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(12) Patent Application Publication (10) Pub. No.: US 2011/0212169 A1 Bae Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2011/0212169 A1 Bae Et Al US 2011 0212169A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0212169 A1 Bae et al. (43) Pub. Date: Sep. 1, 2011 (54) METHOD FOR PRODUCING POWDER A63/496 (2006.01) CONTAINING NANOPARTICULATED A63L/439 (2006.01) SPARINGLY SOLUBLE DRUG, POWDER A6II 3L/26 (2006.01) PRODUCED THEREBY AND A63L/92 (2006.01) PHARMACEUTICAL COMPOSITION A6IP 700 (2006.01) CONTAINING SAME (ASAMENDED) A6IP37/06 (2006.01) A6IPI/00 (2006.01) (75) Inventors: Joon-Ho Bae, Gyeonggi-do (KR): A6IP3 L/10 (2006.01) Hyeok Lee, Gyeonggi-do (KR): A6IP3/06 (2006.01) Deok-Ki Hong, Gyeonggi-do (KR): B29B 9/12 (2006.01) Jong-Hwi Lee, Seoul (KR) (52) U.S. Cl. ... 424/451; 424/400; 424/464; 514/254.07; (73) Assignee: Amorepacific Corporation, 514/291; 514/543; 514/568; 264/11 Yongsan-gu (KR) (57) ABSTRACT (21) Appl. No.: 13/127,957 Disclosed are a method for preparing a powder containing a nanoparticulated sparingly soluble drug, a powder prepared (22) PCT Filed: Nov. 10, 2009 thereby, and a pharmaceutical composition containing the same. The disclosed method includes: providing a uniformly (86). PCT No.: dispersed solution of a sparingly soluble drug which is formed into nanoparticles in the presence of a Surface stabi S371 (c)(1), lizer, mixing the uniformly dispersed solution with a water (2), (4) Date: May 5, 2011 soluble dispersant solution; and drying the mixed solution to obtain the powder. (30) Foreign Application Priority Data When the powder containing the nanoparticulated sparingly Nov. 10, 2008 (KR) .......................... 102O080111205 soluble drug obtained by the disclosed method is redispersed in an aqueous solution, the sparingly soluble drug Publication Classification retains aparticle size in the nano scale while the solubility and (51) Int. Cl. the dissolution rate of the drug are increased, thereby provid A6 IK 9/14 (2006.01) ing enhanced bioavailability. Consequently, the present dis A6 IK 9/48 (2006.01) closure can be useful in the development of preparations of a A6 IK 9/20 (2006.01) sparingly soluble drug for oral or parenteral administration. Patent Application Publication Sep. 1, 2011 Sheet 1 of 3 US 2011/0212169 A1 Figure 1) Diameter (m) Figure 2a) Patent Application Publication Sep. 1, 2011 Sheet 2 of 3 US 2011/0212169 A1 Figure 2b Figure 3a) Patent Application Publication Sep. 1, 2011 Sheet 3 of 3 US 2011/0212169 A1 (Figure 3b) US 2011/0212169 A1 Sep. 1, 2011 METHOD FOR PRODUCING POWDER 0011. The sparingly soluble drug may be at least one CONTAINING NANOPARTICULATED selected, for example, from: a nonsteroidal anti-inflammatory SPARINGLY SOLUBLE DRUG, POWDER drug including acetaminophen, acetylsalicylic acid, ibupro PRODUCED THEREBY AND fen, fenbuprofen, fenoprofen, flurbiprofen, indomethacin, PHARMACEUTICAL COMPOSITION naproxen, etodolac, ketoprofen, dexibuprofen, piroXicam or CONTAINING SAME (ASAMENDED) aceclofenac; an immunosuppressantoratopic dermatitis drug including cyclosporin, tacrolimus, rapamycin, mycopheno TECHNICAL FIELD late or pimecrolimus; a calcium channel blocker including nifedipine, nimodipine, nitrendipine, nilvadipine, felodipine, 0001. The present disclosure relates to a method for pre amlodipine or isradipine; an angiotensin II antagonist includ paring a powder containing a nanoparticulated sparingly ing Valsartan, eprosartan, irbesartan, candesartan, telmisar soluble drug, a powder prepared thereby, and a pharmaceuti tan, olmesartan or losartan; a cholesterol synthesis-inhibiting cal composition containing the same. hypolipidemic agent including atorvastatin, lovastatin, simv astatin, fluvastatin, rosuvastatin or pravastatin; a cholesterol BACKGROUND ART metabolism- and secretion-promoting hypolipidemic agent 0002. A sparingly soluble drug which is poorly soluble in including gemfibrozil, fenofibrate, etofibrate or bezafibrate; water or a pharmaceutical composition containing the same an antidiabetic drug including pioglitaZone, rosiglitaZone or may exhibit low bioavailability upon oral administration metformin; a lipase inhibitor including orlistat; an antifungal since it may be excreted before being absorbed in the gas agent including itraconazole, amphotericin B, terbinafine, trointestinal tract. nystatin, griseofulvin, fluconazole or ketoconazole; a hepato 0003. Furthermore, since it is difficult to be prepared for protective drug including biphenyl dimethyl dicarboxylate, parenteral administration Such as injection, various co-sol silymarin or urSodeoxycholic acid; a gastrointestinal drug vents or Surfactants have to be used, which may cause side including Sofalcone, omeprazole, pantoprazole, famotidine, effects or poor patient compliance. itopride or mesalazine; an antiplateletagent including