METHODS AND RELATED COMPOSITIONS FOR REDUCTION OF FAT

• US 20110002896A1
• Filed: 05/18/2010
• Published: 01/06/2011
• Est. Priority Date: 05/19/2004
• Status: Abandoned Application

• Current Assignee: Los Angeles Biomedical Research Institute At Harbor-Ucla Medical Center (University of California), Regents of the University of California (University of California)
• Original Assignee: Habor UCLA Medical Center Incorporated (University of California), University of California Los Angeles (University of California)
• Inventors: Rotunda, Adam M., KOLODNEY, MICHAEL S.
• Application Number:
  US12/782,324
• Publication Number:
  US 20110002896A1
• Time in Patent Office: Days
• US Class Current: 424/93.7
• 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 2800/91 Injection
• CPC Class Codes: A61K 31/185 Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids hydroxamic acids A61K31/16; peroxy acids A61K31/327
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/685 one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
• CPC Class Codes: A61K 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 47/28 Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
• CPC Class Codes: A61K 8/63 Steroids; Derivatives thereof
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 21/02 Muscle relaxants, e.g. for tetanus or cramps
• CPC Class Codes: A61P 25/06 Antimigraine agents
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• 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 29/02 without antiinflammatory effect
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61Q 19/06 : for countering cellulitis
• CPC Class Codes: A61Q 19/08 : Anti-ageing preparations

Abstract

Compositions and methods useful in the reduction of localized fat deposits in patients in need thereof using pharmacologically active detergents are disclosed. The pharmacologically active detergent compositions can additionally include anti-inflammatory agents, analgesics, dispersion or anti-dispersion agents and pharmaceutically acceptable excipients. The pharmacologically active detergent compositions are useful for treating localized accumulations of fat including, for example, lower eyelid fat herniation, lipodystrophy and fat deposits associated with cellulite and do not require surgical procedures such as liposuction.

Claims

1-53. -53. (canceled)

54. A non-surgical method for improving the appearance of a human having a localized fat accumulation and desiring the removal thereof, said method comprises local administration to said fat accumulation a composition consisting essentially of a detergent and phosphatidylcholine, which detergent is deoxycholic acid, or a salt thereof, wherein said detergent reduces the localized fat accumulation thereby improving the appearance of said human, and wherein said detergent is contained in excess of phosphatidylcholine by mass.

56. The method of claim 54 or 55, wherein said fat accumulation is localized in an area selected from the group consisting of:

a thigh, the abdomen, the buttock, calf, an ankle, the upper back, the chin, an arm, the waist, and the hip.

59. The method of any one of claims 54, 57, and 58, wherein the concentration of the detergent is up to 5% (w/v) deoxycholic acid or the salt thereof.

60. The method of any one of claims 54, 57, and 58, wherein the concentration of the detergent is about 0.1%, 0.5%, or 1% (w/v) deoxycholic acid or the salt thereof.

61. The method of any one of claims 54, 57, and 58, wherein said salt is sodium salt.

62. The method of any one of claims 54, 57, and 58, wherein said local administration comprises subcutaneous injection.

63. The method of any one of claims 54, 57, and 58, wherein said composition further comprises a penetration enhancer.

64. The method of any one of claims 54, 57, and 58, wherein said composition further comprises hyaluronidase and/or collagenase.

65. The method of any one of claims 54, 57, and 58, wherein said composition further comprises an active ingredient which is not phosphatidylcholine.

66. The method of claim 65, wherein said active ingredient is an anti-inflammatory agent and/or an analgesic.

67. The method of claim 65, wherein said active agent is an analgesic.

68. The method of claim 67, wherein said analgesic is lidocaine.

69. The method of any one of claims 54, 57, and 58, wherein the ratio of the detergent to phosphatidylcholine is 1:

0.5.

70. The method of any one of claims 54, 57, and 58, wherein the ratio of the detergent to phosphatidylcholine is 1:

0.05.

