Abstract：
:SR16157 (21-(2-N,N-diethylaminoethyl)oxy-7alpha-methyl-19-norpregna-1,3,5(10)-triene-3-O-sulfamate) is a novel, dual-acting estrone sulfatase inhibitor currently in preclinical development for use in breast cancer therapy. The compound has a dual mechanism of action: the sulfamate-containing parent compound SR16157 inhibits estrogen biosynthesis by irreversibly inhibiting the enzyme estrone sulfatase. The phenolic metabolite, SR16137, generated by the sulfatase enzyme is a potent antiestrogen in breast tissues and has beneficial effects in bone and the cardiovascular system. As part of the ongoing preclinical studies, an HPLC assay method has been developed and validated for SR16157. The assay method is specific, accurate (recovery=99.4-101.1), linear (r(2)> or =0.9999), precise (intraday R.S.D.< or =1.1%, intermediate R.S.D.< or =0.8%), and sensitive (limit of detection=1.0 microg/ml). It separates SR16157 from its impurities and forced decomposition products, which have been characterized by LC coupled with mass and UV spectral data. Major decomposition pathways are hydrolysis, hydroxylation, and oxidation.
journal_name
J Pharm Biomed Analjournal_title
Journal of pharmaceutical and biomedical analysisauthors
Wang J,ChunYang,Wang E,Li S,Zaveri N,Liu Pdoi
10.1016/j.jpba.2007.08.015subject
Has Abstractpub_date
2007-11-30 00:00:00pages
572-82issue
4eissn
0731-7085issn
1873-264Xpii
S0731-7085(07)00444-Xjournal_volume
45pub_type
杂志文章abstract：:Clindamycin is widely used in antimicrobial prophylaxis to prevent surgical site infections. Adequate subcutaneous free tissue concentrations should reach therapeutic levels, which have to be maintained throughout the surgical procedure for antibiotic prophylaxis to be efficient. A method was developed and validated u...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2018.02.005
更新日期：2018-05-10 00:00:00
abstract：:The consumption of dietary fats have been long associated to chronic diseases such as obesity, diabetes, cancer, arthritis, asthma, and cardiovascular disease; although some controversy still exists in the role of dietary fats in human health, certain fats have demonstrated their positive effect in the modulation of a...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章,评审
doi：10.1016/j.jpba.2009.05.012
更新日期：2010-01-20 00:00:00
abstract：:Stable isotope analogues of phenytoin are useful for pulse dose pharmacokinetic studies in epilepsy patients. A simultaneous assay was developed to quantitate phenytoin (5,5-diphenylhydantoin) and its stable isotope analogue [13C3]-phenytoin (5,5-diphenyl-2,4,5-13C3-hydantoin) from plasma. Quantitation was achieved by...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(98)00018-1
更新日期：1998-09-01 00:00:00
abstract：:Attachment of antibodies to liposomes endows target specificity to liposomes for a certain cell or organ that express the targeted antigenic determinant. These so-called immunoliposomes hold high promise as targeted drug carriers. One approach of immunoliposome preparation involves conjugating antibodies to hydrophobi...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(97)00101-5
更新日期：1997-11-01 00:00:00
abstract：:The photostability of melatonin, a hormone used as supplementary drug in the alleviation of jet-lag and other sleep disorders, was studied. The drug photodegradation at different pH values was monitored by HPLC methods. The main photoproduct was isolated and characterised on the basis of the NMR, FTIR, and mass spectr...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(00)00259-4
更新日期：2000-08-01 00:00:00
abstract：:The present work describes the development and validation of rapid, sensitive and accurate liquid chromatography method, coupled with tandem mass spectrometry detection, for quantification of tranexamic acid in human plasma using isotopically labeled internal standard (IS). A one-step plasma protein precipitation was ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2013.12.005
更新日期：2014-03-01 00:00:00
abstract：:Two methods are described for the simultaneous determination of tizanidine and rofecoxib in binary mixture. The first method was based on HPTLC separation of the two drugs followed by densitometric measurements of their spots at 311 nm. The separation was carried out on Merck HPTLC aluminium sheets of silica gel 60 F2...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2004.09.036
更新日期：2005-02-07 00:00:00
abstract：:CGS 26214 is a racemic compound having cholesterol-lowering activity in rats, dogs, and monkeys. This compound has two equipotent chiral components CGS 28934(-) and CGS 28935(+). An analytical challenge was to develop a sensitive liquid chromatography/tandem mass spectrometry (LC/MS/MS) method for the analysis of the ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(00)00364-2
