Abstract:
PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on 96-well quartz plates with a Raman microscope. Appearance and crystalline forms of salts prepared on 96-well plates were observed by polarizing light microscope and Raman microscope, respectively. Based on the results of the salt screening, tamoxifen citrate and fumarate salts were prepared on a large scale. The salts prepared were characterized by powder X-ray diffractometry (PXRD) and ion chromatography. RESULTS:The results of the multiwell salt screening indicated that tamoxifen has a tendency toward the formation of mono salt as opposed to hemi salt with polybasic acid, and that most of tamoxifen salts gave several potential polymorphic forms. PXRD patterns of scaled-up tamoxifen citrate and fumarate salts suggested that the same crystalline form was obtained from the binary mixture regardless of molar ratios of 2:1 or 1:1 (tamoxifen/acid). The crystalline forms obtained were tamoxifen monocitrate and monofumarate salts as measured by ion chromatography. CONCLUSIONS:Salt screening on multiwell plates with a Raman microscope provided novel insight into the characteristics prediction of the stoichiometrical salts in addition to potential polymorph information. Based on the stoichiometrical information of salts, the amount of compound and time required for crystalline form selection of drug candidates would be significantly reduced.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Kojima T,Onoue S,Murase N,Katoh F,Mano T,Matsuda Ydoi
10.1007/s11095-006-9644-7subject
Has Abstractpub_date
2006-04-01 00:00:00pages
806-12issue
4eissn
0724-8741issn
1573-904Xjournal_volume
23pub_type
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015852732512
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abstract::In order to study the influence of hydrogen bonding in the amide backbone of a peptide on permeability across a cell membrane, a series of tetrapeptide analogues was prepared from D-phenylalanine. The amide nitrogens in the parent oligomer were sequentially methylated to give a series containing from one to four methy...
journal_title:Pharmaceutical research
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更新日期:2003-12-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011018525121
更新日期:2001-01-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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doi:10.1023/A:1016381017357
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018997101542
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012143915886
更新日期:1997-10-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:2005-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2010-09-01 00:00:00
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更新日期:2015-02-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1014430631844
更新日期:2002-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1013081710135
更新日期:2001-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2013-01-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2019-07-31 00:00:00
abstract::Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. DTZ undergoes extensive metabolism yielding several metabolites, some of which are active like N-desmethyldiltiazem (MA), desacetyldiltiazem (M1) and N-desmethyl,desacetyldiltiazem (M2). Due to the nature of its biotr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016226601988
更新日期:1995-04-01 00:00:00
abstract::For the last 50 years we have known of a broad-spectrum agent tilorone dihydrochloride (Tilorone). This is a small-molecule orally bioavailable drug that was originally discovered in the USA and is currently used clinically as an antiviral in Russia and the Ukraine. Over the years there have been numerous clinical and...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02799-8
更新日期:2020-03-25 00:00:00
abstract:PURPOSE:To evaluate 26 marketed oncology drugs for time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes. Evaluate TDI-positive drugs for potential to generate reactive intermediates. Assess clinical drug-drug interaction (DDI) risk using static mechanistic models. METHODS:Human liver microsomes and CYP-spe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0724-6
更新日期:2012-07-01 00:00:00