IP Library Granted Patent US 8,618,081
Granted Patent B2
US 8,618,081 · App. 13/100,724 · Granted Dec 31, 2013

Compositions, gels and foams with rheology modulators and uses thereof

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Quick Facts
Patent No.
US 8,618,081
App. No.
13/100,724
Granted
Dec 31, 2013
Kind
B2
Abstract

The present disclosure relates generally to compositions for cosmetic or pharmaceutical application. The compositions include a carrier and rheology modulators.

Claims (45)

1. A therapeutic composition comprising:

a first rheology modulator comprising a pharmaceutical or a cosmetic active agent at least part of which is suspended in the therapeutic composition; and

a carrier comprising:

a) a second rheology modulator selected from the group consisting of (i) a combination of at least one fatty alcohol and at least one wax; (ii) a combination of at least one fatty acid and at least one wax; and (iii) a combination of: at least one fatty alcohol, at least one fatty acid, and at least one wax; and

b) at least one hydrophobic solvent;

the carrier being otherwise free of or containing less than 0.1% by weight of surfactant;

wherein the at least one wax comprises a hydrogenated castor oil;

wherein the viscosity of the therapeutic composition is at least about 30% higher than the viscosity of a first partial composition comprising the carrier without the first rheology modulator; and is higher than the viscosity of the first rheology modulator and the at least one hydrophobic solvent without the second rheology modulator; and

wherein the viscosity of the first partial composition is less than about 25,000 cPs at room temperature.

2. The composition of claim 1 wherein the first rheology modulator comprises at least one tetracycline antibiotic.

3. The composition of claim 2 , wherein the tetracycline antibiotic is compatible with the carrier and with the second rheology modulator.

4. The composition of claim 2 , wherein the tetracycline antibiotic is selected from the group consisting of tetracycline, oxytetracycline, demeclocycline, doxycycline, lymecycline, meclocycline, methacycline, minocycline, rolitetracycline, chlorotetracycline, and tigecycline; wherein the tetracycline antibiotic is present in a free base form, a hydrate form, a salt form, or a complex form; and

wherein at least part of the tetracycline antibiotic is not soluble and is suspended in the carrier composition.

5. The composition of claim 3 , wherein the tetracycline antibiotic is minocycline or doxycycline or a mixture of both.

6. The composition of claim 1 , wherein the therapeutic composition is waterless.

7. The composition of claim 1 , wherein the second rheology modulator comprises a compound selected from the group consisting of:

i) at least one fatty alcohol selected from the group consisting of:

(a) a fatty alcohol having 14 or more carbons in its carbon chain, myristyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, cetostearyl alcohol, oleyl alcohol, erucyl alcohol, arachidyl alcohol, behenyl alcohol, tetracosanol, hexacosanol, octacosanol, triacontanol, tetratriacontanol, 1-triacontanol, and a fatty alcohol having a carbon chain between C30 and C50;

(b) a fatty alcohol mixture derived from beeswax; and

(c) a therapeutically-active fatty alcohol;

ii) at least one fatty acid selected from the group consisting of:

(a) a fatty acid having 12 or more carbons in its carbon chain, dodecanoic acid, myristic acid, hexadecanoic acid, heptadecanoic acid, palmitic acid, stearic acid, oleic acid, arachidic acid, behenic acid, tetracosanoic acid, hexacosanoic acid, heptacosanoic acid, octacosanoic acid, triacontanoic acid, dotriacontanoic acid, tritriacontanoic acid, tetratriacontanoic acid, pentatriacontanoic acid, and a fatty acid having a carbon chain between C30 and C50; and

(b) a hydroxy fatty acid;

iii) at least one wax, having the properties of (i) plastic behavior at ambient temperatures, (ii) a melting point above approximately 45° C., (iii) a relatively low viscosity when melted; and (iv) hydrophobic nature, or selected from the group consisting of a beeswax, a hard fat, a paraffin and a hydrogenated castor oil.

8. The composition of claim 7 , wherein the second rheology modulator comprises a combination of (i) at least one fatty alcohol, (ii) at least one fatty acid; and (iii) at least one wax.

9. The composition of claim 7 , wherein the ratio of fatty alcohol to wax or fatty acid to wax or fatty alcohol and fatty acid to wax is between about 1:10 to about 10:1.

10. The composition of claim 1 , wherein the carrier composition is essentially free of at least one of water, polymeric agents, short chain alcohols, and polyols.

