FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2021853889> ?p ?o ?g. }

• W2021853889 endingPage "106" @default.
• W2021853889 startingPage "97" @default.
• W2021853889 abstract "Although lovastatin (LS) is widely used in the treatment of hypercholesterolemia, its bioavailability is known to be around 5%. This study was aimed to increase the solubility and dissolution-permeation rates of LS using solid dispersions (SDs) with bile salts. The solubilities of LS in water, aqueous bile salt solutions and non-aqueous vehicles were determined, and effects of bile salts on the cellulose or duodenal permeation of LS from SDs were evaluated using a horizontal permeation system. SDs were prepared at various ratios of LS to carriers, such as sodium deoxycholate (SDC), sodium glycocholate (SGC) and/or 2-hydroxypropyl--cyclodextrin (HPCD). The addition of bile salts (25 mM) in water increased markedly the solubility of LS by the micellar solubilization. Some non-aqueous vehicles were effective in solubilizing LS. From differential scanning calorimetric studies, it was found that the crystallinity of LS in SDs disappeared, indicating a formation of amorphous state. The SDs showed markedly enhanced dissolution compared with those of their physical mixtures (PMs) and drug alone. In the dissolution-permeation studies using a cellulose membrane, the donor and receptor solutions were maintained as a sink condition using pH 7.0 phosphate buffer containing 0.05% sodium lauryl sulfate (SLS). The flux of LS alone was nearly same as that of LS-SDC-HPCD (1:3:6) PM. However, the flux of LS-SDC-HPCD (1:3:6) SD slightly increased compared with drug alone and PM, suggesting that entrapment of LS in micelles does not significantly hinder the permeation across cellulose membrane. In the dissolution-duodenal permeation studies using a LS-HPCD-SDC (1:3:6) SD, the addition of various bile salts in donor solutions (25 mM) enhanced the permeation of LS markedly, and the fluxes were found to be , , , and for sodium cholate (SC), SDC, SGC, sodium taurodeoxycholate (STDC) and sodium taurocholate (STC), respectively. The stepwise increase of donor SGC concentration increased the flux dose-dependently. From the relationship of donor SGC concentration and flux, the concentration of SGC initiating the permeation across the duodenal mucosa was calculated to be 11.1 mM, which is nearly same as the critical micelle concentration (CMC, 11.6 mM) of SGC. However, with no addition of bile salts and below CMC, the permeation was very limited and irratic, indicating that LS itself is very poor permeable. Higher protions of bile salt in SD such as LS-SDC or LS-SGC (1 : 49 and 1 : 69) showed highly promoted fluxes. In conclusion, SD systems with bile salts, which may form their micelles in intestinal fluids, might be a promising means for providing enhanced dissolution and intestinal permeation of practically insoluble and non-absorbable LS." @default.
• W2021853889 created "2016-06-24" @default.
• W2021853889 creator A5004059878 @default.
• W2021853889 date "2009-04-27" @default.
• W2021853889 modified "2023-10-14" @default.
• W2021853889 title "Dissolution and Duodenal Permeation Characteristics of Lovastatin from Bile Salt Solid Dispersions" @default.
• W2021853889 cites W119853313 @default.
• W2021853889 cites W1484689544 @default.
• W2021853889 cites W1498305210 @default.
• W2021853889 cites W1581747141 @default.
• W2021853889 cites W1992393784 @default.
• W2021853889 cites W1996041024 @default.
• W2021853889 cites W1998336053 @default.
• W2021853889 cites W2001958300 @default.
• W2021853889 cites W2003308807 @default.
• W2021853889 cites W2004919981 @default.
• W2021853889 cites W2011204030 @default.
• W2021853889 cites W2014346720 @default.
• W2021853889 cites W2018126221 @default.
• W2021853889 cites W2018605608 @default.
• W2021853889 cites W2027664960 @default.
• W2021853889 cites W2037693744 @default.
• W2021853889 cites W2045063002 @default.
• W2021853889 cites W2045792728 @default.
• W2021853889 cites W2054800049 @default.
• W2021853889 cites W2063900272 @default.
• W2021853889 cites W2065106251 @default.
• W2021853889 cites W2065813534 @default.
• W2021853889 cites W2078603028 @default.
• W2021853889 cites W2089865736 @default.
• W2021853889 cites W2146318670 @default.
• W2021853889 cites W2147153780 @default.
• W2021853889 doi "https://doi.org/10.4333/kps.2009.39.2.097" @default.
• W2021853889 hasPublicationYear "2009" @default.
• W2021853889 type Work @default.
• W2021853889 sameAs 2021853889 @default.
• W2021853889 citedByCount "0" @default.
• W2021853889 crossrefType "journal-article" @default.
• W2021853889 hasAuthorship W2021853889A5004059878 @default.
• W2021853889 hasConcept C178790620 @default.
• W2021853889 hasConcept C185592680 @default.
• W2021853889 hasConcept C2776371256 @default.
• W2021853889 hasConcept C2778163477 @default.
• W2021853889 hasConcept C2780940807 @default.
• W2021853889 hasConcept C41625074 @default.
• W2021853889 hasConcept C43617362 @default.
• W2021853889 hasConcept C50670333 @default.
• W2021853889 hasConcept C55493867 @default.
• W2021853889 hasConcept C88380143 @default.
• W2021853889 hasConceptScore W2021853889C178790620 @default.
• W2021853889 hasConceptScore W2021853889C185592680 @default.
• W2021853889 hasConceptScore W2021853889C2776371256 @default.
• W2021853889 hasConceptScore W2021853889C2778163477 @default.
• W2021853889 hasConceptScore W2021853889C2780940807 @default.
• W2021853889 hasConceptScore W2021853889C41625074 @default.
• W2021853889 hasConceptScore W2021853889C43617362 @default.
• W2021853889 hasConceptScore W2021853889C50670333 @default.
• W2021853889 hasConceptScore W2021853889C55493867 @default.
• W2021853889 hasConceptScore W2021853889C88380143 @default.
• W2021853889 hasIssue "2" @default.
• W2021853889 hasLocation W20218538891 @default.
• W2021853889 hasOpenAccess W2021853889 @default.
• W2021853889 hasPrimaryLocation W20218538891 @default.
• W2021853889 hasRelatedWork W2011764456 @default.
• W2021853889 hasRelatedWork W2225991183 @default.
• W2021853889 hasRelatedWork W2258441016 @default.
• W2021853889 hasRelatedWork W2350311267 @default.
• W2021853889 hasRelatedWork W2594022762 @default.
• W2021853889 hasRelatedWork W2802242559 @default.
• W2021853889 hasRelatedWork W2897588816 @default.
• W2021853889 hasRelatedWork W2908799665 @default.
• W2021853889 hasRelatedWork W2913831029 @default.
• W2021853889 hasRelatedWork W2950697379 @default.
• W2021853889 hasVolume "39" @default.
• W2021853889 isParatext "false" @default.
• W2021853889 isRetracted "false" @default.
• W2021853889 magId "2021853889" @default.
• W2021853889 workType "article" @default.