更新日期：2000-09-01 00:00:00
abstract：:In our previous work, a new monolithic coating based on vinylpyrrolidone-ethylene glycol dimethacrylate polymer was introduced for stir bar sorptive extraction. The formulation of the prepared vinylpyrrolidone-ethylene glycol dimethacrylate monolithic polymer was optimized and the satisfactory quality of prepared coat...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2018.02.030
更新日期：2018-05-10 00:00:00
abstract：:The stability of ketorolac tromethamine was investigated in acid (0.5M HCl) and alkaline conditions (0.5M NaOH), using the same procedure reported by Devarajan et al. [2]. The acid and base degradation products were identified by liquid chromatography-mass spectrometry (LC-MS). ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2010.01.031
更新日期：2010-06-05 00:00:00
abstract：:Drugs may be metabolised to reactive electrophilic species that spontaneously react with proteins. The presence of such drug-protein adducts has been associated with drug toxicity. In this study, the reactivity of the major metabolite of naproxen--the 1-beta-O-glucuronide (Nap-GlcU)--was compared to the corresponding ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(02)00026-2
更新日期：2002-06-20 00:00:00
abstract：:Botulinum type A toxin (BoNT/A) is defined by its specific endopeptidase cleavage of SNAP25 between Gln(197) and Arg(198) under reducing conditions. The neurotoxin is widely used for therapeutic or cosmetic purposes, but should not contain other toxin serotypes or unwanted protease activities. Using a neoepitope endop...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2010.08.013
更新日期：2011-01-05 00:00:00
abstract：:10 homeopathic remedies commercially available (each in 3 dilutions) as sugar granules, where half of them were of organic (and half inorganic) origin were subjected to solid-state infrared spectroscopy, both in middle infrared (ATR-FTIR) and near infrared (NIR) range. Measurements were repeated six times (six days, e...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2015.06.025
更新日期：2015-11-10 00:00:00
abstract：:The analysis of volatile samples is mostly performed by GC. However, its separation power may not be enough for some complex samples. Comprehensive gas chromatography (GC × GC) increases the separation power by means of a second separation dimension. Parallel to the great technological advances realised since the earl...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章,评审
doi：10.1016/j.jpba.2019.112817
更新日期：2019-11-30 00:00:00
abstract：:Stable isotope labeled (SIL) compounds have been commonly used as internal standards (IS) to ensure the accuracy and quality of liquid chromatography-mass spectrometry (LC-MS) bioanalytical assays. Recently, the application of SIL drugs and LC-MS assays to microdose absolute bioavailability (BA) studies has gained inc...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2018.12.014
更新日期：2019-02-20 00:00:00
abstract：:The possibility of the rapid identification of drug related minor components by HPLC/diode-array UV spectroscopy is demonstrated by three examples. Hydroxylated impurities (degradation products) of norgestrel (6 alpha and beta, 10 beta-hydroxy derivatives) were identified on the basis of their UV spectra and retention...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/0731-7085(95)01579-5
更新日期：1995-12-01 00:00:00
abstract：:The H-point standard additions method (HPSAM) and two versions of the generalized H-point standard additions method (GHPSAM) are evaluated for the UV-analysis of two-component mixtures. Synthetic mixtures of anhydrous caffeine and phenazone as well as of atovaquone and proguanil hydrochloride were used. Furthermore, t...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(99)00111-9
更新日期：1999-10-01 00:00:00
abstract：:To characterize and enable efficient rat pharmacokinetic (PK) screening in early drug discovery, automated sampling of blood time points are routinely employed. With the development of dried blood spot (DBS) technology for drug level quantitation, an opportunity exists for the automated collection of rat PK time point...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2012.04.013
更新日期：2012-08-01 00:00:00
abstract：:Traditional antibody dependent cellular cytotoxicity (ADCC) assays use donor derived natural killer (NK) or peripheral blood mononuclear cells, but donor genetic variability and the technically challenging nature of the assay means that alternative in vitro assay formats are required. We explored the utility of two re...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2017.06.004