11. The composition of claim 1 , wherein the carrier composition is essentially free of water, polymeric agents, short chain alcohols, and polyols.

12. The composition of claim 1 , wherein the viscosity of the therapeutic composition is at least about 50% more than the viscosity of the carrier without the first rheology modulator.

13. The composition of claim 12 , wherein the increase in viscosity is at least about 100%.

14. The composition of claim 13 , wherein the viscosity of the carrier without the first rheology modulator is

i) less than about 12,000 cPs; or

ii) less than about 8,000 cPs; or

iii) less than about 2,000 cPs.

15. The composition of claim 1 , wherein the concentration of the first rheology modulator in the composition is from about 0.01% to about 25% by weight of the therapeutic composition.

16. The composition of claim 1 , wherein the hydrophobic solvent is selected from the group consisting of: a diglyceride, a therapeutic oil, acetylated lanolin alcohol, alexandria laurel tree oil, alkyl benzoate, alkyl octanoate, almond oil, an essential oil, an unsaturated or polyunsaturated oil, apricot stone oil, arachidyl behenate, arachidyl propionate, avocado oil, barley oil, basil oil, beeswax, benzyl laurate, benzyl myristate, benzyl palmitate, bis (octyldodecyl stearoyl) dimer dilinoleate, borage seed oil, butyl myristate, butyl stearate, C12-C15 alkyl benzoate, C12-C15 alkyl octanoate, calendula oil, camphor oil, canelle nut tree oil, canola oil, capric/caprylic triglycerides, caprylyl methicone, cardamom oil, carrot oil, castor oil, cetearyl ethylhexanoate, cetearyl isononanoate, cetearyl octanoate, cetyl acetate, cetyl dimethicone, cetyl ethylhexanoate, cetyl lactate, cetyl myristate, cetyl octanoate, cetyl palmitate, cetyl ricinoleate, citronella oil, clary sage oil, clove oil, cocoglycerides, coconut oil, cod-liver oil, corn oil, cotton oil, cottonseed oil, cyclohexasiloxane, cyclomethicone, Cyclomethicone 5-NF (cyclopentasiloxane), cyclotetrasiloxane, cypress oil, decyl oleate, diethyleneglycol diethylhexanoate, diethyleneglycol diisononanoate, diethyleneglycol dioctanoate, diethylhexanoate, diethylhexyl adipate, diethylhexyl malate, diethylhexyl succinate, diisopropyl adipate, diisopropyl dimerate, diisopropyl sebacate, diisosteary dimer dilinoleate, diisostearyl fumerate, dimethicone, dimethyl polysiloxane, dioctyl malate, dioctyl sebacate, diisopropyl adipate, dodecyl oleate, Dow Corning 244 Fluid (cyclotetrasiloxane), Dow corning 246 Fluid (d6+d5) (cyclohexasiloxane & cyclopentasiloxane), epoxy-modified silicone oil, ester derivatives of lanolic acid, ester oils, ethylhexyl cocoate, ethylhexyl ethylhexanoate, ethylhexyl hydroxystarate, ethylhexyl isononanoate, ethylhexyl palmitate, ethylhexyl palmytate, ethylhexyl pelargonate, ethylhexyl stearate, evening primrose oil, fatty acid-modified silicone oil, flaxseed oil, fluoro group-modified silicone oil, frankincense oil, gelled mineral oil, ginger oil, glycereth triacetate, glycerol triheptanoate, glyceryl oleate, glyceryl trioctanoate, glyceryl triundecanoate, grape seed oil, grapefruit oil, groundnut oil, hard fat , hazelnut oil, heavy mineral oil, hempseed oil, herring oil, hexadecyl stearate, hexyl laurate, hydrocarbon oils, hyssop oil, isoamyl laurate, isocetearyl octanoate, isocetyl behenate, isocetyl lanolate, isocetyl palmitate, isocetyl salicylate, isocetyl stearate, isocetyl stearoyl stearate, isodecyl ethylhexanoate, isodecyl isononanoate, isodecyl oleate, isododecane, isohexadecane, isododecane, isohexadecanol, isohexyl decanoate, isononyl isononanoate, isononyl octanoate, isoparaffin, isopropyl isostearate, isopropyl lanolate, isopropyl laurate, isopropyl myristate, isopropyl palmitate, isopropyl stearate, isostearyl citrate, isostearyl