Abstract:
:p-Bromospiperone was prepared from the reaction of spiperone with bromine. It was tested for dopamine receptor binding affinity in vitro and its ability to stimulate prolactin secretion in vivo. The results indicate no significant change of biological activities due to the bromination of spiperone.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Huang CC,Friedman AM,So R,Simonovic M,Meltzer HYdoi
10.1002/jps.2600690835subject
Has Abstractpub_date
1980-08-01 00:00:00pages
984-6issue
8eissn
0022-3549issn
1520-6017pii
S0022-3549(15)43345-3journal_volume
69pub_type
杂志文章abstract::New methods are being applied to distinguish silicone oil droplets from subvisible particles in therapeutic protein formulations. The need to standardize these methods and compare them to established methods is critical to increase the understanding of the risks from protein aggregation and other subvisible particulat...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23554
更新日期:2013-06-01 00:00:00
abstract::One manifestation of cystic fibrosis (CF) is the presence of a viscid mucus secretion in the lungs. The clearance of this mucus is significantly slower than in "normals" due to uncoordinated beating of the cilia and the increased viscosity of the mucus. In these studies, the permeabilities of p-aminosalicylic acid, is...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js950381s
更新日期:1996-06-01 00:00:00
abstract::We report the preparation and structural characterization of a family of primary alcohol solvates of a small-molecule hydrochloride salt. The structures of the solvates are probed by powder and single crystal X-ray diffraction, and the compounds were additionally characterized by polarized light microscopy, thermograv...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2018.01.020
更新日期:2018-06-01 00:00:00
abstract::A recirculation technique was used to study the first-order kinetics of intestinal absorption of un-ionized sulfadiazine, sulfamerazine, and sulfamethazine in rats in situ at 32, 35, and 38 degrees C. The absorption rate constant (Kab) of each sulfonamide increased with increase in temperature and, at each temperature...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600821208
更新日期:1993-12-01 00:00:00
abstract::Therapeutic use of anti-inflammatory steroids is limited due to their potential suppressive effects on pituitary-adrenal function and the immune system. Based on the antedrug concept, a new class of potent locally active compounds with reduced risk of side effects has been synthesized from prednisolone by introducing ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600790716
更新日期:1990-07-01 00:00:00
abstract::In vivo studies were conducted in rats to determine the role of hyperglycemia and hypoinsulinemia in the previously reported reduction in the hepatic accumulation and increase in the serum concentrations of 70-kDa fluorescein-dextran (FD-70) in diabetic (D) rats. The serum, urine, and hepatic concentrations of FD-70 w...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600830719
更新日期:1994-07-01 00:00:00
abstract::The antimalarial endoperoxides, such as artemisinin, are postulated to exert their potent parasiticidal activity via the formation of reactive intermediates in the iron-rich infected erythrocyte. The in vitro chemical reaction profile of putative endoperoxide antimalarials and ferrous iron is often qualitatively used ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20400
更新日期:2005-08-01 00:00:00
abstract::The dissolution behavior and absorption of mefenamic acid following oral and rectal administration from drug:egg albumin solid dispersions have been studied in comparison with those of the drug alone. The interaction of drug with egg albumin in aqueous solution and solid state were examined by solubility analysis, dia...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600800517
更新日期:1991-05-01 00:00:00
abstract::The objective of this study was to generate a water-soluble thiolated chitosan to enable the permeation-enhancing effect of chitosan at pH of at least 5.5 without losing the advantages of improved mucoadhesive properties. Therefore, the thiol-bearing polyoxyethylene ligand {O-(3-carboxylpropyl)-O'-[2-[3-mercaptopropio...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23832
更新日期:2014-02-01 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::Using quantitative structure-retention relationships (QSRR) methodologies the Kovats gas chromatographic retention indices for both apolar (DB-1) and polar (DB-Wax) columns for 48 compounds from Ylang-Ylang essential oil were empirically predicted from calculated and experimental data on molecular structure. Topologic...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js960196u
更新日期:1997-05-01 00:00:00
abstract::Three dissolution apparatus, the rotating basket, the rotating paddle, and the rotating filter--stationary basket, were evaluated for their suitability as production control tools and their relation to blood level studies in dogs. The rotating basket and rotating paddle assemblies were easier to use and less variable ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600671226
更新日期:1978-12-01 00:00:00
abstract::A program is described that permits iterative least-squares nonlinear regression fitting of polyexponential curves using the Hewlett Packard HP 41 CV programmable calculator. The program enables the analysis of pharmacokinetic drug level profiles with a high degree of precision. Up to 15 data pairs can be used, and in...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600740510
更新日期:1985-05-01 00:00:00
abstract::Locally recurrent prostate cancer can lead to significant morbidity, metastasis, and even death. The objective of this study was to evaluate the efficacy of an injectable polymeric paste formulation containing paclitaxel against orthotopic prostate tumor in rats. The Dunning R-3327 rat prostate adenocarcinoma is exper...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21492
更新日期:2009-03-01 00:00:00
