Abstract:
:Two polymorphs of the 1:1 fumarate salt of 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester, developed for the treatment of cognitive symptoms of schizophrenia and Alzheimer disease, have been characterized. The 2 crystal structures have been solved, and their phase relationships have been established. The space group of form I is P2₁/c with a unit-cell volume of 1811.6 (5) Å(3) with Z = 4. The crystals of form I were 2-component nonmerohedral twins. The space group of form II is P2₁/n with a unit-cell volume of 1818.6 (3) Å(3) with Z = 4. Relative stabilities have been inferred from experimental and topological P-T diagrams exhibiting an overall enantiotropic relationship between forms I and II although the solid-solid transition has never been observed. The slope of the I-II equilibrium in the P-T diagram is negative, form II is the stable phase below the solid-solid transition temperature of 371 K, and form I exhibits a stable melting equilibrium. The I-II transition temperature has been obtained from the intersection of the sublimation curves of the 2 solid forms.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Robert B,Perrin MA,Barrio M,Tamarit JL,Coquerel G,Ceolin R,Rietveld IBdoi
10.1016/j.xphs.2015.10.015subject
Has Abstractpub_date
2016-01-01 00:00:00pages
64-70issue
1eissn
0022-3549issn
1520-6017pii
S0022-3549(15)00016-7journal_volume
105pub_type
杂志文章abstract::Nipecotic acid (1), one of the most potent in vitro inhibitors of neuronal and glial gamma-amino butyric acid (GABA) uptake, is inactive as an anticonvulsant when administered systemically. To obtain in vivo active prodrugs of (1), we synthesized four new nipecotic acid esters (3-6), which were obtained by chemical co...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js980302n
更新日期:1999-05-01 00:00:00
abstract::We have recently reported the time course of acute myocardial drug uptake and simultaneous pharmacodynamic effects for metoprolol (4 mg; n = 12) and sotalol (20 mg; n = 10) in patients with ischemic heart disease. The acute pharmacodynamic effects of the two drugs included reductions in both spontaneous heart rate and...
journal_title:Journal of pharmaceutical sciences
pub_type: 临床试验,杂志文章
doi:10.1021/js9702776
更新日期:1998-02-01 00:00:00
abstract::Numerous studies have demonstrated that the administration of nonsteroidal anti-inflammatory drugs (NSAIDs) increases small intestinal permeability, and this has been suggested to be a prerequisite to enteropathy. It is believed that the inhibitory effect of chiral NSAIDs on the synthesis of prostaglandins and hence t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js960276y
更新日期:1996-11-01 00:00:00
abstract::Sucrose is a common cryoprotectant and lyoprotectant to stabilize labile biopharmaceuticals during freeze-drying and storage. Sucrose-based formulations require low primary drying temperatures to avoid collapse and monoclonal antibody (mAb) containing products need to be stored refrigerated. The objective of this stud...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2019.10.016
更新日期:2020-01-01 00:00:00
abstract::Complexation of ferrous cytochrome P450 by metabolic intermediates formed during NADPH-catalyzed metabolism of compounds structurally related to orphenadrine was studied. This so-called metabolic intermediate complexation was determined in rat liver microsomes, obtained from phenobarbital-pretreated rats, at 455 nm us...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600730723
更新日期:1984-07-01 00:00:00
abstract::Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23246
更新日期:2012-10-01 00:00:00
abstract::It has been shown that significant pore induction (electroporation) occurs in human epidermal membrane (HEM) during iontophoresis even at moderate applied voltages (1-10 V). Recent efforts in our laboratory have been aimed at quantifying HEM electroporation by examining the proportionality between flux enhancement due...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.1044
更新日期:2001-07-01 00:00:00
abstract::Targeted echogenic liposome dispersions for ultrasonic enhancement of vasoactive and pathological components of endothelium and atherosclerosis have recently been developed. The component lipids required for acoustic and targeting properties include phosphatidylcholine, phosphatidylethanolamine phosphatidylglycerol (P...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.1142
更新日期:2001-12-01 00:00:00
