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dc.contributor.author최한곤-
dc.date.accessioned2018-04-12T02:43:42Z-
dc.date.available2018-04-12T02:43:42Z-
dc.date.issued2016-07-
dc.identifier.citationCOLLOIDS AND SURFACES B-BIOINTERFACES, v. 146, Page. 754-761en_US
dc.identifier.issn0927-7765-
dc.identifier.issn1873-4367-
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0927776516305276-
dc.identifier.urihttp://hdl.handle.net/20.500.11754/65625-
dc.description.abstractThe objective of this study was to develop a novel prasugrel base microsphere-loaded tablet (PBMST) with enhanced stability as a bioequivalent to the commercial prasugrel hydrochloride-loaded tablet. Numerous prasugrel base-loaded microspheres were prepared with hydroxypropylmethyl cellulose (HPMC), colloidal silica and various acidifying agents using a spray-drying process, and the physicochemical properties, solubility and stability were investigated. The PBMSTs were prepared and their dissolution, pharmacokinetics in beagle dogs and stability were evaluated compared to commercial prasugrel hydrochloride-loaded tablets. Among the acidifying agents tested, phosphoric acid provided the greatest increase in drug solubility, by as much as 110-fold. The prasugrel base-loaded microspheres composed of prasugrel base, HPMC, colloidal silica and phosphoric acid at a weight ratio of 10/10/5/2.5 provided an amorphous drug and reduced particle size of about 11.3 mu m. Moreover, it exhibited excellent solubility and improved stability compared to prasugrel base and hydrochloride. Moreover, PBMST drug dissolution was improved in comparison to the prasugrel base-loaded tablet (PBT), with similar dissolution to the commercial prasugrel hydrochloride-loaded tablet at pH 1.2 and 4.0. PBMST provided significantly higher plasma concentrations of AUC and Cinax in beagle dogs compared to PBT. In particular, the AUC of PBMST was approximately four times greater than PBT, leading to improved oral bioavailability. There were no significant differences observed for all pharmacokinetic parameters between PBMST and the commercial prasugrel hydrochloride-loaded tablet, suggesting their bioequivalence in beagle dogs. Furthermore, the prepared PBMSTs were stable for at least six months. Therefore, this novel prasugrel base microsphere-loaded tablet could be a potential alternative for enhancing the stability and bioavailability of prasugrel. (C) 2016 Elsevier B.V. All rights reserved.en_US
dc.description.sponsorshipThis work was supported by a National Research Foundation of Korea (NRF) grant funded by the Korean government (MEST) (No. 2015R1A2A2A05027872) and a grant (16173MFDS542) from Ministry of Food and Drug Safety in 2016.en_US
dc.language.isoen_USen_US
dc.publisherELSEVIER SCIENCE BVen_US
dc.subjectPrasugrel baseen_US
dc.subjectMicrosphereen_US
dc.subjectPhosphoric aciden_US
dc.subjectStabilityen_US
dc.subjectSolubilityen_US
dc.subjectBioavailabilityen_US
dc.subjectBioequivalenceen_US
dc.titleDevelopment of novel prasugrel base microsphere-loaded tablet with enhanced stability: Physicochemical characterization and in vivo evaluation in beagle dogsen_US
dc.typeArticleen_US
dc.relation.volume146-
dc.identifier.doi10.1016/j.colsurfb.2016.07.025-
dc.relation.page754-761-
dc.relation.journalCOLLOIDS AND SURFACES B-BIOINTERFACES-
dc.contributor.googleauthorKim, KS-
dc.contributor.googleauthorKim, JC-
dc.contributor.googleauthorJin, SG-
dc.contributor.googleauthorKim, DW-
dc.contributor.googleauthorKim, DS-
dc.contributor.googleauthorYong, CS-
dc.contributor.googleauthorKim, JO-
dc.contributor.googleauthorYoun, YS-
dc.contributor.googleauthorOh, KT-
dc.contributor.googleauthorWoo, JS-
dc.contributor.googleauthorChoi, HS-
dc.relation.code2016001589-
dc.sector.campusE-
dc.sector.daehakCOLLEGE OF PHARMACY[E]-
dc.sector.departmentDEPARTMENT OF PHARMACY-
dc.identifier.pidhangon-
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COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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