Pharmaceutical composition for reducing local fat and uses thereof
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.
1. A subcutaneous injection formulation to be administered at a local site of a subject, comprising:
a curcumin; and
a pharmaceutically acceptable polyoxyethylene castor oil derivative;
wherein, the weight ratio of the curcumin to the polyoxyethylene castor oil derivative is 1:8˜1:500; the pharmaceutically acceptable polyoxyethylene castor oil derivative and the curcumin together form a plurality of curcumin-containing micelles, and the hydrophilic-lipophilic balance value (HLB value) of the polyoxyethylene castor oil derivative is greater than 10.
2. The subcutaneous injection formulation of claim 1 , the polyoxyethylene castor oil derivative is at least one of Kolliphor ELP (also known as Cremophor ELP), cremophor RH 40, and other polyoxyethylene castor oil derivatives, or combination thereof.
3. The subcutaneous injection formulation of claim 1 , the weight ratio of the curcumin to the polyoxyethylene castor oil derivative is 1:8˜1:150.
4. The subcutaneous injection formulation of claim 3 , the weight ratio of the curcumin to the polyoxyethylene castor oil derivative is 1:20˜1:150.
5. The subcutaneous injection formulation of claim 1 , the concentration of curcumin in the subcutaneous injection formulation is 0.3˜120 mg/g.
6. The subcutaneous injection formulation of claim 5 , the concentration of curcumin in the subcutaneous injection formulation is 2˜91 mg/g.
7. The subcutaneous injection formulation of claim 1 , the diameter of the curcumin containing micelles is 3-50 nm.
8. The subcutaneous injection formulation of claim 7 , the diameter of the curcumin containing micelles is 5-20 nm.
9. The subcutaneous injection formulation of claim 1 , the curcuminoid is curcumin.
10. The subcutaneous injection formulation of claim 1 , the subcutaneous injection formulation further comprises a pharmaceutically acceptable aqueous solution.
11. The subcutaneous injection formulation of claim 1 , the subcutaneous injection formulation further comprises a second lipophilic drug-containing micelles; the second lipophilic-drug containing micelle is a second microstructure formed by a second polyoxyethylene castor oil derivative, and a second lipophilic drug is encapsulated in said second drug-containing micelles.
12. The subcutaneous injection formulation of claim 11 , the hydrophilic-lipophilic balance value (HLB value) of the second polyoxyethylene castor oil derivative is greater than 10.
13. The subcutaneous injection formulation of claim 11 , the second polyoxyethylene castor oil derivative is at least one of Kolliphor ELP (also known as Cremophor ELP), cremophor RH 40, and other polyoxyethylene castor oil derivatives, or combination thereof.
14. The subcutaneous injection formulation of claim 11 , the second lipophilic drug is at least one of quercetin, synephrin, puerarin, resveratrol, and other lipophilic drug except curcumin, or combination thereof.
15. The subcutaneous injection formulation of claim 11 , the weight ratio of the curcumin to the second lipophilic drug is 30:1˜1:10.
16. The subcutaneous injection formulation of claim 1 , the subcutaneous injection formulation further comprises a hydrophilic drug.
17. The subcutaneous injection formulation of claim 16 , the hydrophilic drug is at least one of green tea extract, epigallocatechin gallate, epicatechin, epicatechin gallate, epigallocatechin, gallocatechin gallate, gallocatechin, catechin gallate, catechin, epigallocatechin gallate (EGCG), caffeine, carnitine, L-carnitine, synephrine, chlorogenic acid, and other hydrophilic drugs, or combination thereof.
18. The subcutaneous injection formulation of claim 16 , the weight ratio of the curcumin to the hydrophilic drug is 30:1 to 1:10.