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(12) Patent Application Publication (10) Pub. No.: US 2014/0328917 A1 Tada Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2014/0328917 A1 Tada Et Al US 20140328917A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2014/0328917 A1 Tada et al. (43) Pub. Date: Nov. 6, 2014 (54) ORGANIC COMPOUND NANO-POWDER, BO2C23/8 (2006.01) METHOD FOR PRODUCING THE SAME AND A63/67 (2006.01) SUSPENSION A63L/92 (2006.01) A613 L/405 (2006.01) (71) Applicant: Activus Pharma Co., Ltd., A613 L/4I (2006.01) Funabashi-shi, Chiba (JP) A 6LX3/573 (2006.01) A613 L/7048 (2006.01) (72) Inventors: Takahiro Tada, Funabashi-shi (JP); A63L/96 (2006.01) Kazuhiro Kagami, Funabashi-shi (JP): (52) U.S. Cl. Shiro Yokota, Funabashi-shi (JP) CPC ........... A61 K9/1682 (2013.01); A61 K3I/7048 (2013.01); A61 K3I/445 (2013.01); A61 K (21) Appl. No.: 14/001,645 3 1/57 (2013.01); A61 K3I/I2 (2013.01); A61 K 31/196 (2013.01); A61K 31/167 (2013.01); (22) PCT Filed: May 11, 2013 A6 IK3I/192 (2013.01); A61 K3I/405 (86). PCT No.: PCT/UP2013/003023 (2013.01); A61 K3I/41 (2013.01); A61 K 31/573 (2013.01); B02C 23/18 (2013.01) S371 (c)(1), USPC 424/489: 514/27: 514/317; 514/179; 514/29: (2), (4) Date: Aug. 26, 2013 514/679:514/567; 514/629; 514/570; 514/31; 514/.420, 514/382: 514/180; 24.1/15 (30) Foreign Application Priority Data (57) ABSTRACT May 11, 2012 (JP) ................................. 2012-108.972 An organic compound nano-powder comprising a granular organic compound with an average particle diameter of 500 Publication Classification nm or less and a 90%-diameter of less than 1500 nm and a carbohydrate compound comprising at least any one of a (51) Int. Cl. Sugar and a Sugar alcohol and with amount of 0.3 times or A6 IK 9/16 (2006.01) more by mass relative to amount of the organic compound, a A6 IK3I/445 (2006.01) method for producing the same, and a Suspension having the A 6LX3/57 (2006.01) organic compound dispersed in a liquid dispersion medium in A6 IK3I/2 (2006.01) which the organic compound is insoluble or poorly soluble. US 2014/0328917 A1 Nov. 6, 2014 ORGANIC COMPOUND NANO-POWDER, 0006. In accordance with recent development of a nano METHOD FOR PRODUCING THE SAME AND technology, the preparation of the nano-sized organic com SUSPENSION pound to satisfy the requirements as mentioned above has attracted high attention. For example, a particulate formula CROSS REFERENCE TO RELATED tion which contains a steroid or a steroid derivative with APPLICATION median of the particle distribution in the range of 0.005 to 5 um and with the 90%-diameter of 10 um or less has been 0001. The present patent application claims priority from known (for example, see Patent Document 1). However, the Japanese Patent Application No. 2012-108972 filed in Japan coarse particles present with a small percentage in the par on May 11, 2012, and the disclosures of thereof are incorpo ticulate formulation due to so wideness of the particle diam rated herein by reference. In addition, the disclosures of the eter distribution causes a problem of instability of a suspen patents, patent applications and documents cited in the sion thereof, i.e., a problem of low dispersivity of the present application are incorporated herein by reference. particulate formulation. 0007 For example, as one of methods for finely-milling TECHNICAL FIELD the organic compound to the level of nano-powder with a 0002 The present invention relates to an organic com narrow particle diameter distribution, a method for milling pound nano-powder, a method for producing the same, and a the organic compound by a bead mill using beads made of Suspension having an organic compound dispersed therein. ceramic, glass, or the like is well known (for example, see Patent Document 2). Nano-powder with a narrow particle BACKGROUND ART diameter distribution can be obtained by applying such a 0003. In order to fulfill an inherent function of an active mechanical impact or a grinding force to the particles of the ingredient contained in a formulation or a health food without organic compound. In addition, a wet milling method for excessively taking it, it is necessary to enhance the bioavail milling the organic compound in organic liquid using salt ability for the formulation or the health food. Taking the particles as a milling medium is also known (for example, see formulation as an example, while an oral formulation has the Patent Documents 3 and 4). The method using salt particles is advantages of being convenient and causing little distress more advantageous than the method using the beads in view compared to an injectable formulation, it has the disadvan of less contamination with impurities coming from a milling tage of providing low bioavailability. The oral formulation medium. While the impurities coming from the beads are