TOPICAL FORMULATIONS HAVING ENHANCED BIOAVAILABILITY
The present disclosure provides compositions suitable for delivering lipophilic bioactive agents. The compositions may be utilized to treat numerous diseases and conditions that would benefit from the application of a lipophilic bioactive agent.
1 - 22 . (canceled)
23 . A concentrate comprising:
a phospholipid selected from the group consisting of lecithin, lysolecithin, phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol, phosphatidylglycerol, phosphatidic acid, phosphatidylserine, lysophosphatidylcholine, lysophosphatidylethanolamine, lysophosphatidylglycerol, lysophosphatidic acid, lysophosphatidylserine, PEG-phosphatidylethanolamine, PVP-phosphatidylethanolamine, and combinations thereof;
at least one lipophilic bioactive agent that comprises Coenzyme Q10; and
at least one solubilizer selected from the group consisting of polyoxyalkylene dextrans, fatty acid esters of saccharose, fatty alcohol ethers of oligoglucosides, fatty acid esters of glycerol, polyoxyethylene-type compounds, polyethoxylated fatty acid esters of sorbitan, fatty acid esters of poly(ethylene oxide), fatty alcohol ethers of poly(ethylene oxide), alkylphenol ethers of poly(ethylene oxide), polyoxyethylene-polyoxypropylene block copolymers, ethoxylated oils, and combinations thereof; and
wherein the lipophilic bioactive agent is present in an amount of from about 10% to about 30% by weight of the concentrate.
24 . The concentrate of claim 23 , wherein the concentrate comprises an additional lipophilic bioactive agent selected from the group consisting of acutretin, albendazole, albuterol, aminogluthemide, amiodarone, amlodipine, amphetamine, amphotericin B, atorvastatin, atovaquone, azithromycin, baclofen, beclomethsone, benezepril, benzonatate, betamethasone, bicalutanide, budesonide, bupropion, busulphan, butenafine, calcifediol, calciprotiene, calcitriol, camptothecan, candesartan, capsaicin, carbamezepine, carotenes, celecoxib, cerivistatin, cetrizine, chlorpheniramine, cholecalciferol, cilostazol, cimetidine, cinnarizine, ciprofloxacin, cisapride, clarithromycin,clemastine, clomiphene, clomipramine, clopidrogel, codeine, cyclobenzaprine, cyclosporine, danazol, dantrolene, dexchlopheniramine, diclofenac, dicoumarol, digoxin, dihydroepiandrosterone, dihydroergotamine, dihydrotachysterol, dirithromycin, donepezil, efavirenz, eposartan, ergocalciferol, ergotamine, essential fatty acid sources, etodolac, etoposide, famotidine, fenofibrate , fentanyl, fexofenadine, finasteride, flucanazole, flurbiprofen, fluvastatin, fosphenytion, frovatriptan, furazolidone, gabapentin, gemfibrozil, glibenclamide, glipizide, glyburide, glymepride, griseofulvin, halofantrine, ibuprofen, irbesartan, irinotecan, isosorbide dinitrate isotreinoin, itraconazole, ivermectin, ketoconazole, ketorolac, lamotrigine, lanosprazole, leflunomide, lisinopril, loperamide, loratadine, lovastatin, L-thryroxine, lutein, lycopene, medroxyprogesterone, mefepristone, mefloquine, megesterol acetate, methadone, methoxsalen, metronidazole, metronidazole, miconazole, midazolam, miglitol, minoxidil, mitoxantrone, montelukast, nabumetone, nalbuphine, naratiptan, nelfinavir, nifedipine, nilsolidipine, nilutanide, nitrofurantoin, nizatidine, omeprazole, oprevelkin, osteradiol, oxaprozin, paclitaxel, paricalcitol, paroxetine, pentazocine, pioglitazone, pizofetin, pravastatin, prednisolone, probucol, progesterone, pseudo-ephedrine, pyridostigmine, rabeprazole, raloxifene, refocoxib, repaglinide, rifabutine, rifapentine, rimexolone, ritanovir, rizatriptan, rosigiltazone, saquinavir, sertraline, sibutramine, sildenafil citrate, simvastatin, sirolimus, spironolactone, sumatriptan, tacrine, tacrolimus, tamoxifen, tamsulosin, targretin, tazarotene, telmisartan, teniposide, terbinafine, terzosin, tetrahydrocannabinol, tiagabine, ticlidopine, tirofibran, tizanidine, topiramate, topotecan, toremifene, tramadol, tretinoin, troglitazone, trovafloxacin, valsartan, venlafaxine, vertoporfin, vigabatrin, vitamin A, vitamin D, vitamin E, vitamin K, zafirlukast, zileuton, zolmitriptan, zolpidem, zopiclone and a combination thereof.
25 . The concentrate of claim 23 , wherein the lipophilic bioactive agent is present in an amount of from about 18% to about 26% by weight of the concentrate.
26 . The concentrate of claim 25 , wherein the lipophilic bioactive agent is present in an amount of from about 21% to about 22% by weight of the concentrate.
27 . The concentrate of claim 26 , wherein the lipophilic bioactive agent is present in an amount of about 21% or about 22% by weight of the concentrate.
28 . The concentrate of claim 23 , wherein the amount of phospholipid in the concentrate is from about 1% to about 20% by weight of the concentrate.
29 . The concentrate of claim 28 , wherein the amount of phospholipid in the concentrate is from about 4% to about 12% by weight of the concentrate.
30 . The concentrate of claim 28 , further comprising a solvent, a humectant, and a preservative.
31 . The concentrate of claim 23 , wherein the phospholipid comprises lecithin.
32 . The concentrate of claim 23 , wherein the solubilizer is selected from the group consisting of polysorbate 80, polysorbate 20, polysorbate 60, polysorbate 65, polysorbate 85, and combinations thereof.
33 . The concentrate of claim 23 , further comprising a solvent.
34 . The concentrate of claim 33 , wherein the solvent is water.
35 . The concentrate of claim 23 , further comprising a humectant.
36 . The concentrate of claim 35 , wherein the humectant comprises propylene glycol.
37 . The concentrate of claim 35 , wherein the humectant comprises pentylene glycol.
38 . The concentrate of claim 23 , further comprising a preservative.
39 . The concentrate of claim 38 , wherein the preservative comprises phenoxyethanol.
40 . The concentrate of claim 23 , wherein the concentrate comprises a polyethoxylated fatty acid ester of sorbitan, a phosphtidylcholine lecithin, phenoxytheanol, propylene glycol, and water.