IP Library Granted Patent US 11,045,479
Granted Patent B2
US 11,045,479 · App. 16/038,805 · Granted Jun 29, 2021

Treatments for resistant acne

Inventors: Shiladitya Sengupta (Delhi, IN); Suresh Rameshlal Chawrai (Pune, IN); Shamik Ghosh (Delhi, IN); Sumana Ghosh (Delhi, IN); Nilu Jain (New Delhi, IN); Suresh Sadhasivam (Salem, IN); Richard Buchta (Melbourne, AU); Anamika Bhattacharyya (Delhi, IN)
Assignee: VYOME THERAPEUTICS LIMITED
A61K31/55A61K9/0014A61K31/192A61K31/4709A61K45/06A61K47/02A61K47/08A61K47/10A61K47/32A61K47/36A61K47/38C07D513/04Y02A50/30
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Quick Facts
Patent No.
US 11,045,479
App. No.
16/038,805
Granted
Jun 29, 2021
Kind
B2
Abstract

The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.

Claims (74)

1. A method for treating acne, comprising administering a therapeutically effective amount of besifloxacin to a subject in need thereof, wherein acne is drug resistant acne, and wherein besifloxacin is comprised in a formulation comprising besifloxacin and at least one carrier or excipient, wherein the formulation comprises besifloxacin in an amount from about 1% to about 50% (w/w or w/v) and has a viscosity in a range of 1,000 mPa·s to 15,000 mPa·s.

2. The method of claim 1 , wherein the acne is not responding to a therapeutic amount of clindamycin, minocycline, doxycycline, tetracycline or erythromycin.

3. The method of claim 1 , wherein the besifloxacin is in form of a drug carrier, and wherein the drug carrier comprises the besifloxacin and at least one additional compound selected from the group consisting of lipids, oils, polymers, peptides, proteins, carbohydrates, glycolipids, phospholipids, lipoproteins, cationic molecules, and any combinations thereof.

4. The method of claim 1 , wherein the composition further comprises a second active agent.

5. The method of claim 1 , wherein the besifloxacin is a particle having a size of 5 nm to 100 μm.

6. The method of claim 1 , wherein the besifloxacin is formulated in a composition comprising the besifloxacin and at least one polymer.

7. The method of claim 6 , wherein the composition comprises the polymer in an amount from about 0.001% to about 10% w/w.

8. The method of claim 6 wherein the polymer is a cellulose, cellulose derivative, polyacrylate, copolymer or terpolymer of acrylic acid, carbomer, carbomer derivative, chitosan, carbopol, sodium hyaluronate, poloxamer, poloxamine, copolymer of 1-vinyl-2-pyrrolidone.

9. The method of claim 1 , wherein the besifloxacin is formulated in a composition comprising the besifloxacin, and wherein the composition comprises dispersed particles or droplets.

10. The method of claim 1 , wherein the besifloxacin is uncoated or coated.

11. The method of claim 1 , wherein the besifloxacin is formulated in a composition comprising the besifloxacin and an additional anti-acne agent.

12. The method of claim 11 , wherein the additional anti-acne agent is selected from the group consisting of adapalene, retinoic acid, retinoid, salicylic acid, sulfur, lactic acid, glycolic acid, pyruvic acid, lauric acid, urea, resorcinol, N-acetylcysteine, isotretinoin, tretinoin, tazarotene, clindamycin, tetracyclines, erythromycin, folic acid, nicotinamide, zinc, benzoyl peroxide, octopirox, triclosan, azelaic acid, phenoxyethanol, phenoxypropanol, and flavonoids.

13. A method for treating inflammation associated with acne, comprising administering a therapeutically effective amount of besifloxacin to a subject in need thereof, and wherein besifloxacin is comprised in a formulation comprising besifloxacin and at least one carrier or excipient, wherein the formulation comprises besifloxacin in an amount from about 1% to about 50% (w/w or w/v) and has a viscosity in a range of 1,000 mPa·s to 15,000 mPa·s.

14. A formulation comprising an 8-chloro fluoroquinolone and an additional anti-acne agent, wherein the additional anti-acne agent is selected from the group consisting of adapalene, retinoic acid, retinoid, salicylic acid, lactic acid, glycolic acid, pyruvic acid, lauric acid, urea, resorcinol, N-acetylcysteine, isotretinoin, tretinoin, tazarotene, clindamycin, tetracyclines, erythromycin, folic acid, nicotinamide, benzoyl peroxide, octopirox, triclosan, azelaic acid, phenoxyethanol, and phenoxypropanol.

15. The formulation of claim 14 , wherein the 8-chloro fluoroquinolone is besifloxacin and the formulation comprises:

(i) 0.5 to 4 (% w/w) Besifloxacin.HCl (Equivalent to Besifloxacin);

(ii) 2 to 7 (% w/w) diethylene glycol monoethyl ether;

(iii) 0.1 (% w/w) Edetate disodium dehydrate (EDTA);

(iv) 2 to 10 (% w/w) glycerin;

(v) 0.9 to 1.75 (% w/w) hydroxyethyl cellulose;

(vi) 0 to 0.8 (% w/w) carbomer;

(vii) 0.3 to 0.7 (% w/w) phenoxyethanol;

(viii) 2 to 7 (% w/w) polyethylene glycol 400;

(ix) 0 to 0.5 (% w/w) sodium hyaluronate;

(x) sodium hydroxide;

(xi) purified water; and

(x) an additional anti-acne agent.