enters into the intestine via the stomach and the duodenum, is difficult to remove, the impurities coming from the Salt par absorbed into blood mainly through the intestinal tract and ticles are easy to remove by a water-washing process (also then is delivered to the liver via the portal vein. A part of the called salt-removing process) due to high water Solubility of oral formulation is decomposed by undergoing the action of a salt. gastric acid or the like or being metabolized in the liver during passing through Such a long path, whereby converted into a PRIOR ART PUBLICATIONS totally different substance. One of the major reasons for the Patent Documents low bioavailability is that the oral formulation is difficult to be absorbed from digestive organs like the intestine. In order to 0008 Patent Document 1: Japanese Patent Laid-Open enhance the bioavailability for the formulation, it is necessary Publication No. 2006-089386 to get the size down of the organic compound with medicinal 0009 Patent Document 2: Japanese Patent Laid-Open ingredients to a level required to facilitate the absorption of Publication No. HO4-29.5420 the compound from the digestive organs into the blood. 0010 Patent Document 3: International Publication 0004. In the case of the injectable formulation, a typical WO/2008/126,797 example of parenteral formulations, effective functioning of a 0011 Patent Document 4: International Publication medicinal ingredient in the formulation requires the reaching WOf2O1 O/O32434 of the medicinal ingredient through blood vessels in the body to a target site. The inner diameter of a capillary blood vessel, SUMMARY OF INVENTION which is the narrowest among the blood vessels, is about 5 um. Accordingly, in order to make pass the organic compound Problem to be Solved by the Inventions with the medicinal ingredient through the capillary blood 0012. The wet milling method using the salt particles as vessel without causing occlusion, the particle diameter of this milling medium is advantageous in view of avoiding contami organic compound needs to be 5 um or less. Further, for the nation of irremovable impurities, but needs furthermore same reason as the oral formulation, it is necessary for a improvements. One of the improvements is to perform the health food to get the size down of the organic compound with production process as simple as possible with no water-wash active ingredients to a level required to facilitate the absorp ing to remove the salt that contaminates an organic compound tion of the compound from the digestive organs into the after milling. When the salt particles are used as milling blood. medium, usually the salt with the amount of preferably 10 to 0005. In the case of a solid skin-lightening ingredient and 30 times by mass relative to the organic compound to be a moisturizing ingredient contained in a cosmetic, less milled is served into a wet milling apparatus. Unless thus agglomeration and the Smaller particle size are required in large amount of salt is not removed after milling, the organic order to make them easily attached and thinly spread on a skin compound after milling cannot be safely used in or on a living surface while if it is in the form of a milky lotion, not to cause body. Another of improvements is to prevent the wet milling phase separation in a container in which this cosmetic is apparatus from rusting out. Contamination due to rust must be contained so that a uniform dispersion state may be Sustain definitely avoided when the organic compound is used in a able. living body. Use of an anti-rust agent as a general anti-rusting US 2014/0328917 A1 Nov. 6, 2014 method is also well known, but contact thereof with the ericin B, diclofenac sodium, indomethacin, felbinac, pran organic compound is not also allowed. Alternatively, a wet lukast hydrate, dexamethasone and fenofibrate. milling apparatus which is constructed by a material difficult 0024. One embodiment according to the present invention to rust (for example, a personally-ordered apparatus which is is a Suspension having at least an organic compound, which is coated with a ceramic on its inner Surface) may be opted, but contained in the organic compound nano-powder according the apparatus is disadvantageous in view of high cost due to to any one of the above-mentioned, dispersed in a liquid use of a special apparatus. dispersion medium in which the organic compound is 0013 The present invention was made to satisfy the insoluble or poorly soluble. requirements as mentioned above and has an object to provide 0025. One embodiment according to the present invention an organic compound nano-powder conveniently, with low is a method for producing an organic compound nano-powder cost and with less contamination of impurities to be removed.
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