# US 11,298,314 B2 · Injectable composition for localized fat reduction without pain, edema, and side effects, and method for preparing same

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- Number: US 11,298,314 B2
- Document ID: US11298314B2
- Status: Granted
- Kind: B2
- Application number: 16/311,960
- Filed: 2018-04-20
- Published: 2019-07-04
- Granted: 2022-04-12
- Earliest claimed: 2017-04-21
- Assignees: AMI Pharm Co., Ltd.
- Applicants: Ami Pharm Co., Ltd.
- Inventors: Ki Taek Lee
- Web page: https://patentgrep.com/patent/US11298314B2

## CPC

- 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)}
- A61K 31/575: substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
- A61K 31/685: one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/28: Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
- A61P 3/04: Anorexiants; Antiobesity agents
- 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 composition comprising glycocholic acid or taurocholic acid and phosphatidylcholine at a particular mixing ratio for reducing localized fat without side effects such as a pain, edema, necrosis of muscle cells, fibroblasts and vascular endothelial cells other than adipocytes, anesthesia of administration sites, extensive swelling, erythema, induration, paresthesia, nodule, pruritus, burning sensation, nerve injury, and dysphagia, and a method for preparing the same. The inventor has found that the effect of PPC injectable composition on fat reduction may be reduced or enhanced during its subcutaneous administration, depending on the types of solubilizing agents, especially the types of bile acids, which are combined so as to prepare a safe and stable PPC injection using insoluble PPC. The PPC injectable composition solubilized with GCA or TCA selectively reduces adipocytes without inducing necrosis of fibroblasts, muscle cells and vascular endothelial cells, thereby alleviating the known clinical side effects.

## Claims

### Claim 1

A method for removing localized fat deposition with a reduced pain and side effect in a subject, the method comprising administering an effective amount of a composition or preparation consisting essentially of phosphatidylcholine; and at least one solubilizing agent of phosphatidylcholine selected from the group consisting of glycocholic acid, taurocholic acid and salt thereof to the subject having localized fat deposition, wherein a molar ratio of the solubilizing agent of phosphatidylcholine to the phosphatidylcholine in the composition or preparation is in a range of 0.7 to 3.0, and wherein the phosphatidylcholine is contained in the composition or preparation in a concentration of 0.3125 to 10% (w/v).

### Claim 2 (depends on 1)

The method of claim 1, wherein the localized fat deposition is non-surgically removed.

### Claim 3 (depends on 1)

The method of claim 1, wherein the side effect is at least one selected from the group consisting of edema; necrosis of muscle cells, fibroblasts and vascular endothelial cells other than adipocytes; anesthesia of administration sites;
extensive swelling; erythema; induration; paresthesia; nodule; pruritus; burning sensation; nerve injury; and dysphagia.

### Claim 4 (depends on 1)

The method of claim 1, wherein the step of administration comprises a subcutaneous injection.

### Claim 5

A method for non-surgically removing localized fat deposition with a reduced pain and side effect in a subject having localized fat deposition, the method comprising administering a composition or preparation consisting essentially of (i) phosphatidylcholine; and (ii) at least one selected from the group consisting of glycocholic acid, taurocholic acid and salt thereof to the subject having localized fat deposition, wherein a molar ratio of (ii) to (i) in the composition or preparation is in a range of 0.7 to 3.0, and wherein the phosphatidylcholine is contained in the composition or preparation in a concentration of 0.3125 to 10% (w/v).

### Claim 6 (depends on 5)

The method of claim 5, wherein the composition or preparation is in a form of an injectable composition or preparation.

### Claim 7 (depends on 5)

The method of claim 5, wherein the side effect is at least one selected from the group consisting of edema; necrosis of muscle cells, fibroblasts and vascular endothelial cells other than adipocytes; anesthesia of administration sites; extensive swelling; erythema; induration; paresthesia; nodule;
pruritus; burning sensation; nerve injury; and dysphagia.

### Claim 8 (depends on 5)

The method of claim 5, wherein the step of administration comprises a subcutaneous injection.