abstract::The previous paper in this series introduced an X-ray diffraction quantitation method for the polymorphic content in tablets made of pure components. Before the method could be transferred, further studies were required to explain the commonly observed X-ray intensity variation in analyzing compacts. The literature ty...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.10480
更新日期:2003-12-01 00:00:00
abstract::It is understood that a potential issue for drugs with poor aqueous solubility is low oral absorption. If oral exposure issues arise when working with a low solubility drug candidate, the common action is to rely on enabling formulations to solve the issue. However, this approach becomes troublesome in the pre-clinica...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2016.04.003
更新日期:2016-06-01 00:00:00
abstract::The relationship between chemical structure and antifungal activity of quaternary imidazolium compounds is analyzed. The compounds are described by a set of condition attributes concerning structure and by a decision attribute concerning activity. The description builds up an information system. The smallest set of co...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840225
更新日期:1995-02-01 00:00:00
abstract::The aim of this study was to prepare and characterize thiolated chitosan (TC) nanoparticles (NPs) of tizanidine HCl (TZ) and to evaluate its transport across monolayer of RPMI 2650 cells (Human nasal septum carcinoma cell line) followed by assessment of their pharmacokinetic and pharmacodynamic attributes, after intra...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.22780
更新日期:2012-02-01 00:00:00
abstract::Regular insulin, NPH insulin, glargine insulin, calcitonin, and human growth hormone were administered to rats nasally with 0.125% tetradecyl-beta-D-maltoside (TDM), or at various times after TDM treatment. Absorption of all five peptides was enhanced initially and diminished in a time-dependent manner as the interval...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21977
更新日期:2010-04-01 00:00:00
abstract::L-3-(3-Hydroxy-4-pivaloyloxyphenyl)alanine (1, NB-355) is a novel L-dopa prodrug. After oral administration with carbidopa in rats, 1 demonstrated 2.3 times longer duration (MRT) and 1.4 times larger bioavailability (AUC) on plasma L-dopa concentrations than those of L-dopa itself. Similar results were obtained in dog...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600780703
更新日期:1989-07-01 00:00:00
abstract::In this paper the development of a new preparation method of liposomes containing a water soluble marker (fluorescein isothiocyanate-dextran (FITC-dextran) or zinc phthalocyanine tetrasulfonic acid (TSZnPc) using supercritical carbon dioxide (called "the supercritical liposome method") is described. The apparatus used...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1021/js960403q
更新日期:1997-08-01 00:00:00
abstract::Sonication process is regularly adopted for dispersing single-walled carbon nanotubes (SWCNTs) in an aqueous medium. This can be achieved by either covalent functionalization of SWCNTs with strong acid or by noncovalent functionalization using dispersants that adsorb onto the surface of SWCNTs during dispersion. Becau...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24483
更新日期:2015-08-01 00:00:00
abstract::Peptidomimetic drugs have favorable bioavailability owing to H(+)/peptide transporter 1 (PEPT1) located in the intestine. Sartans are commonly used and likely coadministered with peptidomimetic drugs in the clinic; however, in vivo interactions between sartans and peptidomimetic drugs have not been systemically unders...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.23805
更新日期:2014-02-01 00:00:00
abstract::In the present work, authors produced tablets of anhydrous sodium naproxen by wet granulation using a high-shear mixer-granulator. Drug hydrated to the tetrahydrated form, as observed by X-ray powder diffractometry. After wet granulation, authors then performed two different drying procedures, obtaining granules of di...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.21400
更新日期:2008-12-01 00:00:00
abstract::Previously available GLC methods for ethambutol may only be used to measure quantities of drugs much greater than those found in biological fluids such as plasma and dialysate. A previously published GLC method for plasma samples is extended to measure ethambutol in dialysate. A second GLC method, involving derivatiza...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600670407
更新日期:1978-04-01 00:00:00
abstract::In this work, a novel risk-based methodology for lot release is proposed. Its objective is to assess the risk that a lot declared to have passed truly meets product specifications. The methodology consists of 3 parts: adaptive sample size determination, estimation of the probability that the product was within specifi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1016/j.xphs.2019.10.011
更新日期:2020-02-01 00:00:00
abstract::The quantitative analysis of a new pharmaceutically active amine hydrochloride is described. Samples are extracted with chloroform. A yellow amine-dye complex is formed by buffering a sample-bromthymol blue solution at pH 8.5 +/- 0.1 and subsequently extracted with chloroform. The complex is treated with 0.01 N NaOH t...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600651035
更新日期:1976-10-01 00:00:00
abstract::This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.24059
更新日期:2014-08-01 00:00:00
abstract::The peptide hormone calcitonin (CT) is a potent drug for the therapy of different bone diseases. Salmon CT (sCT) is reported to be more active than human CT (hCT). Human CT, but not sCT, has a strong tendency to aggregate and fibrillate in aqueous solutions. Recent investigations of the fibrillation mechanisms contrib...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.2600840610
更新日期:1995-06-01 00:00:00
abstract::To date, research on the effect of single nucleotide polymorphisms (SNPs) on P-glycoprotein (P-gp) expression and functionality has rendered inconsistent results. This study systematically evaluates the impact of MDR1 haplotypes (1236/2677, 1236/3435, 2677/3435, 1236/2677/3435) on P-gp functionality compared to indivi...
journal_title:Journal of pharmaceutical sciences
pub_type: 杂志文章
doi:10.1002/jps.20717
更新日期:2006-10-01 00:00:00