Abstract:
:Cevimeline is muscarinic receptor agonist which increases secretion of exocrine glands. Cevimeline base is a liquid (m.p. 20-25 °C) at ambient conditions, therefore its pharmaceutical formulation as a solid hydrochloride hemihydrate has been developed. The synthesis of cevimeline yields its cis- and trans-isomers and only the cis-isomer is recognized as the API and used in the finished formulation. In this study structural and physicochemical investigations of hydrochloride hemihydrates of cis- and trans-cevimelines have been performed. Single crystal X-ray analyses of both cis- and trans-isomers of cevimeline are reported here for the first time. It was found that the cis-isomer, the API, has less dense crystal packing, lower melting point and higher solubility in comparison to the trans-isomer.
journal_name
J Pharm Biomed Analjournal_title
Journal of pharmaceutical and biomedical analysisauthors
Stepanovs D,Tetere Z,Rāviņa I,Kumpiņš V,Zicāne D,Bizdēna Ē,Bogans J,Novosjolova I,Grigaloviča A,Meri RM,Fotins J,Čerkasovs M,Mishnev A,Turks Mdoi
10.1016/j.jpba.2015.11.006subject
Has Abstractpub_date
2016-01-25 00:00:00pages
404-409eissn
0731-7085issn
1873-264Xpii
S0731-7085(15)30226-0journal_volume
118pub_type
杂志文章abstract::The methods for analysis of platinum-based anti-cancer drugs in biological media are reviewed in this paper. Although emphasis is placed on cisplatin, attention is also given to several of its analogues (carboplatin, iproplatin) and their degradation and biotransformation products. In an introductory section a short d...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章,评审
doi:10.1016/0731-7085(90)80003-8
更新日期:1990-01-01 00:00:00
abstract::The pharmaceutical industry is under stringent regulations on quality control of their products because is critical for both, productive process and consumer safety. According to the framework of "process analytical technology" (PAT), a complete understanding of the process and a stepwise monitoring of manufacturing a...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2015.05.002
更新日期:2015-10-10 00:00:00
abstract::Alkyl quinolone molecules 2-heptyl-4-quinolone (HHQ) and 2-heptyl-3-hydroxy-4(1H)-quinolone (PQS) are important quorum sensing signals, which play a mediatory role in the pathogenesis of acute and chronic Pseudomonas aeruginosa infection. A targeted approach inhibiting the bacterial 'multiple virulence factor regulon'...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2017.02.034
更新日期:2017-05-30 00:00:00
abstract::The caseins comprise a milk protein fraction of high nutritional value and, as more recently discovered, of immunologic relevance. In particular, αS1-casein (CSN1S1) is of interest being a potential autoantigen. So far, the concentration of caseins in human milk was primarily determined by indirect methods. The aim of...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2014.10.034
更新日期:2015-01-25 00:00:00
abstract::Imidazol(in)e derivatives, having the chemical structure similar to clonidine, exert diverse pharmacological activities connected with their interactions with alpha2-adrenergic receptors, e.g. hypotension, bradycardia, sedation as well as antinociceptive, anxiolytic, antiarrhythmic, muscle relaxant and mydriatic effec...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2017.03.053
更新日期:2017-09-10 00:00:00
abstract::A reversed-phase high-performance liquid chromatographic (RP-HPLC) separation method with UV spectrophotometric detection has been developed for the determination of major components in leaves and caulomas of Schisandra chinensis Baill. The flavonols (quercetin and kaempferol) and (E)-cinnamic acid were analysed after...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/s0731-7085(00)00539-2
更新日期:2001-03-01 00:00:00
abstract::The coupling of sequential injection analysis (SIA) and fluorimetric solid phase transduction is here applied to the determination of paracetamol in pharmaceuticals. The reaction product between the analyte and sodium nitrite in acidic medium is inserted, after alkalinization, in the system. This product is transitori...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2007.05.004
更新日期:2007-10-18 00:00:00
abstract::The recent interest in RX77368 for the treatment of Motor Neurone Disease (MND) has led to the requirement for an assay (RIA) capable of detecting the peptide at low levels in plasma. Several drug conjugates were prepared in which RX77368 was covalently linked to larger proteins, e.g. bovine serum albumin, keyhole lim...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/0731-7085(91)80230-7
