Quickly soluble oral film dosage containing steviosides as a unpleasant taste masking agent

Abstract

Disclosed is a quickly soluble oral film dosage for masking a nasty taste, in particular, a quickly soluble oral film dosage comprising a stevioside based sweetener and a high potency sweetener in a ratio by weight (w/w) of 1:3 to 3:1, which may efficiently mask a bitter or nasty taste of a medicine and may be quickly dissolved in a mouth without water, thereby improving an aftertaste thereof thus enhancing dosage acceptability of a patient.

1 . A quickly soluble oral film dosage, comprising:
 at least one water-soluble polymer; at least one active pharmaceutical ingredient; a stevioside based sweetener as an aftertaste enhancer; and at least one primary sweetening agent as a taste masking agent.   
     
     
         2 . The oral film dosage according to  claim 1 , wherein the stevioside based sweetener includes at least one selected from a group consisting of stevioside, enzyme degradable stevioside, rebaudioside A and products containing them with high contents. 
     
     
         3 . The oral film dosage according to  claim 1 , wherein the primary sweetening agent is at least one selected from a group consisting of aspartame, acesulfame salts, neotame, sucralose, thaumatine, saccharine, licorice extract, neohesperidin and moneyline. 
     
     
         4 . The oral film dosage according to  claim 1 , wherein the film contains 0.1 to 10 wt. % of the stevioside based sweetener and the primary sweetening agent, respectively, relative to the total weight of the quickly soluble film and wherein the stevioside based sweetener and the primary sweetening agent are contained in a relative ratio by weight (w/w) of 1:3 to 3:1. 
     
     
         5 . The oral film dosage according to  claim 1 , wherein the water-soluble polymer is at least one selected from a group consisting of pullulan, gelatin, pectin, low viscosity pectin, hydroxypropylmethyl cellulose, low viscosity hydroxylpropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, carboxymethyl cellulose, polyvinylalcohol, polyacrylic acid, methyl methacrylate copolymer, carboxyvinyl polymer, polyethyleneglycol, alginic acid, low viscosity alginic acid, sodium alginate, modified starch, casein, whey protein extract, soy protein extract, zein, levan, elsinan, gluten, acacia gum, carageenan, Arabic gum, guar gum, locust bean gum, xanthan gum, gellan gum and agar. 
     
     
         6 . The oral film dosage according to  claim 5 , wherein the water soluble polymer is at least one selected from a group consisting of pullulan, gelatin, low viscosity pectin, low viscosity alginic acid and low viscosity hydroxylpropylmethyl cellulose. 
     
     
         7 . The oral film dosage according to  claim 1 , wherein the active pharmaceutical ingredient is at least one selected from a group consisting of diabetic remedy; insomnia remedy;
 genito-urinary remedy; obesity remedy; enzyme; gastric ulcer remedy; cough remedy and expectorant; dermal disorder remedy; antinausea drug; antidepression drug; antihistamine drug; antipyretic, analgesic and antiphlogistic remedy; hormone drug; circulatory organ remedy; gastrointestinal remedy; psychoneurotic drug; impotency remedy; osteoporosis remedy; arthritis remedy; epilepsy remedy; muscle relaxing agent; cerebral function enhancer; schizophrenia remedy; immuno-suppression agent; antibiotic agent; anticancer agent; Supportives in tumor therapy; vaccine; oral cleanser; anemia remedy; constipation remedy; vitamin; nutrient; probiotic preparation; multi-symptom cold/flue medications; and health functional foods.   
     
