Pharmaceutical formulation

• US 7,709,536 B2
• Filed: 09/16/2005
• Issued: 05/04/2010
• Est. Priority Date: 08/14/2002
• Status: Expired due to Term

• Current Assignee: GW Research Limited (Jazz Pharmaceuticals Plc)
• Original Assignee: GW Pharmaceuticals Limited (Jazz Pharmaceuticals Plc)
• Inventors: Whittle, Brian
• Primary Examiner(s): PRYOR, ALTON NATHANIEL
• Application Number:
  US11/229,052
• Publication Number:
  US 20060068034A1
• Time in Patent Office: 1,691 Days
• Field of Search: 424/725, 424/435
• US Class Current: 514/725
• CPC Class Codes: A61K 31/05 Phenols cannabinoids A61K31/658
• CPC Class Codes: A61K 31/352 condensed with carbocyclic rings, e.g. methantheline cannabinoids A61K31/658
• CPC Class Codes: A61K 36/185 Magnoliopsida (dicotyledons)
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants
• CPC Class Codes: A61P 25/14 for treating abnormal movements, e.g. chorea, dyskinesia
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/00 Drugs for disorders of the metabolism of the blood or the extracellular fluid A61P7/00
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: B65B 31/00 Packaging articles or materials under special atmospheric or gaseous conditions; Adding propellants to aerosol containers
• CPC Class Codes: B65D 65/38 Packaging materials of special type or form

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

1. A liquid pharmaceutical formulation, for use in the administration of a lipophilic medicament via a mucosal surface, comprising:

at least one lipophilic medicament, a solvent and 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 formulation has a water content of less than 5% and the formulation is packaged for delivery as a spray, wherein the lipophilic medicament comprises tetrahydrocannabinol (THC) and cannabidiol (CBD), wherein the lipophilic medicament is at least one extract from at least one cannabis plant, and wherein the extract from at least one cannabis plant is a botanical drug substance.

2. A liquid pharmaceutical formulation as claimed in claim 1, wherein the botanical drug substance is a CO₂ extract of one or more cannabis plants.

3. A liquid pharmaceutical formulation as claimed in claim 1, wherein the THC and CBD are present in a ratio (w/w) of from 0.9:

1.1 to 1.1;

0.9.

7. A liquid pharmaceutical formulation as claimed in either claim 1 or claim 4, which is packaged for delivery as a spray having a mean aerodynamic particle size, when delivered, of from 20-40 microns.

8. A liquid pharmaceutical formulation as claimed in either claim 1 or claim 4, which is packaged for delivery as a pump-action spray, and wherein the formulation is dispensed through a mechanical pump, wherein the mechanical pump comprises a VP7 actuator valve.

9. A liquid pharmaceutical formulation as claimed in claim 7, which is packaged for delivery as a spray having a mean aerodynamic particle size, when delivered, of from 25-35 microns.

10. A liquid pharmaceutical formulation as claimed in claim 9, which is packaged for delivery as a spray having a mean aerodynamic particle size, when delivered, of from 30-35 microns.

4. A liquid pharmaceutical formulation comprising in a 1 ml vol:

tetrahydrocannabinol (THC) 25-27 mg/ml based on amount of cannabinoid in a botanical drug substance, cannabidiol (CBD) 25 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 wherein the formulation has a water content less than 5%.

5. A liquid pharmaceutical formulation as claimed in claim 4, wherein the THC and CBD form part of at least one extract from at least one cannabis plant, said at least one extract comprising all the naturally occurring cannabinoids in said plant.

6. A liquid pharmaceutical formulation as claimed in claim 5, wherein the at least one extract is prepared by supercritical or subcritical fluid extraction of dried cannabis plant.