Composition comprising lidocaine, l-carnosine and dexpanthenol

Patent metadata

Field	Value
Publication number	US-11903992-B2
Application number	US-202217650664-A
Country	US
Kind code	B2
Filing date	Feb 10, 2022
Priority date	Jan 23, 2021
Publication date	Feb 20, 2024
Grant date	Feb 20, 2024

Abstract

The present disclosure provides a composition comprising Lidocaine or salt or hydrate or solvate thereof, L-Carnosine or salt or hydrate or solvate thereof and dexpanthenol or salt or hydrate or solvate thereof. The composition may further comprise one or more other active agents. In an embodiment, the composition is formulated as an oral formulation. The compositions of the present disclosure may find utility in treatment of oral mucositis, ulcers, ulcer mediated pain and the like conditions. Aspects of the present disclosure also relates to method of treating oral, pharyngeal, oropharyngeal and esophageal diseases or conditions using the advantageous compositions of the present disclosure.

First claim

What is claimed is:

1. A composition comprising: lidocaine, or a salt or a hydrate or a solvate thereof, L-Carnosine, or a salt or a hydrate or a solvate thereof; and dexpanthenol; or a salt or a hydrate or a solvate thereof, wherein said composition is formulated as an oral formulation; and wherein the composition further comprises at least one excipient that is a fatty acid derivative selected from a group consisting of diglyceryl lauryl fumarate, diglyceryl lauryl succinate, diglyceryl capryl succinate, and any combination thereof.

2. The composition of claim 1 , wherein the composition comprises lidocaine, or a salt or a hydrate or a solvate thereof; L-Carnosine, or a salt or a hydrate or a solvate thereof, and dexpanthenol; or a salt or a hydrate or a solvate thereof; in a weight ratio ranging from 1:1:1 to 7:1:20.

3. The composition of claim 1 , wherein the composition comprises, or a salt or a hydrate or a solvate thereof, L-Carnosine, or a salt or a hydrate or a solvate thereof; and dexpanthenol; or a salt or a hydrate or a solvate thereof, in a weight ratio ranging from 1:1:1 to 5:1:10.

4. The composition of claim 1 , wherein the composition further comprises at least one additional excipient.

5. The composition of claim 1 , wherein the composition further comprises at least one other active agent.

6. The composition as claimed in claim 4 , wherein the at least one additional excipient is selected from a group consisting of a diluent, an antioxidant, a preservative, a solvent, a flavoring agent, a sweetener, a fatty acid or derivative thereof, an amino acid or metabolite or derivative thereof, a vitamin, a surfactant, a solubilizer, a stabilizer, and any combination thereof.

