Cyclosporine emulsion

• US 9,040,487 B2
• Filed: 09/30/2011
• Issued: 05/26/2015
• Est. Priority Date: 10/01/2010
• Status: Active Grant

• Current Assignee: Abliva AB
• Original Assignee: NeuroVive Pharmaceutical AB
• Inventors: Elmr, Eskil
• Primary Examiner(s): Ha, Julie
• Assistant Examiner(s): KOMATSU, LI N
• Application Number:
  US13/877,326
• Publication Number:
  US 20130323270A1
• Time in Patent Office: 1,334 Days
• Field of Search: None
• US Class Current: 514/20.5
• CPC Class Codes: A61K 38/13 Cyclosporins
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• 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 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 13/12 of the kidneys
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 37/06 Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• 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

Abstract

The present invention relates to a cyclosporine emulsion containing: i) a cyclosporine ii) a natural oil (long chain triglyceride) iii) a phosphatidylcholine, iv) glycerol, v) a pharmaceutically tolerable alkali salt of a free fatty acid, vi) a medium chain triglyceride-oil vii) optionally, hydrochloric acid or sodium hydroxide for pH adjustment viii) water.

Claims

1. A cyclosporine oil-in-water emulsion comprising

i) 5 g/L cyclosporine,

ii) 100 g/L soya bean oil,

iii) 12 g/L egg lecithin,

iv) 25 g/L water-free glycerol,

v) 0.3 g/L sodium oleate,

vi) 100 g/L medium chain triglyceride-oil selected from the group consisting of coconut oil, palm oil, and combinations thereof, and

vii) water for injection,

wherein the emulsion is isoosmolar and has an osmolarity of from 280 to 305 mosm/l, and

wherein the composition does not contain polyethoxylated castor oil.

2. The cyclosporine emulsion according to claim 1 having an osmolarity of from about 295 to about 300 mosm/1.

3. The emulsion according to claim 1, wherein pH of the emulsion is from about 6 to about 8.8.

4. The cyclosporine emulsion of claim 1, further comprising:

hydrochloric acid or sodium hydroxide for pH adjustment.