更新日期:1991-01-01 00:00:00
abstract::A study was performed to compare the pharmacokinetics of major bioactive analytes in rhubarb plants to explore the pharmacological differences between raw pieces (RP) and steamed pieces (SP) of rhubarb. A rapid and efficient ultra-performance liquid chromatographic coupled with mass/mass spectrometry (UPLC-MS/MS) meth...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2019.04.002
更新日期:2019-07-15 00:00:00
abstract::A method is described for analysis of the tetracycline antibiotic minocycline using capillary zone electrophoresis. Potential impurities are 4-epiminocycline, 6-deoxy-6-demethyltetracycline, 7-didemethylminocycline, 7-monodemethylminocycline and 9-minocycline. Method development was undertaken with a mixture consistin...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/s0731-7085(96)01732-3
更新日期:1996-06-01 00:00:00
abstract::Charge variant profiling of therapeutic proteins is required by the International Council for Harmonisation guidelines and is traditionally performed by capillary electrophoresis or ion exchange chromatography. Recently, improvements in the hyphenation of capillary electrophoresis with mass spectrometry and the introd...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2020.113218
更新日期:2020-06-05 00:00:00
abstract::A study was carried out to investigate compatibility of atenolol, a beta(1) blocker, with a variety of pharmaceutical excipients. The binary mixtures (1:1) of atenolol with the excipients were stored for 1 month at 40 degrees C/75% RH. The samples were directly observed for the physical changes, and also analyzed by a...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2009.01.014
更新日期:2009-05-01 00:00:00
abstract::Etimicin intermediate 3,2″,6″-N,N,N-triacetyl gentamicin C1a (P1), is a key intermediate of etimicin, which is a semi-synthetic aminoglycoside antibiotic effective to both gram-positive and gram-negative bacteria infections. Four major related impurities of P1 were detected by HPLC-ELSD and ESI-MS(n) methods. Weakly a...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2014.04.024
更新日期:2014-08-01 00:00:00
abstract::In LC method development, the choice of suitable experimental conditions is often challenging for the analyst because of the huge diversity of stationary phases, mobile phase pH and organic modifiers, that could significantly alter the selectivity. The influence of these parameters on selectivity was experimentally te...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2012.01.019
更新日期:2012-04-07 00:00:00
abstract::The colorimetric method of evaluation of antioxidant activity by scavenging 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical is with certain shortcomings like failure to indicate antioxidant activity of certain drugs and interference from color pigments of natural products. A specific HPLC method was developed for ev...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2005.07.042
更新日期:2006-02-13 00:00:00
abstract::An LC procedure was developed to separate diatrizoate sodium from three known impurities. These impurities are 2,4- and 2,6-diiodo-3,5-diacetamidobenzoic acid (DDZA), and the free amine (5-acetamido-3-amino-2,4,6-triiodobenzoic acid). The separation was achieved using a Hamilton, PRP-X100, anion exchange column. The r...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/s0731-7085(97)00007-1
更新日期:1997-09-01 00:00:00
abstract::In this brief review a superficial introduction is given to the important area of biologically active carbohydrates. The complexity of carbohydrate chemistry is considered and the possible uses of carbohydrates as drugs and diagnostic agents are outlined. The analytical tools and methods that are especially useful for...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/0731-7085(86)80007-3
更新日期:1986-01-01 00:00:00
abstract::Tramadol is a centrally acting analgesic drug used in veterinary and human clinical practice. Its metabolism has been largely characterized in human being but is still long to be comprehended in several animal species, especially in the dog. The aim of the present study was to develop and validate a new analytical pro...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2010.03.016
更新日期:2010-10-10 00:00:00
