Development of a solidified self-microemulsifying drug delivery system (S-SMEDDS) for atorvastatin calcium with improved dissolution and bioavailability
DC Field | Value | Language |
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dc.contributor.author | Yeom, Dong Woo | - |
dc.contributor.author | Son, Ho Yong | - |
dc.contributor.author | Kim, Jin Han | - |
dc.contributor.author | Kim, Sung Rae | - |
dc.contributor.author | Lee, Sang Gon | - |
dc.contributor.author | Song, She Hyon | - |
dc.contributor.author | Chae, Bo Ram | - |
dc.contributor.author | Choi, Young Wook | - |
dc.date.available | 2019-03-08T12:56:37Z | - |
dc.date.issued | 2016-06 | - |
dc.identifier.issn | 0378-5173 | - |
dc.identifier.issn | 1873-3476 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/6826 | - |
dc.description.abstract | To improve the dissolution and oral bioavailability (BA) of atorvastatin calcium (ATV), we previously introduced an optimized self-microemulsifying drug delivery system (SMEDDS) using Capmul (R) MCM (oil), Tween (R) 20 (surfactant), and tetraglycol (cosurfactant). In this study, various solid carriers were employed to develop a solidified SMEDDS (S-SMEDDS): mannitol (M) and lactose (L) as water-soluble carriers, and Sylysia (R) 350 (S) and Aerosil (R) 200 (A) as water-insoluble carriers. Maximum solidifying capacities (SCmax) of water-insoluble carriers were significantly greater than those of water-soluble carriers were. The resultant powders were free flowing with an angle of repose <40 degrees and Carr's index 5-20%, regardless of the solid carrier types. S-SMEDDS with mannitol (S(M)-SMEDDS) or lactose (S(L)SMEDDS) had a smaller droplet size and greater dissolution than S-SMEDDS with Sylysia (R) 350 (S(S)SMEDDS) or Aerosil (R) 200 (S(A)-SMEDDS). Following oral administration of various formulations to rats at a dose equivalent to 25 mg/kg of ATV, plasma drug levels were measured by LC-MS/MS. The relative BAs (RBAs) of SMEDDS, S(M)-SMEDDS, and S(S)-SMEDDS were 345%, 216%, and 160%, respectively, compared to that of ATV suspension. Additionally, at a reduced dose of ATV equivalent to 5 mg/kg, the RBAs of S(M)-SMEDDS and S(S)-SMEDDS compared to that of SMEDDS were 101% and 65%, respectively. These results suggest that S(M)-SEMDDS offers great potential for the development of solid dosage forms with improved oral absorption of drugs with poor water solubility. (c) 2016 Elsevier B.V. All rights reserved. | - |
dc.format.extent | 10 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | ELSEVIER SCIENCE BV | - |
dc.title | Development of a solidified self-microemulsifying drug delivery system (S-SMEDDS) for atorvastatin calcium with improved dissolution and bioavailability | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.ijpharm.2016.04.059 | - |
dc.identifier.bibliographicCitation | INTERNATIONAL JOURNAL OF PHARMACEUTICS, v.506, no.1-2, pp 302 - 311 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000377031200032 | - |
dc.identifier.scopusid | 2-s2.0-84964615062 | - |
dc.citation.endPage | 311 | - |
dc.citation.number | 1-2 | - |
dc.citation.startPage | 302 | - |
dc.citation.title | INTERNATIONAL JOURNAL OF PHARMACEUTICS | - |
dc.citation.volume | 506 | - |
dc.type.docType | Article | - |
dc.publisher.location | 네델란드 | - |
dc.subject.keywordAuthor | Atorvastatin | - |
dc.subject.keywordAuthor | SMEDDS | - |
dc.subject.keywordAuthor | Solidified SMEDDS | - |
dc.subject.keywordAuthor | Solid carrier | - |
dc.subject.keywordAuthor | Sylysia (R) 350 | - |
dc.subject.keywordAuthor | Mannitol | - |
dc.subject.keywordPlus | REDISPERSIBLE DRY EMULSIONS | - |
dc.subject.keywordPlus | IN-VITRO | - |
dc.subject.keywordPlus | STATE CHARACTERIZATION | - |
dc.subject.keywordPlus | POROUS CARRIERS | - |
dc.subject.keywordPlus | OPTIMIZATION | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | FORMULATIONS | - |
dc.subject.keywordPlus | LIQUID | - |
dc.subject.keywordPlus | PHARMACOKINETICS | - |
dc.subject.keywordPlus | PERFORMANCE | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | sci | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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