# US 9,040,487 B2 · Cyclosporine emulsion

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- Number: US 9,040,487 B2
- Document ID: US9040487B2
- Status: Granted
- Kind: B2
- Application number: 13/877,326
- Filed: 2011-09-30
- Published: 2013-12-05
- Granted: 2015-05-26
- Earliest claimed: 2010-10-01
- Assignees: Neurovive Pharmaceutical AB
- Applicants: Eskil Elmér
- Inventors: Eskil Elmér
- Web page: https://patentgrep.com/patent/US9040487B2

## CPC

- A61K 38/13: Cyclosporins
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/12: Carboxylic acids; Salts or anhydrides thereof
- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 47/24: containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
- 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)
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 13/12: of the kidneys
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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

### Claim 4 (depends on 1)

The cyclosporine emulsion of claim 1, further comprising: hydrochloric acid or sodium hydroxide for pH adjustment.