abstract::An ion mobility spectrometry (IMS) method was developed to screen for the presence of undeclared synthetic erectile dysfunction (ED) drugs or drug analogues in herbal dietary supplements claiming to enhance male sexual performance. Ion mobility spectra of authenticated reference materials including three FDA approved ...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2008.12.002
更新日期:2009-04-05 00:00:00
abstract::SU101 or leflunomide, has been studied extensively because of its anti-cancer and immunomodulating properties. The parent isoxazole compound is converted in vitro and metabolized in vivo to an open ring isomeric form, SU0020. Several pharmacological activities have been reported for the parent and metabolite compounds...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/s0731-7085(01)00654-9
更新日期:2002-05-15 00:00:00
abstract::A rapid, sensitive and specific high-performance liquid chromatographic (HPLC) assay is reported for the determination of 4-amino-1-hydroxybutane-1, 1-diphosphonic acid (AHBuDP) monosodium salt trihydrate, a new inhibitor of bone resorption. The compound does not demonstrate any intrinsic UV properties and thus pre-co...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/0731-7085(89)80186-4
更新日期:1989-01-01 00:00:00
abstract::Bromadiolone (BRD), a substituted 4-hydroxycoumarin derivative, is known to possess anti-coagulant activity with acute toxicity. In this paper, we report a study on the interaction of bromadiolone with the plasma proteins bovine serum albumin (BSA) and human serum albumin (HSA), using the intrinsic fluorescence emissi...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2005.01.023
更新日期:2005-07-01 00:00:00
abstract::The Sceletium plant has been reported to contain psychoactive alkaloids, specifically mesembrine, mesembrenone, mesembrenol and other related alkaloids. Sceletium is marketed through health shops and on the internet as dried plant powder and as pharmaceutical dosage forms. The objectives of this research was to develo...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2008.01.002
更新日期:2008-09-29 00:00:00
abstract::A simple and rapid high performance liquid chromatography electrospray ionization ion-trap tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the quantitative determination of esculentoside A (EsA) in dog plasma using ginsenoside Rg1 as the internal standard (IS). After liquid-liquid extra...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2012.09.002
更新日期:2013-01-01 00:00:00
abstract::The purpose of this study was to investigate the in vitro release of 5-aminosalicylic acid from single extrudates by UV imaging and to explore the technique as a visualization tool for detecting film coating defects on extrudates coated with a thin ethyl cellulose layer. 5-Aminosalicylic acid extrudates were film coat...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2013.04.028
更新日期:2013-09-01 00:00:00
abstract::As a part of our investigations on the content and stability of herbal drug preparations, we evaluated the content and stability of tinctures and mother tinctures of Hawthorn leaves and flowers and Hawkweed. Hawthorn preparations are mainly used by patients with cardiac diseases; Hawkweed is employed for the treatment...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2007.01.046
更新日期:2007-05-09 00:00:00
abstract::3'-Deoxy-3'-[18F]fluorothymidine ([18F]-FLT) has recently been described as a positron emission tomography (PET) radiopharmaceutical for visualizing cellular proliferation in vivo. All published radiosyntheses of [18F]-FLT provide crude products that must be purified before injection to human. This study describes a r...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2007.04.034
更新日期:2007-09-21 00:00:00
abstract::Stir-bar Sorptive Extraction (SBSE) in combination with thermal desorption and gas chromatography-mass spectrometry (TD-GC-MS) is widely accepted as the gold-standard analysis method for trace amounts of organic substances, including leachables in aqueous matrices. Meanwhile, as far as pharmaceutical quality control i...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/j.jpba.2018.01.045
更新日期:2018-04-15 00:00:00
abstract::A selective and sensitive isocratic high-performance liquid chromatographic (HPLC) method was developed for the quantitative analysis of low concentrations of fluoxetine (FLX) in human plasma, with ultra-violet detection at 226 nm. A reversed-phase column, LiChrospher 60 RP-Select B (125 x 3 mm i.d., 5 microm) (Merck)...
journal_title:Journal of pharmaceutical and biomedical analysis
pub_type: 杂志文章
doi:10.1016/s0731-7085(00)00367-8
更新日期:2000-11-01 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