COMPOSITIONS AND METHODS FOR DELIVERY OF POORLY SOLUBLE DRUGS

• US 20130129828A1
• Filed: 01/15/2013
• Published: 05/23/2013
• Est. Priority Date: 09/03/2007
• Status: Active Grant

• Current Assignee: Nanoshift, LLC
• Original Assignee: Nanotherapeutics, Inc. (National Resilience, Inc.)
• Inventors: Talton, James David
• Granted Patent: US 9,554,996 B2
• Time in Patent Office: Days
• US Class Current: 424/490
• 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 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61K 9/146 with organic macromolecular compounds
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: A61K 9/5021 Organic macromolecular compounds
• CPC Class Codes: A61K 9/5026 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/5089 Processes
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 25/30 for treating abuse or dependence
• CPC Class Codes: A61P 25/36 Opioid-abuse

Abstract

Described herein are compositions comprising particles of poorly soluble drugs encapsulated by stabilizers. Further described are pharmaceutical compositions comprising such encapsulated compositions. Also described are methods of making such encapsulated particle compositions, and methods of making the corresponding pharmaceutical compositions. The encapsulated particle compositions described herein allow poorly soluble drugs to be administered with good bioavailability by routes that are non-invasive to patients, such as by oral administration.

Claims

1-53. -53. (canceled)

54. A particle delivery system (PDS) comprising dry particles having an average diameter of less than about 2 mm, wherein the dry particles comprise a poorly soluble drug and polyethylene glycol (PEG), wherein

the amount of the poorly soluble drug present in the dry particles ranges from about 0.2% to about 4% by mass of the dry particles,

the poorly soluble drug is encapsulated by the PEG, and

the poorly soluble drug comprises at least one opioid selected from codeine, fentanyl, hydrocodone, hydromorphone, morphine, methylnaltrexone, nalbuphine, nalmefene, oxymorphone, oxycodone, pethidine, tramadol, and combinations or mixtures thereof.

55. The composition of claim 54, wherein the PEG has an average molecular weight ranging from about 100 Daltons to about 100,000 Daltons.

56. The PDS of claim 55, wherein the PEG is PEG 3350.

57. The PDS of claim 54, further comprising a surfactant.

58. The PDS of claim 57, wherein the surfactant is a nonionic surfactant.

59. A pharmaceutical composition comprising the PDS of claim 54 and at least one second compound.

60. The pharmaceutical composition of claim 59, wherein the composition is formulated for oral administration.

61. The pharmaceutical composition of claim 59, wherein the at least one second compound is a drug chosen from opioid receptor antagonists, anti-inflammatory drugs, analgesics, and combinations or mixtures thereof.

62. The pharmaceutical composition of claim 61, wherein the drug comprises an opioid receptor antagonist.

63. The pharmaceutical composition of claim 62, wherein the drug comprises naloxone or a pharmaceutically acceptable salt thereof.

64. The pharmaceutical composition of claim 63, wherein the naloxone salt is naloxone HCl.