Compositions and methods for treatment of pain

• US 20080132751A1
• Filed: 11/30/2006
• Published: 06/05/2008
• Est. Priority Date: 11/30/2006
• Status: Abandoned Application

• Current Assignee: Betazone Laboratories, Inc.
• Original Assignee: Betazone Laboratories, Inc.
• Inventors: Rey, Camilo, Useche, Jorge, Keller, Brian C.
• Application Number:
  US11/607,830
• Publication Number:
  US 20080132751A1
• Time in Patent Office: Days
• US Class Current: 600/26
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/196 the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/1271 Non-conventional liposomes, e.g. PEGylated liposomes, liposomes coated with polymers liposome as conjugate A61K47/6911

Abstract

The present invention provides compositions and methods for treating pain by the administration of analgesics. The analgesics are encapsulated in diacylglycerol-polyethyleneglycol (DAG-PEG) liposomes and delivered sublingually as aerosols.

Claims

1. A method of delivering an analgesic, the method comprising:

combining the analgesic with a DAG-PEG to produce a liposome suspension; and

administering the suspension sublingually.

2. The method of claim 1, where the suspension is delivered by means of an aerosol spray.

3. The method of claim 1, where the analgesic is chosen from the group comprising naproxen, ibuprofen and acetaminophen ketoprofen, diclofenac, hydrocodone, morphine, fentanyl, hydromorphone, methadone, meperidine, oxycodone, and levorphanol.

4. The method of claim 2, further comprising providing the liposome suspension in the reservoir of an aerosol deliverer.

5. The method of claim 1, where the DAG-PEG has a P.sub.a between about 0.84 and 0.88 and a P.sub.v between about 0.88 and 0.93 and where P.sub.a is the packing parameter with respect to surface and P.sub.v is the packing parameter with respect to volume.

6. The method of claim 5, where said combining occurs at a temperature above the melting point of the DAG-PEG.

7. The method of claim 1, where the PEG chain of the DAG-PEG has a molecular weight between about 300 Daltons and 5000 Daltons.

8. The method of claim 1, where the DAG-PEG is selected from the group consisting of PEG-12 glycerol dioleate (GDO), PEG-12 glycerol dimyristate (GDM), PEG-23 glycerol dipalmitate (GDP), PEG-12 glycerol distearate (GDS), and PEG-23 GDS, where the number after “

PEG”

indicates the numbers of C₂H₄O subunits in the PEG chain.

9. The method of claim 1, where the melting point of the DAG-PEG is below about 40 degrees C., and where the acyl chains of the DAG-PEG are greater than or equal to 14 carbons in length.

10. An aerosol delivery system comprising:

an aerosol deliverer;

a reservoir;

a liposomal suspension contained in the reservoir, such liposomal suspension comprising an analgesic and a DAG-PEG.

11. The system of claim 10, where the analgesic is chosen from the group comprising naproxen, ibuprofen and acetaminophen, ketoprofen, diclofenac, hydrocodone, morphine, fentanyl, hydromorphone, methadone, meperidine, oxycodone, and levorphanol.

12. The system of claim 10, where the DAG-PEG has a P.sub.a between about 0.84 and 0.88 and a P.sub.v between about 0.88 and 0.93 and where P.sub.a is the packing parameter with respect to surface and P.sub.v is the packing parameter with respect to volume.

13. The system of claim 10, where the PEG chain of the DAG-PEG has a molecular weight between about 300 Daltons and 5000 Daltons.

14. The system of claim 10, where the DAG-PEG is selected from the group consisting of PEG-12 glycerol dioleate (GDO), PEG-12 glycerol dimyristate (GDM), PEG-23 glycerol dipalmitate (GDP), PEG-12 glycerol distearate (GDS), and PEG-23 GDS, where the number after “

PEG”

indicates the numbers of C₂H₄O subunits in the PEG chain.

15. The system of claim 10, where the melting point of the DAG-PEG is below about 40 degrees C., and where the acyl chains of the DAG-PEG are greater than or equal to 14 carbons in length.

17. The suspension of claim 10, where the analgesic is chosen from the group comprising naproxen, ibuprofen and acetaminophen, ketoprofen, diclofenac, hydrocodone, morphine, fentanyl, hydromorphone, methadone, meperidine, oxycodone, and levorphanol.

18. The suspension of claim 10, where the DAG-PEG has a P.sub.a between about 0.84 and 0.88 and a P.sub.v between about 0.88 and 0.93 and where P.sub.a is the packing parameter with respect to surface and P.sub.v is the packing parameter with respect to volume.

19. The suspension of claim 10, where the PEG chain of the DAG-PEG has a molecular weight between about 300 Daltons and 5000 Daltons.

20. The suspension of claim 10, where the DAG-PEG is selected from the group consisting of PEG-12 glycerol dioleate (GDO), PEG-12 glycerol dimyristate (GDM), PEG-23 glycerol dipalmitate (GDP), PEG-12 glycerol distearate (GDS), and PEG-23 GDS, where the number after “

PEG”

indicates the numbers of C₂H₄O subunits in the PEG chain.

21. The suspension of claim 10, where the melting point of the DAG-PEG is below about 40 degrees C., and where the acyl chains of the DAG-PEG are greater than or equal to 14 carbons in length.

16. A liposomal suspension comprising:

a DAG-PEG; and

an analgesic.