Abstract：
PURPOSE:Calculation of the ideal solubility of a crystalline solute in a liquid solvent requires knowledge of the difference in the molar heat capacity at constant pressure of the solid and the supercooled liquid forms of the solute, delta Cp. Since this parameter is not usually known, two assumptions have been used to simplify the expression. The first is that delta Cp can be considered equal to zero; the alternate assumption is that the molar entropy of fusion, delta Sf, is an estimate of delta Cp. Reports claiming the superiority of one assumption over the other, on the basis of calculations done using experimentally determined parameters, have appeared in the literature. The validity of the assumptions in predicting the ideal solubility of five structurally unrelated compounds of pharmaceutical interest, with melting points in the range 420 to 470 K, was evaluated in this study. METHODS:Solid and liquid heat capacities of each compound near its melting point were determined using differential scanning calorimetry. Linear equations describing the heat capacities were extrapolated to the melting point to generate the differential molar heat capacity. RESULTS:Linear data were obtained for both crystal and liquid heat capacities of sample and test compounds. For each sample, ideal solubility at 298 K was calculated and compared to the two estimates generated using literature equations based on the differential molar heat capacity assumptions. CONCLUSIONS:For the compounds studied, delta Cp was not negligible and was closer to delta Sf than to zero. However, neither of the two assumptions was valid for accurately estimating the ideal solubility as given by the full equation.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Neau SH,Bhandarkar SV,Hellmuth EWdoi
10.1023/a:1012148910975subject
Has Abstractpub_date
1997-05-01 00:00:00pages
601-5issue
5eissn
0724-8741issn
1573-904Xjournal_volume
14pub_type
杂志文章abstract：PURPOSE:To evaluate organic anion transporter-mediated drug-drug interaction (DDI) potential for individual active components of Danshen (Salvia miltiorrhiza) vs. combinations using in vitro and in silico approaches. METHODS:Inhibition profiles for single Danshen components and combinations were generated in stably-ex...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2014-12-01 00:00:00
abstract：PURPOSE:Labrasol and Gelucire 44/14 are defined admixtures of acylglycerols and PEG esters which are substrates for digestive lipases. METHODS:We investigated their in vitro gastrointestinal lipolysis to understand which compounds are, after digestion, responsible for keeping poorly water-soluble drugs in solution. Th...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9906-2
更新日期：2009-08-01 00:00:00
abstract：PURPOSE:To examine the inhibitory potential of enalapril [and other angiotensin converting enzyme (ACE) inhibitors] on glycylsarcosine (GlySar) transport by the high-affinity renal peptide transporter. METHODS:Studies were performed in rabbit renal brush border membrane vesicles in which the uptake of radiolabeled Gly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018847818766
更新日期：1999-05-01 00:00:00
abstract：PURPOSE:To provide the physicochemical properties of vitrified trehalose for predicting its recrystallization. METHODS:Thin films of vitrified trehalose solutions were prepared at room temperature and exposed to various humid and temperature atmospheres. The in-situ amount of retained water in the vacuum-dried trehalo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-018-2420-7
更新日期：2018-05-10 00:00:00
abstract：PURPOSE:The purpose of this study was to use a replicate designed trial to assess the overall, intra- and inter-subject variabilities in pharmacokinetic parameters of CGP 33101 after oral administration of tablets relative to that of powder suspended in water, and to determine the relative proportion of the intra-subje...
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：1995-12-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1013391001141
更新日期：2001-12-01 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：2008-10-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0713-9
更新日期：2012-07-01 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2007-03-01 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：2008-09-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1988-z
更新日期：2016-11-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018813700535
更新日期：1999-06-01 00:00:00
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pub_type： 杂志文章
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更新日期：2008-04-01 00:00:00
abstract：PURPOSE:To investigate the possible pathways for transport of wheat germ agglutinin conjugated PEG-PLA nanoparticles (WGA-NP) into the brain after nasal administration. METHODS:The nose-to-brain pathways were investigated using WGA-NP containing 6-coumarin (as a fluorescent marker) and (125)I-labeled WGA-NP. Ex vivo i...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0641-0
更新日期：2012-02-01 00:00:00
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pub_type： 杂志文章,评审
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更新日期：2012-05-01 00:00:00
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pub_type： 杂志文章
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更新日期：2005-11-01 00:00:00
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pub_type： 杂志文章
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更新日期：2006-06-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016361921803
更新日期：1985-01-01 00:00:00
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更新日期：2015-01-01 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：2003-10-01 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：1986-02-01 00:00:00
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更新日期：2018-08-30 00:00:00
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journal_title：Pharmaceutical research
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更新日期：2005-08-01 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：2010-06-01 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：2013-03-01 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：2003-09-01 00:00:00
abstract：PURPOSE:For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability. We hypothesized that this assumption was invalid for hig...
journal_title：Pharmaceutical research
pub_type： 临床试验,杂志文章
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更新日期：1996-06-01 00:00:00
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 ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2006-04-01 00:00:00