     
         8 . The oral film dosage according to  claim 7 , wherein the active pharmaceutical ingredient is at least one selected from a group consisting of triclosan, cetylpyridium chloride, domiphen bromide, quaternary ammonium salt, zinc compounds, sanguinarine, fluoride, alexidine, octenidine, EDTA, aspirin, acetaminophen, ibuprofen, ketoprofen, diflunisal, fenoprofen calcium, naproxen, tolmetin sodium, indomethacin, benzonatate, caramiphen, edisylate, menthol, dextromethorphan hydrobromide, chlophedianol hydrochloride, diphenhydramine, pseudoephedrine hydrochloride, phenylephrine, phenylpropanolamine, pseudoephedrine sulfate, bromophenylamine maleate, chlorophenylamine maleate, carbinoxamine maleate, clemastine fumarate, dexchlorpheniramine maleate, diphenhydramine hydrochloride, diphenhydramine citrate, diphenylpyraline hydrochloride, doxylamine succinate, promethazine hydrochloride, pyrilamine maleate, tripelennamine citrate, triprolidine hydrochloride, acrivastine, loratadine, brompheniramine, dexbrompheniramine, guaifenesin, ipecac, calcium iodide, terpine hydrate, loperamide, famotidine, ranitidine, omeprazole, lansoprazole, aliphatic alcohol, nicotine, caffeine, strychnine, picrotoxin, pentylenetetrazol, phenylhydantoin, phenobarbital, primidone, carbamazepine, ethosuximide, methosuximide, phensuximide, trimethadione, diazepam, benzodiazepine, phenacemide, pheneturide, acetazolamide and sulthiame, bromide levodopa, amantadine, morphine, heroin, hydromorphone, methophone, oxymorphone, levorphanol, codeine, hydrocodone, xycodone, nalorphine, naloxone, naltrexone, salicylate, phenylbutazone, indomethacin, phenacetin, chloropromazine, methotrimeprazine, haloperidol, clozapine, reserpine, imipramine, tranylcypromine, phenelzine, lithium, apomorphine, sildenafil, tadalafil, vardenafil, ondansetron, donepezil, zolpidem tartrate, granisetron, montelukast, pholcodine, butylscopolamine, fentanyl citrate, oxycodone hydrochloride, buprenorphine hydrochloride, escitalopram oxalate, rivastigmine tartrate, esomeprazole magnesium, aripiprazole, zolmitriptan, rizatriptan benzoate, telmisartan, risperidone, benzocaine, cetirizine hydrochloride, bambuterol hydrochloride, galantamine hydrobromide, lercanidipine hydrochloride, paroxetine hydrochloride, meloxicam, tolterodine tartrate, doxazosin mesylate, and pharmaceutically available salts thereof. 
     
     
         9 . The oral film dosage according to  claim 8 , wherein one of the ondansetron salts is an ondansetron hydrochloride, and a quickly soluble film including the ondansetron hydrochloride as the active pharmaceutical ingredient has bioequivalence. 
     
     
         10 . The oral film dosage according to  claim 8 , wherein one of the montelukast salts is a montelukast sodium, and a quickly soluble film including the montelukast sodium as the active pharmaceutical ingredient has bioequivalence. 
     
     
         11 . The oral film dosage according to  claim 8 , wherein one of the sildenafil salts is a sildenafil citrate, and a quickly soluble film including the sildenafil citrate as the active pharmaceutical ingredient has bioequivalence. 
     
     
         12 . The oral film dosage according to  claim 1 , wherein the quickly soluble film further comprises at least one of additives. 
     
     
         13 . The oral film dosage according to  claim 12 , wherein the additives comprise at least one selected from a group consisting of a filler, a plasticizer, a secondary sweetening agent, an acidic agent, a flavor, an emulsifier, a pigment and a cooling agent. 
     
     
         14 . The oral film dosage according to  claim 13 , wherein the filler is at least one selected from a group consisting of microcrystalline cellulose, cellulose polymer, magnesium carbonate, calcium carbonate, limestone powder, silicate, clay, talc, titanium dioxide and calcium phosphate. 
     
     
         15 . The oral film dosage according to  claim 13 , wherein the plasticizer is at least one selected from a group consisting of sorbitol, maltitol, xylitol, glycerin, polyethyleneglycol, propyleneglycol, hydrogenated starch syrup, starch syrup, triacetin, glycerol oleate, sucrose fatty acid ester and double chain fatty acid. 
     
     
         16 . The oral film dosage according to  claim 13 , wherein the secondary sweetening agent is at least one selected from a group consisting of sugar, glucose, maltose, oligosaccharides dextrin, alpha cyclodextrin, beta cyclodextrin, gamma cyclodextrin, hydroxypropy beta cyclodextrin, methyle beta cyclodextrin, cluster dextrin, indigestible dextrin, hydrogenated indigestible dextrin, invert sugar, fructose, lactose, galactose, starch syrup, sorbitol, maltitol, xylitol, erythritol, hydrogenated starch syrup, mannitol and trehalose. 
     
     
         17 . The oral film dosage according to  claim 13 , wherein the acidic agent is at least one selected from a group consisting of citric acid, malic acid, fumaric acid, tartaric acid, ascorbic acid, succinic acid, adipic acid and lactic acid. 
     
     
         18 . The oral film dosage according to  claim 13 , wherein the flavor is a natural flavor, an artificial flavor or a mixture thereof. 
     
     
         19 . The oral film dosage according to  claim 13 , wherein the emulsifier is at least one selected from a group consisting of glycerin fatty acid ester, sucrose fatty acid ester, lecithin, enzyme treated lecithin, polysorbate, sorbitan fatty acid ester and propyleneglycol