# US 11,433,034 B2 · Pharmaceutical composition for reducing local fat and uses thereof

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- Number: US 11,433,034 B2
- Document ID: US11433034B2
- Status: Granted
- Kind: B2
- Application number: 16/749,266
- Filed: 2020-01-22
- Published: 2020-05-28
- Granted: 2022-09-06
- Earliest claimed: 2015-08-28
- Assignees: Caliway Biopharmaceuticals Co., Ltd.
- Applicants: Caliway Biopharmaceuticals Co., Ltd.
- Inventors: Yu-Fang Ling
- Web page: https://patentgrep.com/patent/US11433034B2

## CPC

- A61K 31/12: Ketones
- A61K 8/11: Encapsulated compositions
- A61K 8/347: {Phenols}
- A61K 8/86: Polyethers
- 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 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/107: Emulsions {; Emulsion preconcentrates; Micelles (composition of emulsions A61K47/00)}
- A61K 9/1075: {Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers (A61K9/0026 takes precedence)}
- A61K 31/05: Phenols {(cannabinoids A61K31/658)}
- A61K 36/82: Theaceae (Tea family), e.g. camellia
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61Q 19/06: for countering cellulitis
- 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
- A61Q: SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS

## Abstract

The present invention provides a pharmaceutical composition for reducing localized fat, comprising drug-containing micelles made of surfactants, and curcumin encapsulated in said drug-containing micelles. This pharmaceutical composition for reducing localized fat can reduce the fat at the administration site, and has the advantages of high stability, high bioavailability for fat tissue, few side effects, and sustained release.

## Claims

### Claim 1

A method for reducing the subcutaneous fat at a local site of a subject, comprising administering a pharmaceutical composition to the local site of the subject, wherein, the pharmaceutical composition comprises: drug-containing micelles; and curcuminoid encapsulated in said drug-containing micelles; wherein, the drug-containing micelle is a microstructure formed by a pharmaceutically acceptable non-ionic surfactant, and the hydrophilic-lipophilic balance value (HLB value) of the non-ionic surfactant is greater than 10; and wherein the weight ratio of the curcuminoid to the non-ionic surfactant is 1:8 to 1:500; wherein the non-ionic surfactant comprises polysorbate 80, polyoxyl 15 hydroxystearate, polyoxyethylene castor oil derivatives, or a combination thereof.

### Claim 2 (depends on 1)

The method of claim 1, wherein the non-ionic surfactant comprises polyoxyethylene castor oil derivatives.

### Claim 3 (depends on 2)

The method of claim 2, wherein the polyoxyethylene castor oil derivative comprises polyoxyl 35 castor oil, polyoxyl 40 hydrogenated castor oil, or a combination thereof.

### Claim 4 (depends on 1)

The method of claim 1, wherein the concentration of the curcuminoid in the pharmaceutical composition is 0.3˜120 mg/g.

### Claim 5 (depends on 1)

The method of claim 1, wherein the diameter of the drug-containing micelles is 3˜50 nm.

### Claim 6 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition further comprises a pharmaceutically acceptable aqueous solution.

### Claim 7 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition further comprises a second lipophilic drug-containing micelles; wherein, the second lipophilic drug-containing micelle is a second microstructure formed by a second non-ionic surfactant, and a second lipophilic drug is encapsulated in said second lipophilic drug-containing micelles.

### Claim 8 (depends on 7)

The method of claim 7, wherein the hydrophilic-lipophilic balance value (HLB value) of the second non-ionic surfactant is greater than 10.

### Claim 9 (depends on 7)

The method of claim 7, wherein the second non-ionic surfactant comprises polysorbate 80, polyoxyl 15 hydroxystearate, polyoxyethylene castor oil derivatives, or a combination thereof.

### Claim 10 (depends on 9)

The method of claim 9, wherein the second non-ionic surfactant comprises polyoxyl 35 castor oil, polyoxyl 40 hydrogenated castor oil, or a combination thereof.

### Claim 11 (depends on 7)

The method of claim 7, wherein the second lipophilic drug comprises quercetin, synephrine, puerarin, resveratrol, or a combination thereof.

### Claim 12 (depends on 7)

The method of claim 7, wherein the weight ratio of the curcuminoid to the second lipophilic drug is 30:1˜1:10.

### Claim 13 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition further comprises a hydrophilic drug.

### Claim 14 (depends on 13)

The method of claim 13, wherein the hydrophilic drug comprises green tea extract, epicatechin, epicatechin gallate, epigallocatechin, gallocatechin gallate, gallocatechin, catechin gallate, catechin, epigallocatechin gallate (EGCG), caffeine, carnitine, L-carnitine, synephrine, chlorogenic acid, or a combination thereof.

### Claim 15 (depends on 1)

The method of claim 1, wherein the weight ratio of the curcuminoid to the hydrophilic drug is 30:1 to 1:10.

### Claim 16 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition is a subcutaneous injection formulation, a subcutaneous fat layer injection formulation, a solution for implanted infusion, a cream formulation, or a patch formulation.

### Claim 17 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition is injected at the local site of the subject at a dose of 0.02˜20 mg/cm2.

### Claim 18 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition is injected at the local site of the subject at a dose of 0.01˜40 mg/kg.

### Claim 19 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition is administered to the subject at a frequency of 1˜12 times every other day to every 30 days.

### Claim 20 (depends on 1)

The method of claim 1, wherein the pharmaceutical composition further comprises a cosolvent, a suspending agent, and an oil phase excipient, or a combination thereof.

### Claim 21 (depends on 20)

The method of claim 20, wherein the microstructure is co-formed by at least the non-ionic surfactant, the oil phase excipient, and the cosolvent.