7. The composition as claimed in claim 5 , wherein the at least one other active agent is selected from a group consisting of benzocaine, clonidine, bupivacaine, ropivacaine, mepivacaine, morphine, fentanyl, orthoform, levo-bupivacaine, bibucaine, prilocaine, acetaminophen, procaine, diphenhydramine, polaprezinc, benzydamine, pentoxifylline, ortetracaine, ketamine, misoprostol, amifostine, palifermin, chlorhexidine gluconate, dusquetide, melatonin, indraline, androstenetriol, actovegin, rebamipide, EC-18, brilacidin, validive, streptomycin, kanamycin, neomycin, gentamicin, betamethasone, betamethasone esters, clobetasol, clobetasol propionate, clobetasone, clocortolone, clocortolone esters, dexamethasone, dexamethasone esters, diflorasone, diflucortolone, diflucortolone valerate, fluclorolone, flumetasone, fluocortin, fluocortolone, fluocortolone esters, fluprednidene acetate, fluticasone, fluticasone furoate, fluticasone propionate, halometasone, meprednisone, mometasone, mometasone furoate, ulobetasol, 2-mercaptoethane sodium sulphonate, 2-Mercaptoethylguanidine, methylprednisolone, beclomethasone dipropionate, fluocinonide, betamethasone sodium phosphate, prednisolone, colchicine, azathioprine, thalidomide, dapsone, mycophenolate mofetil, adalimumab, clofazimine, levamisole, hydrocortisone sodium succinate, montelukast, triamcinolone, sulodexide, α-Lipoic acid, cysteamine, folic acid, hydrolytic enzyme, mucotrol, traumeel, tretinoin, calcipotriene, calcitriol, ergosterol, 1α-hydroxycholecalciferol, vitamin D2, vitamin D3, ascorbic acid, calcium ascorbate, nicotinamide ascorbate, sodium ascorbate, α-carotene, β-carotene, δ-carotene, vitamin A, cobamamide, hydroxocobalamin, sodium folate, vitamin B12, menadiol, menadione, menadoxime, menaquinones, phylloquinone, vitamin K5, inositol, α-tocopherol, γ-tocopherol, vitamin E, zinc, selenium, potassium, copper, manganese, aluminum, zinc sulfate, magnesium, magnesium aluminum hydroxide, magnesium sulfate, calcium phosphate, magnesium stearate, magnesium silicate, magnesium chloride, magnesium bromide, magnesium acetate, magnesium lactate, magnesium pidolate, magnesium thiosulphate, Cu2+ salts, copper sulfate pentahydrate, copper sulfate, copper malonate, copper citrate, copper oxalate, copper tartarate, copper lactate, copper chloride, copper bromide, copper pidolate, copper phosphate, copper nitrate, copper thiosulphate, Al+3 salts, aluminum oxide, aluminum palmitate, aluminum stearate, aluminum chloride, aluminum oxychloride, aluminum barium silicate, Aluminum magnesium hydroxide stearate, aluminum propionate aluminum dipropionate, aluminum aceto propionate, aluminum citro propionate, aluminum lacto propionate, aluminum tartaro propionate, aluminum acetodipropionate, aluminum citrodipropionate, aluminum lacto dipropionate, aluminum tartarodipropionate, polymers, carbomer, methyl cellulose, sodium carboxyl methyl cellulose, carrageenan, colloidal silicon dioxide, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, polyethylene oxide, hyaluroinic acid, hydrated silica, hydroxypropyl chitosan, chitosan sulfate, ethyl cellulose, hydroxymethyl cellulose, carboxy methyl cellulose, chitosan pyrrolidone carboxylate, amphotericin B, benzoxonium chloride, chlorhexidine, chlortetracycline, clotrimazole, cetylpyridinium chloride, domiphen bromide, amoxicillin, cephalexin, ciprofloxacin, clindamycin, azithromycin, sulfamethoxazole, trimethoprim, clavulanate, levofloxacin, doxycycline, eugenol, hexetidine, hydrogen peroxide, mepartricin, metronidazole, miconazole, minocycline, natamycin, oxyquinoline, polynoxylin, sodium perborate, tetracycline, tibezonium iodide, amlexanox, acetylsalicylic acid, becaplermin, epinephrine, adrenalone, triclosan, mycophenolic acid, cyclosporines, leflunomide, teriflunomide, ciclosporin, pimecrolimus, tacrolimus, voclosporin, lenalidomide, pomalidomide, sirolimus, everolimus, ridaforolimus, temsirolimus, umirolimus, zotarolimus, baricitinib, blisibimod, nilotinib, filgotinib, tofacitinib, upadacitinib, abatacept, belatacept, etanercept, pegsunercept, aflibercept, alefacept, rilonacept, glyceryl trinitrate, isosorbide dinitrate, isosorbide mononitrate, isoamyl nitrite, apremilast, arofylline, atizoram, benafentrine, catramilast, CC-1088, CDP-840, CGH-2466, cilomilast, cipamfylline, crisaborole, denbutylline, difamilast, drotaverine, etazolate, filaminast, glaucine, HT-0712, ICI-63197 indimilast, irsogladine, lavamilast, lirimilast, lotamilast, luteolin, mesembrenone, mesembrine, mesopram, oglemilast, piclamilast, pumafentrine, revamilast Ro 20-1724, roflumilast, rolipram, ronomilast, RPL-554, RS-25344, tetomilast, tofimilast, YM-976, zardaverine, ibudilast, roflumilas, adibendan, amrinone, anagrelide, bucladesine, carbazeran, cilostamide, cilostazol, enoximone, imazodan, KMUP-1, meribendan, milrinone, olprinone, parogrelil, pimobendan, quazinone, siguazodan, trequinsin, vesnarinone, pde 5 inhibitors, acetildenafil, aildenafil, avanafil, beminafil, benzamidenafil, dasantafil, icariin, gisadenafil, homosildenafil, lodenafil, mirodenafil, MY-5445, nitrosoprodenafil, norcarbodenafil, SCH-51866, sildenafil, sulfoaildenafil, T-0156, tadalafil, udenafil, vardenafil, abrocitinib, momelotinib, oclacitinib, peficitinib, ruxolitinib, tasocitinib, CP-690550, atiprimod, AZD-1480, CHZ868, cucurbitacin I, CYT387, lestaurtinib, NSC-7908, NSC-33994, pacritinib, SD-1008, cercosporamide, decernotinib, TCS-21311, WHI-P 15 ZM-39923, ZM-449829, methotrexate, diclofenac, indomethacin, sulindac, mefenamic acid, piroxicam, ibuprofen, ketoprofen, naproxen, phenylbutazone, meloxicam, nimesulide, celecoxib, etoricoxib WBI-1001, MRX-6, valdecoxib, and any mixture thereof.

8. The composition of claim 1 , wherein the composition is formulated as an oral rinse formulation.

9. The composition of claim 1 , wherein the composition comprises
lidocaine or a salt or a hydrate or a solvate thereof in an amount ranging from 0.25% w/v to 10% w/v;
L-Carnosine or a salt or a hydrate or a solvate thereof in an amount ranging from 0.25% w/v to 5% w/v;
dexpanthen

Assignees

• Cellix Bio Private Ltd

Inventors

• Kandula Mahesh

Classifications

• A61K38/05 Primary

  Dipeptides · CPC title

• A61K9/006

  Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays · CPC title

• A61K31/164

  of a carboxylic acid with an aminoalcohol, e.g. ceramides · CPC title

• A61K31/167

  having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol · CPC title

• A61K31/728 Primary

  Hyaluronic acid · CPC title