least 60% by weight of the oil phase consists of eicosapentaenoic acid ethylester, docosahexaenoic acid ethylester or mixtures thereof.

3. The composition of claim 1 , wherein the oil phase comprises a mixture of eicosapentaenoic acid ethylester and docosahexaenoic acid ethylester and wherein the weight ratio of the eicosapentaenoic acid ethylester to the docosahexaenoic acid ethylester is in the range of from 1 to 9 to 9 to 1.

4. The composition of claim 1 , further comprising an agent with antioxidant activity.

5. The composition of claim 1 , wherein the amphoteric surfactant is lecithin.

6. The composition of claim 1 , wherein the anionic surfactant is sodium oleate.

7. The composition of claim 1 , wherein the composition further comprises a tonicity agent.

8. The composition of claim 1 , wherein the composition comprises in sum less than 1% by weigh of polyethylene glycol and propylene glycol, based on the total weight of the composition.

9. The composition of claim 1 , wherein the composition comprises less than 0.01% by weight oleic acid.

10. A method for preparing a composition, wherein the method comprises:
(a) providing an aqueous phase comprising an amphoteric surfactant and an anionic surfactant,
(b) providing an oil phase comprising eicosapentaenoic acid ethylester, docosahexaenoic acid ethylester or mixtures thereof, and
(c) mixing the oil phase according to (b) with the aqueous phase according to (a), wherein the oil phase constitutes 5 to 30% by weight of the total composition, and the composition comprises less than 1% by weight medium chain triglycerides and less than 0.05% by weight oleic acid.

11. The method of claim 10 , further comprising
(d) homogenizing the mixture obtained from step (c) at a temperature in the range of from 50 to 60° C. and at a pressure in the range of from 450 to 550 bar.

12. The method of claim 11 , further comprising
(e) autoclaving the mixture obtained from step (c) or step (d) at a temperature in the range of from 119° C. to 122° C. for a time in the range of from 10 min to 15 min.

13. A composition obtained by the method of claim 10 .

14. A method of providing parenteral nutrition to a patient suffering from stroke, sepsis, Alzheimer's disease or cancer, the method comprising parenterally administering to the patient an effective amount of the composition of claim 1 .

15. An infusion bag comprising the composition of claim 1 .

16. The composition of claim 4 , wherein the agent with antioxidant activity is alpha-tocopherol, beta-tocopherol, gamma-tocopherol, ascorbic acid, ascorbic acid palmitate, or an antioxidant obtained or obtainable from rosemary or rosemary extract.

17. The composition of claim 7 , wherein the tonicity agent is glycerol.

Assignees

• Fresenius Kabi Deutschland Gmbh
• Fresenius Kabi Deutchland Gmbh

Inventors

• Brito De La Fuente Edmundo
• Gallegos-Montes Crispulo
• Quinchia-Bustamente Lida A

Classifications

• A61K9/107

  Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)} · CPC title

• A61K47/24

  containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids · CPC title

• A61K47/12

  Carboxylic acids; Salts or anhydrides thereof · CPC title

• A61K9/0029 Primary

  Parenteral nutrition; Parenteral nutrition compositions as drug carriers · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title