O/W-EMULSIONS COMPRISING SEMIFLUORINATED ALKANES

• US 20140004197A1
• Filed: 01/03/2012
• Published: 01/02/2014
• Est. Priority Date: 01/04/2011
• Status: Abandoned Application

• Current Assignee: Novaliq GmbH
• Original Assignee: Bernhard Gunther
• Inventors: Theisinger, Bastian, Theisinger, Sonja, Gnther, Bernhard
• Application Number:
  US13/978,334
• Publication Number:
  US 20140004197A1
• Time in Patent Office: Days
• US Class Current: 424/489
• CPC Class Codes: A61K 31/05 Phenols cannabinoids A61K31/658
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61K 9/0019 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 Class Codes: A61K 9/0026 Blood substitute; Oxygen transporting formulations; Plasma extender
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives

Abstract

The invention provides liquid compositions in the form of physically stable emulsions comprising a semifluorinated alkane. The semifluorinated alkane is comprised in the dispersed phase, which may also include an active pharmaceutical ingredient. One of the preferred active ingredients is propofol. The compositions are optionally heat sterilisable and can be used for pharmaceutical or cosmetic product applications, and administered topically, intravenously, or via other routes.

Claims

1. A liquid composition in the form of a physically stable O/W-emulsion comprising:

(a) a dispersed phase comprising a semifluorinated alkane according to formula

RFRH

or

RFRHRF;

(b) an aqueous continuous phase, and

(c) at least one surfactant;

wherein;

RF is a perfluorinated hydrocarbon segment with 20 or less carbon atoms,

RH is a non-fluorinated hydrocarbon segment with 3 to 20 carbon atoms, wherein perfluorinated compounds are absent in the dispersed phase, and wherein the average droplet size of the dispersed phase is below about 1 μ

m.

3. The composition of claim 1, wherein the semifluorinated alkane is selected from F4H5, F4H6, F4H8, F6H6 and F6H8.

4. The composition of claim 3, further characterised in that it is sterile and/or heat sterilisable.

5. The composition of claim 1, comprising a nonionic surfactant, further characterised in that the aqueous continuous phase comprises a salt or ionic compound.

6. The composition of claim 1, comprising an ionic surfactant, further characterised in that the aqueous continuous phase comprises a physiologically acceptable, nonionic osmotic agent.

7. The composition of claim 1, wherein the continuous aqueous phase comprises a compound selected from buffers and amino acids.

8. The composition of claim 1, wherein the dispersed phase comprises an active pharmaceutical ingredient.

9. The composition of claim 8, wherein the active pharmaceutical ingredient is propofol.

10. The composition of claim 9, wherein the concentration of propofol in the dispersed phase is at least about 10 wt.-%.

11. A method for the induction and/or maintenance of anaesthesia, or for sedation, wherein the method comprises the parenteral administration of the composition of claim 9 to a patient in need thereof.

12. The composition of claim 1, wherein the dispersed phase represents at least about 50 wt.-% of the emulsion.

13. A method of treatment of a patient suffering from a disease or condition said method comprising the administration of the composition of claim 1.

14. The method of treatment according to claim 13, wherein the composition is topically administered.

15. A method of preserving and/or storing and/or transporting an organ transplant, said method comprising the use of the composition of claim 1 as a medium.

16. The composition of claim 3, wherein the dispersed phase further comprises propofol and wherein the surfactant is selected from lecithins, phosphatidylcholines, polysorbates and poloxamers.

17. The composition of claim 16, further characterised in that the aqueous continuous phase comprises a physiologically acceptable, nonionic osmotic agent.

18. The composition of claim 16, further characterized in that it is sterile and/or heat sterilisable.

19. A method for the induction and/or maintenance of anaesthesia, or for sedation, wherein the method comprises the parenteral administration of the composition of claim 10 to a patient in need thereof.

2. A liquid composition in the form of a physically stable O/W-emulsion comprising:

(a) a dispersed phase comprising a semifluorinated alkane according to formula

RFRH;

(b) an aqueous continuous phase, and

(c) at least one surfactant;

wherein;

RF is a linear perfluorinated hydrocarbon segment with 4 to 12 carbon atoms,

RH is a linear alkyl group with 4 to 8 carbon atoms, and wherein the average droplet size of the dispersed phase is below about 1 μ

m.