Method for improving water solubility of slightly soluble substance 机翻标题: 暂无翻译,请尝试点击翻译按钮。

公开号/公开日
US2015010638 A1 2015-01-08 [US20150010638]US9248103 B2 2016-02-02 [US9248103] / 2015-01-082016-02-02
申请号/申请日
2013US-14380442 / 2013-02-21
发明人
SAKUMA SHUJI;KIKUKAWA KEIICHIRO;MIYASAKA RYOSUKE;
申请人
SANGI;
主分类号
IPC分类号
A01N-025/00A01N-025/26A23L-029/00A61K-008/02A61K-008/19A61K-008/24A61K-008/44A61K-008/46A61K-008/67A61K-009/14A61K-009/16A61K-009/50A61K-031/10A61K-031/167A61K-031/18A61K-031/195A61K-031/40A61K-031/426A61K-031/4515A61K-031/505A61K-031/7048A61Q-019/00B05D-003/12B05D-005/04
摘要
(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.
机翻摘要
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地址
代理人
代理机构
;
优先权号
2012JP-0047399 2012-03-02 2013WO-JP01000 2013-02-21
主权利要求
(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.
法律状态
(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 - Ready for Examination    Event publication date=2014-08-22  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2014-08-22  Event code=US/ENT  Event type=Administrative notifications  Entity Status Set to Undiscounted    Event publication date=2014-09-29  Event code=US/APPFILEREC  Event type=Administrative notifications  Event type=OAO  Filing Receipt    Event publication date=2014-09-29  Event code=US/M903  Event indicator=Pos  Event type=Examination events  Event type=OAO  Notice of DO/EO Acceptance Mailed    Event publication date=2014-10-28  Event code=US/DOCK  Event indicator=Pos  Event type=Examination events  Case Docketed to Examiner    Event publication date=2014-11-18  Event code=US/RESTREQ  Event type=Examination events  Event type=Corrections  Event type=OAO  Restriction/Election Requirement    Event publication date=2015-01-08  Event code=US/A1  Event type=Examination events  Application published  Publication country=US  Publication number=US2015010638  Publication stage Code=A1  Publication date=2015-01-08  Standardized publication number=US20150010638     Event publication date=2015-01-08  Event code=US/PGPUBN  Event indicator=Pos  Event type=Examination events  Event type=OAO  PG-Pub Issue Notification    Event publication date=2015-01-20  Event code=US/ELC  Event type=Examination events  Event type=OAI  Response to Election / Restriction Filed    Event publication date=2015-01-20  Event code=US/IDS  Event type=Examination events  Event type=OAI  Information Disclosure Statement Filed    Event publication date=2015-01-28  Event code=US/CTNF  Event type=Examination events  Event type=OA  Event type=OAO  Non-Final Rejection    Event publication date=2015-04-22  Event code=US/CTNFR  Event type=Examination events  Event type=OAI  Response after Non-Final Action    Event publication date=2015-06-01  Event code=US/EXET  Event type=Examination events  Event type=OAO  Event type=INT  Interview Summary - 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
专利类型码
A1B2
国别省市代码
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