Journal Article10.1016/J.JCHROMB.2007.02.053
Concurrent determination of ezetimibe and its phase-I and II metabolites by HPLC with UV detection: quantitative application to various in vitro metabolic stability studies and for qualitative estimation in bile.
Shaik Jafar Sadik Basha,Shaik Abdul Naveed,Nirbhay Kumar Tiwari,Dhanya Shashikumar,Syed Muzeeb,Thammera Ranjith Kumar,Nyavanandi Vijay Kumar,Nadipalli Prabhakar Rao,N. R. Srinivas,Ramesh Mullangi,Nuggehally R. Srinivas +10 more
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TL;DR: Overall, the method is suitable for simultaneous measurement of EZM, and its phase-I and phase-II metabolite (EZM-G) in in vitro and in vivo studies.
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About: This article is published in Journal of Chromatography B. The article was published on 15 Jun 2007. The article focuses on the topics: Metabolite & High-performance liquid chromatography.
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Citations
Study of surfactant combinations and development of a novel nanoemulsion for minimising variations in bioavailability of ezetimibe.
Vikas Bali,Mushir Ali,Javed Ali +2 more
TL;DR: N nanoemulsion formulation is established to be one of the possible alternatives to traditional oral formulations of ezetimibe to improve its bioavailability and stability, pharmacodynamic and pharmacokinetic potential.
260
Nanocarrier for the enhanced bioavailability of a cardiovascular agent: in vitro, pharmacodynamic, pharmacokinetic and stability assessment.
Vikas Bali,Mushir Ali,Javed Ali +2 more
TL;DR: Nanoemulsion was corroborated to be a promising choice to improve the bioavailability of ezetimibe and superior absorption from nanoemulsion as compared to the marketed formulation and drug suspension.
105
Health risks associated with the pharmaceuticals in wastewater.
TL;DR: An applied framework for planning and policy-making is suggested to mitigate the health risks and optimally employ reclaimed wastewater for human purposes.
Effect of hydroxypropylcellulose and Tween 80 on physicochemical properties and bioavailability of ezetimibe-loaded solid dispersion.
Rehmana Rashid,Dong Wuk Kim,Fakhar ud Din,Omer Mustapha,Abid Mehmood Yousaf,Jong Hyuck Park,Jong Oh Kim,Chul Soon Yong,Han-Gon Choi +8 more
TL;DR: HPC greatly affected the solubility, dissolution and oral bioavailability of drug, but Tween 80 hardly did, and this ezetimibe-loaded binary solid dispersion prepared only with HPC would be suggested as a potential formulation for oral administration of ezETimibe.
86
Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe
Rehmana Rashid,Dong Wuk Kim,Abid Mehmood Yousaf,Omer Mustapha,Fakhar ud Din,Jong Hyuck Park,Chul Soon Yong,Yu-Kyoung Oh,Yu Seok Youn,Jong Oh Kim,Han-Gon Choi +10 more
TL;DR: Among the various formulations tested in this study, the SESD system would be strongly recommended as a drug delivery system for the oral administration of ezetimibe with poor water solubility.
References
Comparison of the activity and disposition of the novel cholesterol absorption inhibitor, SCH58235, and its glucuronide, SCH60663
Margaret van Heek,Constance Farley,Douglas S Compton,Lizbeth M. Hoos,Kevin B. Alton,Edmund J. Sybertz,Harry R. Davis +6 more
TL;DR: It is demonstrated that the phenolic glucuronide (SCH60663) of SCH58 235, was more potent at inhibiting cholesterol absorption in rats than SCH58235, when administered by the intraduodenal route.
352
Effectiveness and tolerability of ezetimibe in patients with primary hypercholesterolemia: pooled analysis of two phase II studies
Harold E. Bays,Paul B Moore,Margaret Drehobl,Sidney Rosenblatt,Phillip D Toth,Carlos A. Dujovne,Robert H Knopp,Leslie Lipka,Alexandre LeBeaut,Bo Yang,L. Mellars,Cynthia Cuffie-Jackson,Enrico P. Veltri +12 more
TL;DR: Ezetimibe significantly decreased plasma LDL-C levels and increased plasma HDL-C Levels, with a tolerability profile similar to that of placebo, in these two 12-week studies.
324
Ezetimibe selectively inhibits intestinal cholesterol absorption in rodents in the presence and absence of exocrine pancreatic function.
TL;DR: Ezetimibe is a potent inhibitor of intestinal free cholesterol absorption that does not require exocrine pancreatic function for activity and affects the absorption of vitamin A, D or taurocholate, as a bile acid sequestrant (cholestyramine) would.
224
Development and validation of a reversed-phase HPLC method for the determination of ezetimibe in pharmaceutical dosage forms
TL;DR: The developed method was successfully applied to estimate the amount of ezetimibe in tablets and was found to be linear from 0.5 to 50 microg/ml.
151
Identification of human UDP-glucuronosyltransferase enzyme(s) responsible for the glucuronidation of ezetimibe (Zetia).
Anima Ghosal,Neil Hapangama,Yuan Yuan,Joana Achanfuo-Yeboah,Robert M. Iannucci,Swapan K. Chowdhury,Kevin B. Alton,James E. Patrick,Shmuel Zbaida +8 more
TL;DR: This study identified the isoform(s) of human liver and intestinal UDP-glucuronosyltransferase (UGT) enzymes responsible for the glucuronidation of ezetimibe and identified the main circulating metabolite of this drug in human plasma, SCH 60663.
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