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|Title:||Hydrophilic, non-aqueous pharmaceutical carriers and compositions and uses|
|Abstract:||A waterless composition suitable for delivery of an active agent to a body surface or cavity includes a vehicle having about 70% to about 99% by weight of a hydrophilic polar solvent, said hydrophilic solvent selected from the group consisting of (i) a mixture of two or more different polyethylene glycols (PEGs), wherein at least one PEG is a high molecular weight PEG having a melting point greater than 25.degree. C.; and (ii) propylene glycol (PG); about 0% to about 10% of at least one surface active agent; about 0% to about 5% of a polymeric agent; about 0% to about 30% of a secondary hydrophilic solvent; and about 0% to about 5% of a silicone oil; and about 3% to about 25% hydrophobic propellant. The composition is otherwise substantially free of a hydrophobic solvent and includes at least one of a surface active agent and a polymeric agent. The vehicle and the propellant are sufficiently miscible that the components may be homogeneously distributed with mild shaking.|
|Inventor(s):||Tamarkin; Dov (Maccabim, IL), Eini; Meir (Ness Ziona, IL), Friedman; Doron (Karmei Yosef, IL), Besonov; Alex (Rehovot, IL), Schuz; David (Moshav Gimzu, IL), Berman; Tal (Rishon LeZiyyon, IL), Danziger; Jorge (Rishom Lezion, IL), Keynan; Rita (Rehovot, IL), Zlatkis; Ella (Rehovot, IL)|
|Assignee:||Foamix Ltd. (Rehovot, IL)|
|Filing Date:||Jan 14, 2008|
|Claims:||1. A waterless composition suitable for delivery of an active agent to a body surface or cavity comprising: a vehicle comprising: a) about 70% to about 96.5% by weight of a mixture of PEG 200 and PEG 400; b) about 0.01% to about 10% of at least one surface active agent and/or about 0.01% to about 5% of a polymeric agent; c) about 0% to about 30% of a secondary hydrophilic solvent; and d) about 0% to about 5% of a silicone oil; and e) about 3% to about 25% hydrophobic propellant; wherein the composition is otherwise substantially free of a hydrophobic solvent; and wherein the vehicle and the propellant are sufficiently miscible that the components may be homogeneously distributed with mild shaking. |
2. The composition of claim 1, wherein the mixture of PEG 200 and PEG 400 is selected to provide viscosity of the vehicle of less than 52,000 CPs, as measured at room temperature at 10 rpm spindle speed.
3. The composition of claim 1, wherein the components of the composition are sufficiently miscible that the vehicle and the propellant do not phase separate upon centrifugation at 1000 rpm.
4. The composition of claim 3, wherein the composition includes a steareth surface active agent and a hydroxypropylcellulose polymeric agent, is otherwise substantially free of a secondary hydrophilic solvent.
5. The composition of claim 1, wherein one or both of the surface active agent and the polymeric agent are selected to increase the solubility of the propellant in the vehicle.
6. The composition of claim 1 wherein the composition comprises a polymeric agent and the polymeric agent is selected from the group consisting of locust bean gum, sodium alginate, sodium caseinate, egg albumin, gelatin agar, carrageenin gum, xanthan gum, quince seed extract, tragacanth gum, guar gum, cationic guars, hydroxypropyl guar gum, starch, an amine-bearing polymer, chitosan, alginic acid, hyaluronic acid, a chemically modified starch, a carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, a polyacrylic acid polymer, a polymethacrylic acid polymer, polyvinyl acetate, a polyvinyl chloride polymer, a polyvinylidene chloride polymer, methylcellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, hydroxy propylmethyl cellulose, methylhydroxyethylcellulose, methylhydroxypropylcellulose, hydroxyethylcarboxymethylcellulose, carboxymethyl cellulose, carboxymethylcellulose carboxymethylhydroxyethylcellulose, a cationic cellulose, PEG 1000, PEG 4000, PEG 6000 and PEG 8000, polycarbophil, carbomer, and acrylates/C10-30 alkyl acrylate crosspolymer.
7. The composition of claim 1, wherein silicone oil is present in the composition and is selected from the group consisting of dimethicone, cyclomethicone and mixtures thereof.
