PHARMACEUTICAL COMPOSITION COMPRISING PROPOFOL

• US 20120238639A1
• Filed: 11/22/2010
• Published: 09/20/2012
• Est. Priority Date: 11/23/2009
• Status: Active Grant

• Current Assignee: Novaliq GmbH
• Original Assignee: Novaliq GmbH
• Inventors: Theisinger, Bastian, Theisinger, Sonja
• Granted Patent: US 8,796,340 B2
• Time in Patent Office: Days
• US Class Current: 514/731
• 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 31/05 Phenols cannabinoids A61K31/658
• CPC Class Codes: A61P 1/08 for nausea, cinetosis or vertigo; Antiemetics
• CPC Class Codes: A61P 23/00 Anaesthetics
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives

Abstract

The invention provides novel pharmaceutical compositions comprising the active ingredient propofol. Preferably, propofol is dissolved in at least one semifluorinated alkane. The compositions, which are preferably liquid or gel-like, may optionally comprise further excipients. They may be used as fill material in capsules, as buccal or nasal sprays, or as aerosols for pulmonary administration. They are particularly useful for the transmucosal administration of propofol.

Claims

1. A pharmaceutical composition comprising a therapeutically effective amount of propofol and a semifluorinated alkane.

2. The composition of claim 1, wherein the semifluorinated alkane is a compound of formula

RFRH

or of formula

RFRHRF

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

wherein RH is a non-fluorinated hydrocarbon segment with 3 to 20 carbon atoms.

3. The composition of claim 2, wherein the semifluorinated alkane is a compound of formula

RFRH

wherein RF is a linear perfluorinated hydrocarbon segment with 3 to 10 carbon atoms, and

wherein RH is a linear alkyl group with 3 to 10 carbon atoms.

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

5. The composition of any preceding claim, wherein the concentration of propofol is about 1 wt.-% or higher.

6. The composition of any preceding claim, wherein essentially all of the propofol comprised therein is in dissolved form.

7. The composition of any preceding claim, being in the form of a liquid or a gel.

8. The composition of any preceding claim, being substantially free of lipids such as trigylcerides or phospholipids.

9. A pharmaceutical dosage form comprising the composition of claim 1.

10. The dosage form of claim 9, being selected from a soft capsule or an oral spray, a nasal spray, an inhalable aerosol, an oral gel, and an oral liquid.

11. A pharmaceutical kit comprising a container and therein the composition of claim 1, wherein the container comprises a means for atomising the composition.

12. The use of the composition of claim 1 as a medicine.

13. The use of claim 12, wherein the medicine is for oral, oromucosal or nasal administration.

14. The use of claim 12, wherein the medicine is for inducing anaesthesia, sedation, for neuroprotection in brain injury, or for the treatment of migraine headache or nausea.

15. The use of the composition of claim 1 as a veterinary medicament.

16. The use of the dosage form of claim 9 as a medicine.

17. The use of the dosage form of claim 9 as a veterinary medicament