71. The method of any one of claims 54, 57, and 58, wherein the ratio of the detergent to phosphatidylcholine is 1:

0.005.

55. A non-surgical method for improving the appearance of a human having a localized fat accumulation and desiring the removal thereof, said method comprises local administration to said fat accumulation a composition comprising a detergent and phosphatidylcholine, which detergent is deoxycholic acid, or a salt thereof, wherein said detergent reduces the localized fat accumulation thereby improving the appearance of said human, and wherein said detergent is contained in excess of phosphatidylcholine by mass.

57. A method for treating a patient having lipomas comprising local administration to said lipomas of said patient a composition consisting essentially of a detergent and phosphatidylcholine, which detergent is deoxycholic acid, or a salt thereof, wherein said detergent reduces the size of said lipomas thereby treating said patient, and wherein said detergent is contained in excess of phosphatidylcholine by mass.

58. A method for treating a patient having lipomas comprising local administration to said lipomas of said patient a composition comprising a detergent and phosphatidylcholine, which detergent is deoxycholic acid, or a salt thereof, wherein said detergent reduces the size of said lipomas thereby treating said patient, and wherein said detergent is contained in excess of phosphatidylcholine by mass.

72. A method for non-surgical removal of a localized fat deposit in a patient having such deposit and desiring to remove such deposit, which method comprises contacting the fat deposit with a composition comprising an effective amount of deoxycholic acid or a salt thereof, phosphatidylcholine and a pharmaceutically acceptable excipient, and wherein said deoxycholic acid or the salt thereof is contained in excess of phosphatidylcholine by mass.

73. A method for non-surgical removal of a localized fat deposit in a patient having such deposit and desiring to remove such deposit, which method comprises contacting the fat deposit with a composition consisting essentially of an effective amount of deoxycholic acid or a salt thereof, phosphatidylcholine and a pharmaceutically acceptable excipient, and wherein said deoxycholic acid or the salt thereof is contained in excess of phosphatidylcholine by mass.

74. A cosmetic method for non-surgical removal of a localized fat deposit in a patient having such deposit and desiring to remove such deposit, which method comprises contacting the fat deposit with a composition comprising an effective amount of deoxycholic acid or a salt thereof, phosphatidylcholine and a pharmaceutically acceptable excipient, and wherein said deoxycholic acid or the salt thereof is contained in excess of phosphatidylcholine by mass.

75. A cosmetic method for non-surgical removal of a localized fat deposit in a patient having such deposit and desiring to remove such deposit, which method comprises contacting the fat deposit with a composition consisting essentially of an effective amount of deoxycholic acid or a salt thereof, phosphatidylcholine and a pharmaceutically acceptable excipient, and wherein said deoxycholic acid or the salt thereof is contained in excess of phosphatidylcholine by mass.

76. A syringe for subcutaneous injection wherein said syringe comprises a sterile aqueous composition comprising a fat removing effective amount of up to 5% (w/v) of a detergent which is deoxycholic acid or a salt thereof, and phosphatidylcholine, wherein the detergent is contained in excess of phosphatidylcholine by mass.

77. The syringe of claim 76, further containing at least another active ingredient.

78. The syringe of claim 76, wherein the fat removing effective amount is from 0.05% to 5% (w/v).

79. The syringe of claim 76, wherein the detergent is the salt of deoxycholic acid.

80. The syringe of claim 76, wherein the salt is sodium deoxycholate.

81. A composition comprising an adipose cell and aqueous solution of a fat removing bile acid or a salt thereof at a concentration of no more than 5% (w/v) and phosphatidylcholine, wherein the bile acid or the salt thereof is contained in excess of phosphatidylcholine by mass.

82. The composition of claim 81, wherein the concentration of the bile acid or the salt is from 0.05% to 5% (w/v).

83. The composition of claim 82, wherein the bile acid is deoxycholic acid.

84. The composition of claim 82, wherein the bile acid salt is sodium deoxycholate.