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N-glucuronidation catalyzed by UGT1A4 and UGT2B10 in human liver microsomes: Assay optimization and substrate identification.
J Pharm Biomed Anal
October 2017
Research Center for Biopharmaceutics and Pharmacokinetics, College of Pharmacy, Jinan University, Guangzhou, China; Guangdong Province Key Laboratory of Pharmacodynamic Constituents of TCM and New Drugs Research, Jinan University, Guangzhou, China. Electronic address:
N-glucuronidation is an important pathway for metabolism and disposition of tertiary amines in humans. This reaction is mainly catalyzed by the enzymes UGT1A4 and UGT2B10. However, the metabolic patterns of UGT1A4- and UGT2B10-mediated N-glucuronidation are not fully clear.
View Article and Find Full Text PDFStudies on the interaction between promethazine and human serum albumin in the presence of flavonoids by spectroscopic and molecular modeling techniques.
Colloids Surf B Biointerfaces
September 2016
College of Pharmacy, Liaoning University, Shenyang 110036, China. Electronic address:
Fluorescence, absorption, time-correlated single photon counting (TCSPC), and circular dichroism (CD) spectroscopic techniques as well as molecular modeling methods were used to study the binding characterization of promethazine (PMT) to human serum albumin (HSA) and the influence of flavonoids, rutin and baicalin, on their affinity. The results indicated that the fluorescence quenching mechanism of HSA by PMT is a static quenching due to the formation of complex. The reaction was spontaneous and mainly mediated by hydrogen bonds and hydrophobic interactions.
View Article and Find Full Text PDFComparison of antiemetics for nausea and vomiting of pregnancy in an emergency department setting.
Am J Emerg Med
July 2015
Women & Infants Hospital, Warren Alpert Medical School of Brown University, Providence, RI. Electronic address:
Objective: To compare time from medication administration to disposition from the Emergency Department (ED) between women treated for nausea and vomiting of pregnancy with different antiemetic agents.
Design: We performed a retrospective cohort study of women 13 weeks gestation or less treated in our Women and Infants Hospital ED for nausea and vomiting of pregnancy between 2009 and 2011. Data was collected on patient demographics, antiemetics used, and time to disposition.
In silico mechanistic disposition and in vivo evaluation of zero-order drug release from a novel triple-layered tablet matrix.
Expert Opin Drug Deliv
May 2015
Wits Advanced Drug Delivery Platform Research Unit, Department of Pharmacy and Pharmacology, School of Therapeutic Sciences, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, 7 York Road, Parktown, 2193 , South Africa.
Objectives: The purpose of this study was to formulate novel triple-layered tablet (TLT) matrices employing modified polyamide 6,10 (mPA6,10) and salted-out poly(lactic-co-glycolic acid) (s-PLGA) in an attempt to achieve stratified zero-order drug release.
Methods: mPA6,10 and s-PLGA were employed as the outer drug-carrier matrices, whereas poly(ethylene oxide) (PEO) was used as the middle-layer drug matrix. Diphenhydramine HCl, ranitidine HCl and promethazine were selected as model drugs to pre-optimize the TLT, whereas atenolol, acetylsalicylic acid and simvastatin were employed as a comparable fixed dose combination to test the TLT prototype in vitro and in vivo (Large White Pig model).
Comparative study of interactions between chloroquine and chlorpheniramine or promethazine in healthy volunteers: a potential combination-therapy phenomenon for resuscitating chloroquine for malaria treatment in Africa.
Ann Trop Med Parasitol
January 2008
Malaria Research Laboratories, Institute of Advanced Medical Research and Training, College of Medicine, University College Hospital, Ibadan, Nigeria.
Although, in in-vitro and limited in-vivo studies, chlorpheniramine (CP) and promethazine (PR) have each been shown to reverse chloroquine (CQ) resistance, the pharmacokinetic basis of this reversal has not been fully elucidated. In the present study, 15 healthy volunteers were randomly allotted to receive standard doses of CQ alone or in combination with CP or PR. Blood samples were collected from each volunteer at 21 time-points, from immediately before to 168 h after the initial dose.
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