salicylate, isostearyl tartarate, isostearyl behenate, isostearyl erucate, isostearyl glycolate, isostearyl isononanoate, isostearyl isostearate, isostearyl lactate, isostearyl linoleate, isostearyl linolenate, isostearyl malate, isostearyl neopentanoate, isostearyl palmitate, isotridecyl isononanoate, jasmine oil, jojoba oil, lauryl lactate, lavender oil, lemon oil, light mineral oil, liquid paraffin, liquid triglycerides, lucerne oil, maize germ oil, maleated soybean oil, mandarin oil, manuka oil, marjoram oil, marrow oil, MCT oil, methylphenylpolysiloxane, millet oil, mineral oil, myristyl lactate, myristyl myristate, myristyl neopentanoate, myristyl propionate, myrrh oil, neopentylglycol dicaprate, neopentylglycol dicaprylate/dicaprate, neroli oil, nutmeg oil, octyl palmitate, octyl stearate, octyldodecanol, octyldodecyl behenate, octyldodecyl hydroxystearate, octyldodecyl myristate, octyldodecyl stearoyl stearate, oils from animal origin, oils of plant origin, oleyl erucate, oleyl lactate, oleyl oleate, olive oil, dimethiconol, palm oil, passionflower oil, peanut oil, PEG/PPG 18/18 dimethicone, pentaerythrityl tetrastearate, petitgrain oil, phenyl trimethicone, phenyltrimethicone, poly(dimethylsiloxane)-(diphenyl-siloxane) copolymer, polyalkyl siloxane, polyalkylaryl siloxane, polyalphaolefin, polyaryl siloxane, polyaryl siloxanes, polyether group-modified silicone oil cyclomethicone, polyether siloxane copolymer, polyether siloxane copolymers, polyisobutylene, polyolefin, poppy oil, PPG alkyl ether, PPG-10 cetyl ether, PPG-10 oleyl ether, PPG-11 stearyl ether, PPG-12 butyl ether, PPG-14 butyl ether, PPG-15 butyl ether, PPG-15 stearyl ether, PPG-16 butyl ether, PPG-17 butyl ether, PPG-18 butyl ether, PPG-2 butyl ether, PPG-2 methyl ether, PPG-20 butyl ether, PPG-20 oleyl ether, PPG-22 butyl ether, PPG-23 oleyl ether, PPG-24 butyl ether, PPG-26 butyl ether, PPG-28 cetyl ether, PPG-3 methyl ether, PPG-3 myristyl ether, PPG-30 butyl ether, PPG-30 cetyl ether, PPG-30 isocetyl ether, PPG-30 oleyl ether, PPG-33 butyl ether, PPG-37 oleyl ether, PPG-4 butyl ether, PPG-4 lauryl ether, PPG-4 myristyl ether, PPG-40 butyl ether, PPG-5 butyl ether, PPG-50 cetyl ether, PPG-50 oleyl ether, PPG-52 butyl ether, PPG-53 butyl ether, PPG-7 lauryl ether, PPG-9 butyl ether, PPG-9-13 butyl ether, propyl myristate, propylene glycol dicaprate, propylene glycol dicaprylate, propylene glycol myristyl ether acetate, propylene glycol ricinoleate, rapeseed oil, rosehip oil, rye oil, safflower oil, sage oil, salmon oil, sesame oil, shea butter, silicone oils, soya oil, soybean oil, stearyl caprate, stearyl dimethicone, stearyl heptanoate, stearyl propionate, sunflower oil, sweet almond oil, synthetic isoalkane, sysymbrium oil, syzigium aromaticum oil, tangerine oil, tea tree oil, therapeutic oils, tocopheryl acetate, tocopheryl linoleate, tridecyl ethylhexanoate, tridecyl isononanoate, triisocetyl citrate, unsaturated or polyunsaturated oils, vanilla oil, verbena oil, walnut oil, wheat germ glycerides, wheat germ oil, white petrolatum, and mixtures of any two or more thereof.

17. The composition of claim 16 , wherein the carrier composition further comprises a petrolatum or a paraffin.

18. The composition of claim 7 , further comprising a liquefied or compressed gas propellant, wherein the composition is a foamable composition; wherein the second rheology modulator is about 0.1% to about 20% by weight of the carrier composition; wherein the hydrophobic solvent is about 60% to about 95% by weight of the carrier composition; wherein the ratio of carrier composition to propellant is from about 100:1 to about 100:30; and wherein upon dispensing, the foamable composition forms a breakable foam that breaks upon application of shear force.

