IP Library Granted Patent US 8,211,946
Granted Patent B2
US 8,211,946 · App. 12/704,729 · Granted Jul 3, 2012

Pharmaceutical formulation

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Quick Facts
Patent No.
US 8,211,946
App. No.
12/704,729
Granted
Jul 3, 2012
Kind
B2
Abstract

The invention relates to pharmaceutical formulations, and more particularly to formulations containing cannabinoids for administration via a pump action spray. In particular, the invention relates to pharmaceutical formulations, for use in administration of lipophilic medicaments via mucosal surfaces, comprising: at least one lipophilic medicament, a solvent and a co-solvent, wherein the total amount of solvent and co-solvent present in the formulation is greater than 55% wt/wt of the formulation and the formulation is absent of a self emulsifying agent and/or a fluorinated propellant.

Claims (31)

1. A liquid pharmaceutical formulation, for use in administration of a cannabinoid medicament via a mucosal surface, comprising: one or more cannabinoids, a solvent and a co-solvent, wherein the total amount of solvent and co-solvent present in the formulation is greater than 55% wt/wt of the formulation, the formulation is absent of a self emulsifying agent and a fluorinated propellant and the one or more cannabinoids are present in the formulation in an amount at least 10 mg/ml.

2. A liquid pharmaceutical formulation as claimed in claim 1 wherein the one or more cannabinoids are present in the formulation in an amount of at least 25 mg/ml.

3. A liquid pharmaceutical formulation as claimed in claim 1 wherein solvent is selected from C1-C4 alcohols.

4. A liquid pharmaceutical formulation as claimed in claim 3 wherein the solvent is ethanol.

5. A liquid pharmaceutical formulation as claimed in claim 1 wherein the co-solvent is selected from glycols, sugar alcohols, carbonate esters and chlorinated hydrocarbons.

6. A liquid pharmaceutical formulation as claimed in claim 5 wherein the glycols are selected from propylene glycol and glycerol, and the carbonate ester is propylene carbonate.

7. A liquid pharmaceutical formulation as claimed in claim 1 wherein the co-solvent is propylene glycol.

8. A liquid pharmaceutical formulation as claimed in claim 1 wherein the solvent is ethanol and the co-solvent is propylene glycol.

9. A liquid pharmaceutical formulation as claimed in claim 8 wherein ethanol/propylene glycol are present in relative proportions by weight in the range 60/40 to 40/60.

10. A liquid pharmaceutical formulation as claimed in claim 8 wherein ethanol/propylene glycol are present in relative proportions by weight in the range 55/45 to 45/55.

11. A liquid pharmaceutical formulation as claimed in claim 8 wherein ethanol/propylene glycol are present in the relative proportions by weight of about 50/50.

12. A liquid pharmaceutical formulation as claimed in claim 1 which further comprises a flavouring.

13. A liquid pharmaceutical formulation as claimed in claim 12 wherein the flavouring is peppermint oil.

14. A liquid pharmaceutical formulation as claimed in claim 12 wherein the flavouring is present in an amount up to 0.1% v/v.

15. A liquid pharmaceutical formulation as claimed in claim 1 wherein the one or more cannabinoids are present in the formulation in an amount of at least 50 mg/ml.

16. A liquid pharmaceutical formulation as claimed in claim 1 wherein the cannabinoids medicament is at least one extract from at least one cannabis plant.

17. A liquid pharmaceutical formulation as claimed in claim 16 wherein the extract from at least one cannabis plant is a botanical drug substance.

18. A liquid pharmaceutical formulation as claimed in claim 16 wherein the extract, which is a botanical drug substance, has undergone an extraction step to remove a substantial proportion of waxes and other solvent insoluble materials present in extract.

19. A liquid pharmaceutical formulation as claimed in claim 16 wherein the extract, which is a botanical drug substance, is a CO 2 extract of one or more cannabis plants.

