Supersaturable self-microemulsifying drug delivery system enhances dissolution and bioavailability of telmisartan
DC Field | Value | Language |
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dc.contributor.author | Park, Sun Young | - |
dc.contributor.author | Jin, Chang Hwa | - |
dc.contributor.author | Goo, Yoon Tae | - |
dc.contributor.author | Chae, Bo Ram | - |
dc.contributor.author | Yoon, Ho Yub | - |
dc.contributor.author | Kim, Chang Hyun | - |
dc.contributor.author | Song, Seh Hyon | - |
dc.contributor.author | Han, Sang Beom | - |
dc.contributor.author | Choi, Young Wook | - |
dc.date.accessioned | 2021-07-21T02:43:03Z | - |
dc.date.available | 2021-07-21T02:43:03Z | - |
dc.date.issued | 2021-01 | - |
dc.identifier.issn | 1083-7450 | - |
dc.identifier.issn | 1097-9867 | - |
dc.identifier.uri | https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/47708 | - |
dc.description.abstract | To enhance the dissolution and oral bioavailability of telmisartan (TMS), a poorly water-soluble anti-hypertensive drug, a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) was developed. Amorphous alkalinized TMS (AAT) was formulated into a SMEDDS, composed of Capmul (R) MCM (oil), Cremophor(R)RH40 (surfactant), and tetraglycol (co-surfactant). Although the SMEDDS was rapidly dissolved (>80% within 5 min) in a limited condition (500 mL, pH 6.8), drug precipitation was observed over time, resulting in a decrease in dissolution levels. The precipitation was due to drug recrystallization, as determined by differential scanning calorimetry and powder X-ray diffraction analyses. Several polymers, including Soluplus(R)(SOL), were screened as precipitation inhibitors; ultimately, SuSMEDDS-SOL was prepared by admixing SOL and the SMEDDS at a 5:100 (w/w) ratio. SuSMEDDS-SOL was superior in terms of dissolution efficiency (>90% over 2 h) and dissolution-retaining time (no precipitation over 2 h). Anin vivopharmacokinetic study in rats revealed that the oral bioavailability of SuSMEDDS-SOL was 4.8-, 1.3-, and 1.2-fold greater than those of the TMS suspension, AAT solution, and SMEDDS, respectively. Therefore, SuSMEDDS-SOL is a promising candidate to enhance the dissolution and oral bioavailability of TMS. | - |
dc.format.extent | 9 | - |
dc.language | 영어 | - |
dc.language.iso | ENG | - |
dc.publisher | TAYLOR & FRANCIS LTD | - |
dc.title | Supersaturable self-microemulsifying drug delivery system enhances dissolution and bioavailability of telmisartan | - |
dc.type | Article | - |
dc.identifier.doi | 10.1080/10837450.2020.1834580 | - |
dc.identifier.bibliographicCitation | PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, v.26, no.1, pp 60 - 68 | - |
dc.description.isOpenAccess | N | - |
dc.identifier.wosid | 000579197900001 | - |
dc.identifier.scopusid | 2-s2.0-85092760070 | - |
dc.citation.endPage | 68 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 60 | - |
dc.citation.title | PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY | - |
dc.citation.volume | 26 | - |
dc.type.docType | Article | - |
dc.publisher.location | 영국 | - |
dc.subject.keywordAuthor | Telmisartan | - |
dc.subject.keywordAuthor | supersaturable self-microemulsifying drug delivery system (SuSMEDDS) | - |
dc.subject.keywordAuthor | precipitation inhibitor | - |
dc.subject.keywordAuthor | Soluplus | - |
dc.subject.keywordAuthor | dissolution | - |
dc.subject.keywordAuthor | bioavailability | - |
dc.subject.keywordPlus | WATER-SOLUBLE DRUGS | - |
dc.subject.keywordPlus | ORAL BIOAVAILABILITY | - |
dc.subject.keywordPlus | S-SEDDS | - |
dc.subject.keywordPlus | SMEDDS | - |
dc.subject.keywordPlus | FORMULATION | - |
dc.subject.keywordPlus | PH | - |
dc.subject.keywordPlus | ABSORPTION | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | PRECIPITATION | - |
dc.subject.keywordPlus | SOLUBILITY | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalWebOfScienceCategory | Pharmacology & Pharmacy | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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