8. The composition of claim 1 wherein the secondary hydrophilic solvent is present in the composition and is a polyol selected from the group consisting of a diol, a triol and a saccharide, wherein the triol is selected from the group consisting of glycerin, butane-1,2,3-triol, butane-1,2,4-triol and hexane-1,2,6-triol, and wherein the diol is selected from the group consisting of propylene glycol, butanediol, butenediol, butynediol, pentanediol, hexanediol, octanediol, neopentyl glycol, 2-methyl-1,3-propanediol, diethylene glycol, triethylene glycol, tetra ethylene glycol, dipropylene glycol and dibutylene glycol.
9. The composition of claim 1, wherein the ratio between the polyethylene glycol and the secondary hydrophilic solvent is between about 9:1 and about 1:1.
10. The composition of claim 1 wherein the composition further comprises one or more modulating agents.
11. The composition of claim 10, wherein the modulating agent is selected from the group of triethanol amine, sodium citrate and citric acid.
12. The composition of claim 1, further comprising an active agent.
13. The composition of claim 12, wherein the active agent is selected from the group consisting of antiinfectives, antifungals, antivirals, anesthesic analgesic, corticosteroids, non steroid anti inflammatory, retinoids , lubricating agents anti warts, antiproliferative, vasoactive, keratolytic, insectiside and repellants, dicarboxylic acids and esters; calcium channel blockers, cholinergic, Noxide doners, photodynamic, anti acne, anti wrinkle, antioxidants, self tanning active herbal extracts, acaricides, age spot and keratose removing agents, allergen, analgesics, local anesthetics, anti acne agents, antiallergic agents, anti aging agents, antibacterials, antibiotics, antibum agents, anticancer agents, antidandruff agents, antidepressants, anti dermatitis agents, antiedemics, antihistamines, antihelminths, antihyperkeratolyte agents, antiinflammatory agents, antiirritants, antilipemics, antimicrobials, antimycotics, antiproliferative agents, antioxidants, anti-wrinkle agents, antipruritics, antipsoriatic agents, antirosacea agents antiseborrheic agents, antiseptic, antiswelling agents, antiviral agents, antiyeast agents, astringents, topical cardiovascular agents, chemotherapeutic agents, corticosteroids, dicarboxylic acids, disinfectants, fungicides, hair growth regulators, hormones, hydroxy acids, immunosuppressants, immunoregulating agents, insecticides, insect repellents, keratolytic agents, lactams, metals, metal oxides, mitocides, neuropeptides, nonsteroidal anti-inflammatory agents, oxidizing agents, pediculicides, photodynamic therapy agents, retinoids, sanatives, scabicides, self tanning agents, skin whitening agents, asoconstrictors, vasodilators, vitamins, vitamins A, B, C, D, E, K and derivatives, wound healing agents and wart removers.
14. The composition of claim 12, wherein the active agent is selected from the group consisting of: Acyclovir, Azelaic acid, Benzoyl peroxide, Betamethasone 17 valerate micronized, Caffeine, Calcipotriol hydrate, Ciclopiroxolamine, Diclofenac sodium, Ketoconazole, Miconazole nitrate, Minoxidil, Mupirocin, Nifedipine regular, Permethrin BPC cis:trans 25:75, Piroxicam, Salicylic acid, Terbinafine HCl, estradiol hemihydrate and progesterone or combinations thereof.
15. The composition of claim 12, wherein the active agent includes progesterone, estrogen, a derivative thereof or mixtures thereof.
16. The composition of claim 12 wherein the active agent includes a steroid.
17. The composition of claim 12, wherein the active agent includes a vitamin.
18. The composition of claim 17, wherein the vitamin selected from the group consisting of a Vitamin D, retinol, retinoic acid, tocopherol, Vitamin K, Vitamin C, and Vitamin B, or derivatives thereof.
19. The composition of claim 17, wherein the active agent includes a steroid.
20. The composition of claim 1, wherein the composition comprises a polymeric agent and the polymeric agent is selected from the group of bioadhesive polymers.
21. The composition of claim 20, wherein the composition has a bioadhesive force in the range of about -3 g to about -25 g.
22. The composition of claim 20 wherein the polymeric agent is selected from the group consisting of hydroxypropylcellulose and carbomer.
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