20. A liquid pharmaceutical formulation as claimed in claim 1 , wherein the cannabinoid medicament comprises one or more of: (THC), including Δ 9 -tetrahydrocannabinol, Δ 9 -tetrahydrocannabinol propyl analogue, cannabidiol (CBD), cannabidiol propyl analogue, cannabinol, cannabichromene, cannabichromene propyl analogue, cannabigerol or any mixture thereof.

21. A liquid pharmaceutical formulation as claimed in claim 20 wherein the cannabinoids include tetrahydrocannabinol (THC) and cannabidiol (CBD).

22. A liquid pharmaceutical formulation as claimed in claim 20 wherein THC and CBD are present in a ratio (w/w) of from 0.9:1.1 to 1.1:0.9.

23. A liquid pharmaceutical formulation as claimed in claim 20 which formulation includes from 22.5 to 27.5 mg/ml tetrahydrocannabinol (THC) and from 22.5 to 27.5 mg/ml cannabidiol (CBD).

24. A liquid pharmaceutical formulation as claimed in claim 1 which comprises both the cannabinoids cannabidiol (CBD) and tetrahydrocannabinol (THC), or the cannabinoids tetrahydrocannabinovarin (THCV) and cannabidivarin (CBDV), in a pre-defined ratio by weight.

25. A liquid pharmaceutical formulation as claimed in claim 1 , wherein the at least one extract is prepared by supercritical or sub-critical fluid extraction of dried Cannabis plant.

26. A liquid pharmaceutical formulations as claimed in claim 1 which is packaged for delivery as a pump-action spray, and wherein, in use, a dose is discharged through a break-up button.

27. A liquid pharmaceutical formulation as claimed in claim 1 , which comprises an extract from a high tetrahydrocannabinol (THC) yielding cannabis plant and an extract from a high cannabidiol (CBD) yielding cannabis plant and wherein said extracts each comprise all naturally occurring cannabinoids in said plants.

28. A liquid pharmaceutical formulation comprising in a 1 ml vol: THC 25-50 mg/ml based on amount of cannabinoid in a botanical drug substance, CBD 25-50 mg/ml based on amount of cannabinoid in a botanical drug substance, propylene glycol 0.5 ml/ml, peppermint oil 0.0005 ml/ml, and anhydrous ethanol qs to 1 ml.

29. A liquid pharmaceutical formulation comprising in a 1 ml vol: THC 25-50 mg/ml based on amount of cannabinoid in a botanical drug substance, propylene glycol 0.5 ml/ml, peppermint oil 0.0005 ml/ml, and anhydrous ethanol qs to 1 ml.

30. A liquid pharmaceutical formulation comprising in a 1 ml vol: CBD 25-50 mg/ml based on amount of cannabinoid in a botanical drug substance, propylene glycol 0.5 ml/ml, peppermint oil 0.0005 ml/ml, and anhydrous ethanol qs to 1 ml.

31. A liquid pharmaceutical formulation comprising in a 1 ml volume: THC 22.5-27.5 mg/ml based on amount of cannabinoid in a botanical drug substance, CBD 22.5-27.5 mg/ml based on amount of cannabinoid in a botanical drug substance, propylene glycol 0.5 ml/ml, peppermint oil 0.0005 ml/ml, and anhydrous ethanol qs to 1 ml.

Assignments (3)
SECURITY AGREEMENT Recorded Jul 22, 2021
From: GW PHARMA LIMITED; GW RESEARCH LIMITED
To: U.S. BANK NATIONAL ASSOCIATION
Reel/Frame 056958/0493 →
DEED OF ASSIGNMENT OF INTELLECTUAL PROPERTY RIGHTS Recorded Feb 4, 2021
From: GW PHARMA LIMITED
To: GW RESEARCH LIMITED
Reel/Frame 055222/0457 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 13, 2010
From: WHITTLE, BRIAN
To: GW PHARMA LIMITED
Reel/Frame 024223/0568 →