cilosta 0004 Although there have been attempts to prepare a Zolor clopidogrel; an osteoporosis drug including raloxifene; nanoparticulated sparingly soluble drug in order to improve an antiviral drug including acyclovir, famciclovir, lamivudine solubility in water and bioavailability of the sparingly soluble or oseltamivir; an antibiotic including clarithromycin, cipro drug, it is still difficult to improve bioavailability since the floxacin or cefuroxime; an antiasthmatic or antihistamine nanoparticles tend to aggregate when they are redispersed in drug including pranlukast, budesonide or fexofenadine; a an aqueous Solution. hormone drug including testosterone, prednisolone, estrogen, cortisone, hydrocortisone or dexamethasone; an anticancer drug including paclitaxel, docetaxel, paclitaxel derivatives, DISCLOSURE doxorubicin, adriamycin, daunomycin, camptothecin, etopo Technical Problem side, teniposide or buSulfan; salts thereof, and pharmaceutical derivatives thereof. Specifically, it may be at least one 0005. The present disclosure is directed to providing a selected from naproxen, tacrolimus, Valsartan, simvastatin, method for preparing a powder containing a sparingly soluble fenofibrate, itraconazole, biphenyl dimethyl dicarboxylate, drug, capable of improving solubility in water and bioavail silymarin, Sofalcone, pantoprazole, cilostazol, salts thereof ability of the sparingly soluble drug. and pharmaceutical derivatives thereof. 0006. The present disclosure is also directed to providing 0012 For example, the surface stabilizer may be at least a powder containing a sparingly soluble drug, which is pre one selected from sodium dodecyl sulfate, dioctyl sodium pared by the method. SulfoSuccinate, lecithin, phospholipid, polyoxyethylene Sor 0007. The present disclosure is also directed to providing bitan fatty acid ester, potassium Sorbate, poloxamer, propy a pharmaceutical composition including the powder. lene glycol, methyl cellulose, ethyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, Technical Solution hydroxypropyl methylcellulose, carboxymethyl cellulose, 0008. In one general aspect, the present disclosure pro benzethonium chloride, benzalconium chloride, sorbic acid, vides a method for preparing a powder containing a nanopar potassium Sorbate, benzoic acid, sodium benzoate, propylpa ticulated sparingly soluble drug, including: providing a uni raben, methylparaben, polyvinyl alcohol, polyvinylpyrroli formly dispersed solution of a sparingly soluble drug which is done, alginic acid and sodium alginate. The Surface stabilizer formed into nanoparticles in the presence of a Surface stabi may be used in an amount of about 0.0001-90 wt % based on lizer, mixing the uniformly dispersed solution with a water the weight of the sparingly soluble drug. soluble dispersant solution; and drying the mixed solution to 0013 The uniformly dispersed solution may have an obtain the powder. apparent viscosity ranging from 1 to 100,000 centipoises. 0009. The water-soluble dispersant may be at least one 0014. In another general aspect, the present disclosure Selected from carageenan, gelatin, agar, alginic acid, arabi provides a powder containing a nanoparticulated sparingly noxylan gum, f-glucan, guar gum, arabia gum, locust bean soluble drug, comprising: a sparingly soluble drug which is gum, pectin, starch, Xanthan gum, casein, glucomannan, formed into nanoparticles in the presence of a Surface stabi cyclodextrin, methylcellulose, chitosan, Xyloglucan and glu lizer; and a water-soluble dispersant; when the powder is ten. Specifically, it may be carageenan. redispersed in an aqueous solution, 10 to 90% of the particles 0010. The water-soluble dispersant solution may have a based on a particle size normal distribution curve have a concentration of about 0.1-5 wt %, and the water-soluble particle size ranging from 10 to 1,000 nm. Specifically, the 10 dispersant Solution may be used in an amount of about 0.01 to 90% of the particles may have a particle size of about 10 to 0.1 wt % based on the weight of the sparingly soluble drug. 400 nm based on the particle size normal distribution curve. US 2011/0212169 A1 Sep. 1, 2011 0015. In another general aspect, the present disclosure dipine or isradipine; an angiotensin II antagonist including provides a pharmaceutical composition comprising the pow Valsartan, eprosartan, irbesartan, candesartan, telmisartan, der containing the nanoparticulated sparingly soluble drug. olmesartan or losartan; a cholesterol synthesis-inhibiting 0016 A formulation of the pharmaceutical composition hypolipidemic agent including atorvastatin, lovastatin, simv may be granule, powder, syrup, liquid, Suspension, tablet, astatin, fluvastatin, rosuvastatin or pravastatin; a cholesterol capsule, troche or pill for oral administration, or transdermal
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