(US9248103) It is an object of the present invention to provide a method for improving the solubility of a poorly-soluble substance, which is capable of increasing the solubility of substantially all poorly-soluble substances. This is a method comprising coating the surface of a poorly-soluble substance particle with microparticles of a calcium compound such as calcium phosphate or calcium carbonate, and at least one selected from a pH adjuster and a surfactant, by applying mechanical energy thereto.
(US9248103) The invention claimed is: 1. A method of making a coated substance comprising: providing an active substance with poor water solubility; providing hydroxyapatite microparticles; providing microparticles of a pH adjuster or surfactant as a powder with a particle diameter of 150 mu m or less; applying mechanical energy to a combination of said active substance and said hydroxyapatite microparticles to form a recovered substance; applying mechanical energy to a combination of said recovered substance and said microparticles of a pH adjuster or surfactant to produce a coated substance, wherein the microparticles of the pH adjuster or surfactant are present in an amount of 1/100 to 3 times the amount of the poorly soluble substance; and wherein the coated substance has improved water solubility as compared with the poorly water soluble substance by itself. 2. The method of claim 1, wherein the amount of the surfactant used is 1% to 300% by mass with respect to the poorly water soluble substance. 3. The method of claim 1, wherein the method of applying mechanical energy to the combination of said active substance and said hydroxyapatite microparticles to form a recovered substance is a method involving mechanical fusion. 4. The method of claim 1, wherein the method of applying mechanical energy to the combination of said active substance and said hvdroxvapatite microparticles to form a recovered substance is a method involving hybridization. 5. The method of claim 1, wherein the mean particle diameter of the hydroxyapatite microparticles is 100 mu m or less. 6. The method of claim 5, wherein the mean particle diameter of the calcium compound microparticles is 50 to 200 nm. 7. The method of claim 1, wherein the pH adjuster is selected from the group consisting of disodium hydrogen phosphate, L-arginine, sodium hydrogen carbonate, citric acid, and sodium dihydrogen phosphate. 8. The method of claim 1, wherein the surfactant is sodium dodecyl sulfate. 9. The method of claim 1, wherein the poorly water soluble substance is selected from the group consisting of a pharmaceutical active agent, a veterinary pharmaceutical a cosmetic, an agricultural chemical, and a food additive. 10. A method of claim 1, wherein the poorly water soluble substance is selected from the group consisting of tolbutamide, bezafibrate, famotidine, trimethoprim, probucol, sulpiride, lidocaine, alacepril, erythromycin, and haloperidol. 11. The method of claim 1, wherein the method of applying mechanical energy to the combination of said recovered substance and said microparticles of a pH adjuster or surfactant to produce a coated substance is a method involving hybridization. 12. The method of claim 1, wherein the method of applying mechanical energy to the combination of said recovered substance and said microparticles of a pH adjuster or surfactant to produce a coated substance is a method involving mechanical fusion. 13. The method of claim 1, wherein the method of applying mechanical energy to the combination of said recovered substance and said microparticles of a pH adjuster or surfactant to produce a coated substance is a method involving mechanical fusion or hybridization. 14. The method of claim 1, wherein the method of applying mechanical energy to the combination of said active substance and said hydroxyapatite microparticles to form a recovered substance is a method involving mechanical fusion or hybridization.
(US9248103) LEGAL DETAILS FOR US2015010638 Actual or expected expiration date=2033-02-21 Legal state=ALIVE Status=GRANTED Event publication date=2013-02-21 Event code=US/APP Event indicator=Pos Event type=Examination events Application details Application country=US US14380442 Application date=2013-02-21 Standardized application number=2013US-14380442 Event publication date=2013-02-21 Event code=US/EXMR Event type=Administrative notifications USPTO Examiner Name Primary Examiner: SHOMER, ISAAC Event publication date=2013-02-21 Event code=US/ART Event type=Administrative notifications USPTO Art Group ART=1612 Event publication date=2013-02-21 Event code=US/ENT Event type=Administrative notifications Entity Status Set to Undiscounted Business Entity Status: UNDISCOUNTED Event publication date=2013-02-21 Event code=US/AIA Event type=Administrative notifications First Inventor File Indicated: AIA=No Event publication date=2013-02-21 Event code=US/DK Event type=Examination events Attorney Docket Number Docket Nbr: 14119-105049 Event publication date=2013-02-21 Event code=US/CUST Event type=Examination events Attorney/Agent Customer Number Customer Nbr: 65989 Event publication date=2014-08-22 Event code=US/AS Event type=Change of name or address Event type=Reassignment Assignment Effective date of the event=2014-06-19 ASSIGNMENT OF ASSIGNORS INTEREST ASSIGNORS:SAKUMA, SHUJI KIKUKAWA, KEIICHIRO MIYASAKA, RYOSUKE REEL/FRAME:033589/0958 Event publication date=2014-08-22 Event code=US/PTARDY Event indicator=Pos Event type=Examination events Patent Term Adjustment - 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Examiner Initiated - telephonic Event publication date=2015-06-01 Event code=US/EXIE Event type=Examination events Event type=OAO Event type=INT Interview Summary - Examiner Initiated Event publication date=2015-06-18 Event code=US/CTNF Event type=Examination events Event type=OA Event type=OAO Non-Final Rejection Event publication date=2015-07-08 Event code=US/INVSUM Event type=Examination events Event type=OAI Event type=INT Interview Summary- Applicant Initiated Event publication date=2015-07-08 Event code=US/INVSUM Event type=Examination events Event type=OAI Event type=INT Interview Summary- Applicant Initiated Event publication date=2015-08-25 Event code=US/IDS Event type=Examination events Event type=OAI Information Disclosure Statement Filed Event publication date=2015-09-22 Event code=US/CTNFR Event type=Examination events Event type=OAI Response after Non-Final Action Event publication date=2015-11-09 Event code=US/EXET Event type=Examination events Event type=OAO Event type=INT Interview Summary - Examiner Initiated - telephonic Event publication date=2015-11-10 Event code=US/EXAC Event type=Examination events Event type=OAO Examiner's Amendment Communication Event publication date=2015-11-17 Event code=US/NOAM Event indicator=Pos Event type=Examination events Event type=OAO Mail Notice of Allowance Event publication date=2015-12-28 Event code=US/APRDY Event indicator=Pos Event type=Examination events Application Is Considered Ready for Issue Event publication date=2016-01-13 Event code=US/PAT Event indicator=Pos Event type=Event indicating In Force Patented Case Event publication date=2016-01-13 Event code=US/ISSM Event indicator=Pos Event type=Examination events Event type=OAO Event type=Restitution or restoration Issue Notification Mailed Event publication date=2016-02-02 Event code=US/B2 Event indicator=Pos Event type=Event indicating In Force Granted patent as second publication Publication country=US Publication number=US9248103 Publication stage Code=B2 Publication date=2016-02-02 Standardized publication number=US9248103
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