abstract::The determination of reactive fractal dimension was carried out using two forms of the Noyes-Whitney equation, -dQ/dt = K(Q/Q0)DR/3 and -dQ/dt = K'RDR-3 using the Richardson plot on the basis of previous data obtained by dissolution of an orthoboric acid powder. The correlation of the results provided by the two ways ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js960059x
更新日期:1996-09-01 00:00:00
abstract::The aim of this study to administer hydrocortisone (HC) percutaneously in the form of polymeric nanoparticles (NPs) to alleviate its transcutaneous absorption, and to derive additional wound-healing benefits of chitosan. HC-loaded NPs had varied particle sizes, zeta potentials, and entrapment efficiencies, when drug-t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23446
更新日期:2013-03-01 00:00:00
abstract::A method for the determination of sematilide levels in human plasma is described. After the addition of an internal standard, plasma samples are adjusted to pH 8.5 and extracted with a solution of 7.5% isopropanol in methylene chloride. Separation from co-extracted matrix constituents is performed by reversed-phase HP...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600800214
更新日期:1991-02-01 00:00:00
abstract::Optical crystallographic data were determined on a variety of newer USP drugs for which data had not been previously obtained. The ingredients in an unknown sample can be identified by polarized light microscopy by mounting small amounts of the material in successive specific refractive index liquids and determining r...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600821218
更新日期:1993-12-01 00:00:00
abstract::Mechanisms of inhibitory action of sodium salicylate on L-glutamine-D-fructose-6-phosphate aminotransferase, prepared from rat gastric mucosa, were studied. Sodium salicylate at lower concentrations (10-20 mM) inhibited reversibly aminotransferase activity by competing with fructose-6-phosphate. At higher concentratio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600640711
更新日期:1975-07-01 00:00:00
abstract::The pharmacokinetics of tamsulosin (TAM) was investigated using male Sprague-Dawley rats in which plasma alpha(1)-acid glycoprotein (alpha(1)-AGP) levels were elevated by the subcutaneous injection of 0.2 mL/kg of turpentine oil. alpha(1)-AGP levels increased about eight times after turpentine oil treatment, causing a...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/(SICI)1520-6017(200004)89:4<490::AID-JPS6>
更新日期:2000-04-01 00:00:00
abstract::Naltrexone (NTX) is an opioid antagonist used for treatment of narcotic dependence and alcoholism. Transdermal naltrexone delivery is desirable to help improve patient compliance. The purpose of this study was to increase the delivery rate of NTX across human skin by using lipophilic alkyl ester prodrugs. Straight-cha...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10239
更新日期:2002-12-01 00:00:00
abstract::The pharmacokinetics of valproic acid after oral administration of sustained-release formulations were studied in 12 healthy volunteers. The objective of the present study was to find an appropriate mathematical model to describe the complex drug intake process. The concentration of valproic acid in plasma was measure...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600831019
更新日期:1994-10-01 00:00:00
abstract::The effects of permeant charge (z) on iontophoretic-enhanced transport were investigated with synthetic Nucleopore membranes and with human epidermal membranes using a four-electrode potentiostat with side-by-side diffusion cells. The modified Nernst-Planck model (Nernst-Planck theory with an additional transport term...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js960479m
更新日期:1997-06-01 00:00:00
abstract::Poor dissolution performance is one of the challenges encountered in dosage form design of amorphous solid dispersions (ASDs). This study was aimed to investigate the effect of solid-liquid interactions of an encapsulated ASD on drug release. Drug release profiles of a molecularly interacting amorphous celecoxib solid...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22462
更新日期:2011-06-01 00:00:00
abstract::Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing metronidazole are reviewed. Metronidazole can be assigned to Biopharmaceutics Classification System Class I. Most BE studies that were identifi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22409
更新日期:2011-05-01 00:00:00