更新日期：2017-09-05 00:00:00
abstract：:Guest-host interactions of sildenafil (Sild) with cyclodextrins (CyDs) have been investigated using several techniques including phase solubility diagrams (PSD), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD), proton nuclear magnetic resonance (1H NMR) and molecular mechanical modeling (MM...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2006.01.055
更新日期：2006-06-07 00:00:00
abstract：:In human respiratory disease studies, liquid samples such as nasal secretion (NS), lung epithelial lining fluid (ELF), or upper airway mucosal lining fluid (MLF) are frequently collected, but their volumes often remain unknown. The lack of volume information makes it hard to estimate the actual concentration of recove...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2016.11.001
更新日期：2017-01-30 00:00:00
abstract：:In search of the pathophysiological background of premenstrual syndrome, direct chemical ionization-mass spectrometric profiling was applied to urine samples from 17 patients and 18 control subjects, collected on days 11 and 25 of the menstrual cycle. Oestrogenic compounds and hippuric acid were found to be involved i...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/0731-7085(89)80127-x
更新日期：1989-01-01 00:00:00
abstract：:Isoflavones are suitable guest molecules for inclusion complex formation with cyclodextrins (CDs). The molecular encapsulation with CDs results in a solid, molecularly dispersed form and in a significantly improved aqueous solubility of isoflavones. Genistein, a key isoflavone constituent of Ononidis spinosae radix wa...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2008.06.007
更新日期：2008-11-04 00:00:00
abstract：:Many plant-derived glycosides are used as medications. It is common that these glycosides show poor intestinal absorption but their metabolites generated by intestinal microflora demonstrate strong bioactivity. Hence, it is crucial to develop a method for the identification and characterization of the metabolites, and...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2015.11.029
更新日期：2016-02-05 00:00:00
abstract：:A liquid chromatography-electrospray ionization-tandem mass spectrometry (LC-ESI-MS/MS) assay was developed and qualified for analyzing 4β-hydroxycholesterol and cholesterol in 5 μl of human and mouse plasma. Stable isotope-labeled d7-analogs of both analytes were used as internal standards and 4.2% (w/v) human serum ...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2013.07.016
更新日期：2013-11-01 00:00:00
abstract：:Plants of the Amaryllidaceae family are a well-known source of tetrahydroisoquinoline alkaloids with a wide range of biological activities, including antiviral, antitumoral, antiparasitic, psychopharmacological, and acetylcholinesterase inhibitory, among others. Recent advances in the use of GC or LC coupled to MS hav...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2012.05.009
更新日期：2012-11-01 00:00:00
abstract：:From the reaction between l-lysine and formaldehyde, Nepsilon-formyl-L-lysine was isolated by means of ion-exchange column chromatography. The identification of Nepsilon-formyl-L-lysine was carried out by ion-exchange overpressured-layer chromatography (OPLC) and 1H NMR and 13C NMR spectroscopies. The m.p. and mixed m...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/0731-7085(85)80042-x
更新日期：1985-01-01 00:00:00
abstract：:The angiotensin converting enzyme inhibitor, enalaprilat can exist in solution as cis and trans conformers which interconvert around the amide bond at room temperature. A HPLC with UV detection was performed to study the influence of various chromatographic operational conditions on both rotamers separation and elutio...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(02)00661-1
更新日期：2003-03-26 00:00:00
abstract：:Ultratrace analysis of sample components requires excellent analytical performance in terms of limits of quantitation (LoQ). Micro UHPLC coupling with sensitive tandem mass spectrometry provides state of the art solutions for such analytical problems. Decreased column volume in micro LC limits the injectable sample vo...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/j.jpba.2016.06.024
更新日期：2016-09-10 00:00:00
abstract：:Adulterations with synthetic drugs are common problems with herbal medicine and this can potentially cause serious adverse effects. It is therefore important to determine the presence of synthetic drugs in herbal medicine to ensure patients' safety. The objective of this study was to develop sensitive and specific met...
journal_title：Journal of pharmaceutical and biomedical analysis
pub_type： 杂志文章
doi：10.1016/s0731-7085(02)00637-4
更新日期：2003-02-26 00:00:00