19. The composition of claim 1 , wherein the carrier composition further comprises about 1% to about 25% by weight of the carrier composition of a polar solvent or a penetration enhancer.

20. The composition of claim 1 , wherein the increase in viscosity is a synergistic increase such that the combined viscosity of the first partial composition and the viscosity of the first rheology modulator and the hydrophobic solvent without the second rheology modulator is less than the viscosity of the therapeutic composition.

21. The composition of claim 1 , wherein the fatty alcohol is selected from the group consisting of isostearyl alcohol, behenyl alcohol, stearyl alcohol, cetyl alcohol, oleyl alcohol, myristyl alcohol, and cetostearyl alcohol; the fatty acid is selected from the group consisting of palmitic acid, stearic acid, and oleic acid; and the wax is selected from the group consisting of a beeswax, a hard fat, a paraffin, and a hydrogenated castor oil.

22. The composition of claim 21 , wherein the fatty alcohol is selected from the group consisting of behenyl alcohol, stearyl alcohol, cetyl alcohol, myristyl alcohol, and cetostearyl alcohol; the fatty acid is stearic acid; and the wax is selected from the group consisting of a beeswax, and a hydrogenated castor oil.

23. The composition of claim 22 comprising behenyl alcohol, stearyl alcohol, myristyl alcohol, cetostearyl alcohol, stearic acid, a beeswax, and a hydrogenated castor oil.

24. The composition of claim 16 , wherein the hydrophobic solvent comprises mineral oil.

25. The composition of claim 1 , wherein the hydrophobic solvent is selected from the group consisting of a vegetable oil, a mineral oil, a silicone oil, and mixtures of any two or more thereof.

Assignments (11)
SECURITY INTEREST Recorded Dec 28, 2023
From: JOURNEY MEDICAL CORPORATION; JG PHARMA, INC.
To: SWK FUNDING LLC
Reel/Frame 066157/0079 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2022
From: VYNE THERAPEUTICS INC.; VYNE PHARMACEUTICALS INC.
To: JOURNEY MEDICAL CORPORATION
Reel/Frame 058925/0568 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 22, 2021
From: VYNE THERAPEUTICS INC.
To: VYNE PHARMACEUTICALS INC.
Reel/Frame 058463/0208 →
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2021
From: PERCEPTIVE CREDIT HOLDINGS II, LP
To: VYNE THERAPEUTICS INC. (F/K/A MENLO THERAPEUTICS INC. AND SUCCESSOR-IN-INTEREST TO VYNE PHARMACEUTICALS LTD., F/K/A FOAMIX PHARMACEUTICALS LTD.)
Reel/Frame 057544/0708 →
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2021
From: PERCEPTIVE CREDIT HOLDINGS II, LP
To: VYNE PHARMACEUTICALS LTD. (F/K/A FOAMIX PHARMACEUTICALS LTD.)
Reel/Frame 057544/0138 →
PATENT SECURITY AGREEMENT Recorded Feb 17, 2021
From: VYNE THERAPEUTICS INC.
To: PERCEPTIVE CREDIT HOLDINGS II, LP
Reel/Frame 055326/0009 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 4, 2021
From: VYNE PHARMACEUTICALS LTD.
To: VYNE THERAPEUTICS INC.
Reel/Frame 055215/0298 →
CHANGE OF NAME Recorded Nov 4, 2020
From: FOAMIX PHARMACEUTICALS LTD.
To: VYNE PHARMACEUTICALS LTD.
Reel/Frame 054306/0387 →
PATENT SECURITY AGREEMENT Recorded Jul 30, 2019
From: FOAMIX PHARMACEUTICALS LTD
To: PERCEPTIVE CREDIT HOLDINGS II, LP
Reel/Frame 049912/0045 →
CHANGE OF NAME Recorded Jul 30, 2014
From: FOAMIX LTD.
To: FOAMIX PHARMACEUTICALS LTD.
Reel/Frame 033445/0249 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 8, 2011
From: TAMARKIN, DOV; GAZAL, ELANA; HAZOT, YOHAN; SCHUZ, DAVID; PAPIASHVILI, IRAKLIY
To: FOAMIX LTD.
Reel/Frame 026873/0361 →