Oral particle consisting of an amorphous structure and a submicron domain

Abstract

The present invention relates to compositions and methods of the preparation of an oral particle essentially consisting of an amorphous structure and a submicron domain, wherein both amorphous structure and submicron domain comprise a drug, and wherein the particle shows crystalline property. The desired ratio of the amorphous structure to the submicron domain is between 0.1:5 and 1:1. And, the desired average particle diameter is between mesh 12 (1680 microns) and mesh 100 (149 microns).

We claim: 
     
         1 . An oral solid particle essentially consisting of an amorphous structure and a submicron domain, wherein the amorphous structure comprises a drug and an amphiphilic polymer, wherein the submicron domain essentially consists of a drug, and wherein the ratio of the amorphous structure to the submicron domain is 0.1:5 to 1:1 
     
     
         2 . An oral solid particle essentially consisting of an amorphous structure and a submicron domain, wherein the amorphous structure comprises a drug and a polyvinylpyrrolidone, wherein the submicron domain essentially consists of a drug, and wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4, and wherein the average diameter of the oral particle is from mesh 20 to mesh 100. 
     
     
         3 . An oral solid particle essentially consisting of an amorphous structure and a submicron domain, wherein the amorphous structure comprises a drug and a polyvinylpyrrolidone, wherein the submicron domain essentially consists of a drug, wherein the ratio of the amorphous structure to the submicron domain is 1:50 to 1:4, wherein the average diameter of the submicron domain is about 100 nm, and wherein the average diameter of the oral particle is from mesh 20 to mesh 100. 
     
     
         4 . The oral particle as claimed in  claims 1 - 3 , wherein more than 30 parts water is needed to dissolve 1 part drug. 
     
     
         5 . The oral particle as claimed in  claims 1 - 3 , wherein more than 100 parts water is needed to dissolve 1 part drug. 
     
     
         6 . The oral particle as claimed in  claims 1 - 3 , wherein more than 1000 parts water is needed to dissolve 1 part drug. 
     
     
         7 . The oral particle as claimed in  claims 1 - 3 , wherein more than 10,000 parts water is needed to dissolve 1 part drug. 
     
     
         8 . The oral particle as claimed in  claim 3 , wherein the drug is selected from a group consisting of acetaminophen, alprazolam, atorvastatin calcium, betamethasone acetate, betamethasone benzoate, betamethasone dipropionate, betamethasone valerate, budesonide, buprenorphine hydrochloride, butoconazole nitrate, caffeine, calcitriol, carbamazepine, carprofen, celecoxib, cilostazol, clarithromycin, clobetasol Propionate, clofibrate, clopidogrel bisulfate, clotrimazole, dactinomycin, danazol, dapsone, desoximetasone, dexamethasone acetate, dextromethorphan, diazepam, efavirenz, erythromycin estolate, erythromycin ethylsuccinate, erythromycin, estradiol, ethinyl estradiol, ethotoin, ezetimibe, felodipine, fexofenadine hydrochloride, flurbiprofen, fluvoxamine maleate, gemfibrozil, haloperidol, ibuprofen, idarubicin hydrochloride, indapamide, indomethacin, isofluorophate, isotretinoin, ivermectin, lansoprazole, leflunomide, levonorgestrel, lidocaine, loratadine, lovastatin, medroxyprogesterone acetate, metaxalone, methocarbamol, nabumetone, naproxen, niacin, nifedipine, norethindrone acetate, omeprazole, oxandrolone, oxybenzone, oxymetholone, paclitaxel, perphenazine, phenobarbital, phenyloin, pimozide, pitavastatin, prednisolone, prednisolone tebutate, prochlorperazine, progesterone, propoxyphene napsylate, risperidone, ritonavir, lopinavir, and simvastatin. 
     
     
         9 . The oral particle as claimed in  claim 3 , wherein the drug is niacin. 
     
     
         10 . The oral particle as claimed in  claim 3 , wherein the drug is acetaminophen. 
     
     
         11 . The oral particle as claimed in  claim 3 , wherein the drug is metaxalone. 
     
     
         12 . The oral particle as claimed in  claim 3 , wherein the drug is clopidogrel bisulfate.