abstract::The benzenesulfonate salt of an anti-methicillin-resistant Staphylococcus aureus carbapenem antibiotic studied is a crystalline, nonhygroscopic powder which is stable at room temperature, making it an ideal compound for long-term storage. However, the limited aqueous solubility of this salt prohibits parenteral admini...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10084
更新日期:2002-04-01 00:00:00
abstract::Investigation of the leaves of Montanoa tomentosa Cerv. ssp. microcephala (Sch.-Bip.) Funk (Compositae) resulted in the isolation of three novel guaianolide sesquiterpenes, montacephalin (1), tomencephalin (2), and 5-hydroxytomencephalin (3), which were shown to be cytotoxic (P-388). The structures of these sesquiterp...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600770620
更新日期:1988-06-01 00:00:00
abstract::The aim of the present study was to investigate the mechanism of aqueous degradation of Salinosporamide A (NPI-0052; 1), a potent proteasome inhibitor that is currently in Phase I clinical trials for the treatment of cancer and is characterized by a unique beta-lactone-gamma-lactam bicyclic ring structure. The degrada...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20835
更新日期:2007-08-01 00:00:00
abstract::Surface activity and critical micelle concentrations are reported for two diuretic drugs, furosemide and triamterene. The drugs generate a liquid membrane on a supporting membrane. Transport of chloride, sodium, and potassium ions through the liquid membranes generated by the drugs was studied. The data suggest that t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600731123
更新日期:1984-11-01 00:00:00
abstract::Glasses were prepared from a number of barbiturates. The viscosities and glass transition temperatures of the glasses were dependent on the structure of the groups present on the C-5 and N-1 atoms. Solid dispersions were prepared from three selected barbiturates formulated with citric acid. The glass transition temper...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600671126
更新日期:1978-11-01 00:00:00
abstract::17-(allylamino)-17-demethoxygeldanamycin (17AAG) is a benzoquinone ansamycin Hsp90 inhibitor which has promising anticancer activity in vitro, in animal models and in clinical trials. 17AAG has poor water-solubility which is a potential problem for clinical formulation. The hydroquinone derivative of 17AAG, 17AAG hydr...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21394
更新日期:2008-12-01 00:00:00
abstract::Accurate partition coefficients K = Corg/Caq in chloroform-ammonia can be obtained by measuring the absorbance of the aqueous layer, replenishing with fresh aqueous solvent, and remeasuring the absorption after reequilibration. Provided the solute has a reasonably strong UV absorption, only 0.1-5 mg of material is req...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600730222
更新日期:1984-02-01 00:00:00
abstract::Current drug level predictions in nonlinear pharmacokinetics are based on specific pharmacokinetic models in contrast to the model-independent (structureless), dose-linearity, and superposition principles used in linear pharmacokinetics. Such model-dependent methods may not provide reliable predictions due to their in...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600730614
更新日期:1984-06-01 00:00:00
abstract::It is now becoming apparent that a common pathway of protein aggregation involves the unimolecular structural rearrangement from the native state to a slightly expanded aggregation-competent species. It is the goal of this study to understand the aggregation and the effects of buffer on the stability of IFN-tau. In th...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20471
更新日期:2006-06-01 00:00:00
abstract::The effect of the oral dosing volume (DV) on both gastric emptying and intestinal absorption was examined by analyzing the gastrointestinal disposition of a model solute, L-glucose, in rats. The amount of 14C-labeled L-glucose in the gastric and intestinal contents of sacrificed rats was measured at various times afte...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840417
更新日期:1995-04-01 00:00:00
abstract::The neuroprotective blood-brain barrier (BBB) keeps many drug candidates below therapeutic levels in the central nervous system. Glutathione PEGylated liposomal doxorubicin (2B3-101) has been developed to safely enhance the delivery of doxorubicin to brain tumors. However, doxorubicin concentration in extracellular br...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23994
更新日期:2014-07-01 00:00:00