Method for preparing rapidly disintegrating formulation for oral administration

Abstract

A method and packaging machine for preparing rapidly disintegrating formulations for oral administration are disclosed. The present invention is characterized in that a powdery mixture including a pharmaceutically active ingredient and a sugar or a sugar alcohol powder is filled into a packaging material and, thereafter, the mixture, filled in the packaging material, is heated. The present invention can simply and economically prepare an oral formulation which undergoes rapid disintegration in the oral cavity and provides for high-quality administration to patients.

1 . A method for preparing a rapidly disintegrating formulation for oral administration, which comprises:
 mixing a pharmaceutically active ingredient with a sugar or a sugar alcohol powder to obtain a powdery mixture, and filling the powdery mixture into a packaging material; and   heating the mixture filled in the packaging material obtained in said mixing a pharmaceutically active ingredient to cure the mixture.   
     
     
         2 . The method of  claim 1 , wherein, said mixing a pharmaceutically active ingredient, the powdery mixture after filled is tamped. 
     
     
         3 . The method of  claim 1 , wherein the packaging material used in said mixing a pharmaceutically active ingredient is a lower pocket film which functions as a lower mold. 
     
     
         4 . The method of  claim 3 , which, after said heating the mixture, further comprises covering the lower pocket film with an upper cover film. 
     
     
         5 . The method of  claim 1 , wherein, in heating the mixture, the filled mixture is heated at a temperature ranging from 200 to 1,000□ for a period of 1 to 60 seconds. 
     
     
         6 . The method of  claim 5 , wherein the heating of the filled mixture is performed by radiant heating. 
     
     
         7 . The method of  claim 1 , wherein the pharmaceutically active ingredient used in step said mixing a pharmaceutically active ingredient is an antifebrile agent, an analgesic agent, an anti-inflammatory agent, an anti-gastric ulcer agent, an cardiovascular agent, a vasodilant, an antibiotic, an antitussive, an antiasthmatic, an antiemetic, a stomach function-regulating agent, an impotence-treating agent, a dementia-treating agent, a benign prostatic hyperplasia-treating agent, a migrain-treating agent, a psychostimulant, an antibacterial agent, an antihistamine, an oral antidiabetic, an allergy-treating agent, a contraceptive, a vitamin, an anticoagulant, a muscle-relaxing agent, a cerebral metabolism-improving agent, an antidiuretic, an anticonvulsant, a Parkinson disease-treating agent, an antipsychotic agent, or a mixture thereof. 
     
     
         8 . The method of  claim 1 , wherein the pharmaceutically active ingredient used in said mixing a pharmaceutically active ingredient is selected from the group consisting of tramadol, ibuprofen, dexibuprofen, aspirin, acetaminophen, indomethacin, sodium diclofenac, ketoprofen, isopropyl antipyrine, phenacetin, flurbiprofen, phenyl butazone, etodolac, celecoxib, etoricoxib, cimetidine, famotidine, ranitidine, nizatidine, roxatidine, nifedipine, amlodipine, verapamil, captopril, diltiazem HCl, propranolol, oxprenolol, nitroglycerin, enalapril, ampicillin, amoxicillin, cephalexin, cefuroxime, cefdinir, cefadroxil, cefprozil, cefpodoxime, cefditoren, cefaclor, cefixime, cefradine, loracarbef, ceftibuten, cefatrizin, cefcarpen, erythromycins, tetracyclines, quinolones, theophylline, aminopyrine, codeine phosphate, methylephedrine HCl, dextromethorphan, noscapine, salbutamol, ambroxol, clenbuterol, terbutaline, montelukast, ondansetron, metoclopramide, domperidone, trimebutine maleate, cisapride, levosulpiride, sildenafil, vadenafil, tadalafil, udenafil, donepezil, galantamine, rivastigmine, acetyl carnitine, memantine, zaliprodene, tamsulosin, sumatriptan, zolmitriptan, rizatriptan, loratadine, fexofenadine, glimepiride, torsemide, furosemide, gabapentine, pregavalin, valproate, topiramate, carbamazepine, lamotrigine, oxcarbazepine, selegiline, risperidone, ziprasidone, quetiapine, olanzapine, clozapine, paliperidone, a pharmaceutically acceptable salt thereof, and a mixture thereof. 
     
     
         9 . The method of  claim 1 , wherein the pharmaceutically active ingredient used in said mixing a pharmaceutically active ingredient is employed in an amount ranging from 0.01 to 90% by weight based on the total weight of the powdery mixture. 
     
     
         10 . The method of  claim 1 , wherein the sugar or sugar alcohol used in said mixing a pharmaceutically active ingredient is selected from the group consisting of lactose, glucose, sucrose, fructose, mannitol, sorbitol, xylitol, erythritol, ribulose, maltitol, maltose, maltodextrin, paratinose, trehalose, dextrose, and a mixture thereof. 
     
     
         11 . The method of  claim 1 , wherein the sugar or sugar alcohol used in said mixing a pharmaceutically active ingredient is employed in an amount ranging from 10 to 99.99% by weight based on the total weight of the powdery mixture. 
     
     
         12 . The method of  claim 1 , wherein the powdery mixture of said mixing a pharmaceutically active ingredient further comprises a pharmaceutically acceptable additive selected from the group consisting of a low temperature-melting binding agent, a disintegrator, a lubricant, an excipient, and a mixture thereof. 
     
     
         13 . The method of  claim 12 , wherein the pharmaceutically acceptable additive is employed in an amount ranging from 0.01 to 50 parts by weight based on 100 parts by weight of the powdery mixture. 
     
     
         14 . The method of  claim 12 , wherein the low temperature-melting binding agent is selected from the group consisting of polyethylene glycol, poloxamer, HCO, glycerine, propylene glycol, glycerides, a derivative thereof, and a mixture thereof. 
     
     
         15 . The method of  claim 12 , wherein the disintegrator is selected from the group consisting of cross-linked polyvinylpyrrolidone, cross-linked carboxymethylcellulose, sodium starch glycolate, calcium carboxymethylcellulose, and a mixture thereof.