16. The formulation of claim 14 , wherein the 8-chloro fluoroquinolone is besifloxacin and the formulation comprises:

(i) 1 to 4 (% w/w) Besifloxacin.HCl (Equivalent to Besifloxacin);

(ii) 5 (% w/w) diethylene glycol monoethyl ether;

(iii) 0.1 (% w/w) Edetate disodium dehydrate (EDTA);

(iv) 5 (% w/w) glycerin;

(v) 0.5 to 1.5 (% w/w) hydroxyethyl cellulose;

(vi) 0.3 to 1.2 (% w/w) carbomer;

(vii) 0.7 (% w/w) phenoxyethanol;

(viii) 5 (% w/w) polyethylene glycol 400;

(ix) 0 to 1(% w/w) sodium hyaluronate;

(x) sodium hydroxide;

(xi) purified water; and

(x) an additional anti-acne agent.

17. The formulation of claim 14 , wherein the composition comprises at least one polymer.

18. The formulation of claim 17 , wherein the formulation comprises the polymer in an amount from about 0.001% to about 10% w/w.

19. The formulation of claim 17 , wherein the polymer is a cellulose, cellulose derivative, polyacrylate, copolymer or terpolymer of acrylic acid, carbomer, carbomer derivative, chitosan, carbopol, sodium hyaluronate, poloxamer, poloxamine, copolymer of l-vinyl-2-pyrrolidone.

20. The formulation of claim 14 , wherein the composition comprises dispersed particles or droplets.

21. A method for treating acne, comprising administering a formulation of claim 14 to a subject in need thereof.

22. The method of claim 21 , wherein acne is drug resistant acne.

23. The method of claim 21 , wherein the acne is not responding to a therapeutic amount of clindamycin, minocycline, doxycycline, tetracycline or erythromycin.

24. The method of claim 13 , wherein acne is drug resistant acne.

25. The method of claim 13 wherein besifloxacin is in the formulation comprising:

(i) 0.5 to 4 (% w/w) Besifloxacin.HCl (Equivalent to Besifloxacin);

(ii) 2 to 7 (% w/w) diethylene glycol monoethyl ether;

(iii) 0.1 (% w/w) Edetate disodium dehydrate (EDTA);

(iv) 2 to 10 (% w/w) glycerin;

(v) 0.9 to 1.75 (% w/w) hydroxyethyl cellulose;

(vi) 0 to 0.8 (% w/w) carbomer;

(vii) 0.3 to 0.7 (% w/w) phenoxyethanol;

(viii) 2 to 7 (% w/w) polyethylene glycol 400;

(ix) 0 to 0.5 (% w/w) sodium hyaluronate;

(x) sodium hydroxide;

(xi) purified water.

26. The method of claim 13 wherein besifloxacin is in the formulation comprising:

(i) 1 to 4 (% w/w) Besifloxacin.HCl (Equivalent to Besifloxacin);

(ii) 5 (% w/w) diethylene glycol monoethyl ether;

(iii) 0.1 (% w/w) Edetate disodium dehydrate (EDTA);

(iv) 5 (% w/w) glycerin;

(v) 0.5 to 1.5 (% w/w) hydroxyethyl cellulose;

(vi) 0.3 to 1.2 (% w/w) carbomer;

(vii) 0.7 (% w/w) phenoxyethanol;

(viii) 5 (% w/w) polyethylene glycol 400;

(ix) 0 to 1(% w/w) sodium hyaluronate;

(x) sodium hydroxide; and

(xi) purified water.

27. A method for treating drug resistant acne, comprising administering a therapeutically effective amount of a topical formulation of besifloxacin to a subject in need thereof, wherein said formulation comprises besifloxacin in an amount from about 1% to about 50% (w/w or w/v).

28. A method for treating inflammation associated with acne, comprising administering a therapeutically effective amount of a topical formulation of besifloxacin to a subject in need thereof, wherein said formulation comprises besifloxacin in an amount from about 1% to about 50% (w/w or w/v).

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 18, 2019
From: SENGUPTA, SHILADITYA; CHAWRAI, SURESH RAMESHLAL; GHOSH, SHAMIK; GHOSH, SUMANA; JAIN, NILU; SADHASIVAM, SURESH; BUCHTA, RICHARD; BHATTACHARYYA, ANAMIKA
To: VYOME BIOSCIENCES PVT. LTD.
Reel/Frame 048924/0990 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 3, 2019
From: VYOME BIOSCIENCES PRIVATE LIMITED
To: VYOME THERAPEUTICS LIMITED
Reel/Frame 047894/0139 →
Priority Claims (2)
IN 269/DEL/2014 · Jan 29, 2014 · national
IN 3247/DEL/2014 · Nov 10, 2014 · national
Continuity (2)
Division 15115143
Related Publication 20180318313A1 · Nov 8, 2018