Determination of enzyme or binding constants using generalized linear models, with particular reference to Michaelis-Menten models.

abstract：:A number of isomeric benzoylpyrroleacetic acids (1-6) were prepared and tested in vitro for rat lenses aldose reductase activity. These pyrrole derivatives are structurally related to the acidic nonsteroidal anti-inflammatory drugs. Therefore, their anti-inflammatory properties were also evaluated in the carrageenan-i...

journal_title：Journal of pharmaceutical sciences

authors： Demopoulos VJ,Rekka E

更新日期：1995-01-01 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

authors： Denora N,Potts BC,Stella VJ

更新日期：2007-08-01 00:00:00

abstract：:In vitro percutaneous permeation of betamethasone 17-valerate through excised human skin was studied. Pressure-sensitive silicone adhesive containing betamethasone 17-valerate in suspension was used as a vehicle. Steady-state flux through the split-thickness skin was similar to that through the isolated epidermis. How...

journal_title：Journal of pharmaceutical sciences

authors： Kubota K,Sznitowska M,Maibach HI

更新日期：1993-05-01 00:00:00

abstract：:Historically, recovery had been used to evaluate the data quality of plasma protein binding or tissue binding obtained from equilibrium dialysis assays. Low recovery was often indicative of high nonspecific binding, instability, or low solubility. This study showed that, when equilibrium was fully established in the d...

journal_title：Journal of pharmaceutical sciences

authors： Di L,Umland JP,Trapa PE,Maurer TS

更新日期：2012-03-01 00:00:00

abstract：:The purpose of this study was to examine the external predictability of an in vitro-in vivo correlation (IVIVC) for a metoprolol hydrophilic matrix extended-release formulation, with an acceptable internal predictability, in the presence of a range of formulation/manufacturing changes. In addition, this report evaluat...

journal_title：Journal of pharmaceutical sciences

authors： Mahayni H,Rekhi GS,Uppoor RS,Marroum P,Hussain AS,Augsburger LL,Eddington ND

更新日期：2000-10-01 00:00:00

abstract：:AZ'0908 is a novel microsomal prostaglandin E synthase-1 inhibitor intended for oral administration. Pharmacokinetic experiments in rats showed that bioavailability was much lower than anticipated and increased following pretreatment with the nonspecific cytochrome P450 (CYP) inhibitor 1-aminobenzotriazole, presumably...

journal_title：Journal of pharmaceutical sciences

authors： Bylund J,Bueters T

更新日期：2013-03-01 00:00:00

abstract：:The free radical scavenger properties of vitamin E (DL-alpha-tocopherol), a natural antioxidant, and derivatives were studied using an original in vitro method consisting of free radical production by photoirradiation of pheomelanin and direct detection of the free radicals by a physical, specific technique, electron ...

journal_title：Journal of pharmaceutical sciences

authors： Duval C,Poelman MC

更新日期：1995-01-01 00:00:00

abstract：:The in vitro diffusion of a series of substituted acetanilides across the hamster cheek pouch was studied. The keratinized epithelial layer of the cheek pouch appeared to provide the major barrier to diffusion of these compounds. Linear relationships were found for plots of log epithelial permeability (Pe) versus the ...

journal_title：Journal of pharmaceutical sciences

authors： Garren KW,Repta AJ

更新日期：1989-02-01 00:00:00

abstract：:Fibril formation (aggregation) of human and bovine insulin and six human insulin mutants in hydrochloric acid were investigated by visual inspection, Thioflavin T fluorescence spectroscopy, transmission electron microscopy (TEM), and Fourier transform infrared (FTIR) spectroscopy. The fibrillation tendencies of the wi...

journal_title：Journal of pharmaceutical sciences

authors： Garriques LN,Frokjaer S,Carpenter JF,Brange J

更新日期：2002-12-01 00:00:00

abstract：:A semi-automated protein binding assay using equilibrium dialysis (ED) and a novel mixed-matrix methodology has been developed. This method decreases mass spectrometer run time and reduces the likelihood of experimental artifacts. In this cassette-based approach, a single matrix is prepared following dialysis by mixin...

journal_title：Journal of pharmaceutical sciences

authors： Plise EG,Tran D,Salphati L

更新日期：2010-12-01 00:00:00

abstract：:In drug release systems using hydrogels as carriers, the presence of the polymer network will reduce the drug release rate, which can extend the release period. For a controlled-release process of drug, usually the ideal situation is to get a zero-order drug release rate. In this paper, the mathematical model of hydro...

journal_title：Journal of pharmaceutical sciences

authors： Xu Y,Jia Y,Wang Z,Wang Z

更新日期：2013-05-01 00:00:00

abstract：:Dextran sulfate samples from different sources were examined by 1H and 13C NMR spectroscopy to differentiate the samples on the basis of extent and sites of sulfation. The anomeric (H-1) signal proved to be a good indicator ranging from no sulfation (as in dextran) to virtually complete sulfation at positions 2 and 3,...

journal_title：Journal of pharmaceutical sciences

authors： Neville GA,Rochon P,Rej RN,Perlin AS

更新日期：1991-03-01 00:00:00

abstract：:This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

journal_title：Journal of pharmaceutical sciences

authors： Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

更新日期：2009-01-01 00:00:00

abstract：:Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...

journal_title：Journal of pharmaceutical sciences

authors： Risaliti L,Ambrosi M,Calamante M,Bergonzi MC,Lo Nostro P,Bilia AR

更新日期：2020-10-01 00:00:00

abstract：:Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

journal_title：Journal of pharmaceutical sciences

authors： Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

更新日期：2010-07-01 00:00:00

abstract：:Controlled-release delivery of 6-beta-naltrexol (NTXOL), the major active metabolite of naltrexone, via a transdermal patch is desirable for treatment of alcoholism. Unfortunately, NTXOL does not diffuse across skin at a therapeutic rate. Therefore, the focus of this study was to evaluate microneedle (MN) skin permeat...

journal_title：Journal of pharmaceutical sciences

authors： Banks SL,Pinninti RR,Gill HS,Paudel KS,Crooks PA,Brogden NK,Prausnitz MR,Stinchcomb AL

更新日期：2010-07-01 00:00:00

abstract：:Acrylic acid-esterified starch was produced by reacting starch with acrylic acid chloride. This reaction was rapid and easy to control. Introduction of acrylic groups into starch reduced the enzymatic degradability of starch (e.g., with 12 acrylic groups/100 glucose residues, approximately 75% of the degradation produ...

journal_title：Journal of pharmaceutical sciences

authors： Laakso T,Sjöholm I

更新日期：1987-12-01 00:00:00

abstract：:Gas pycnometry is applied to determine the density of solid materials. The analysis of lyophilisates is particularly challenging because of their porous structure. In this study, the density of raw materials and freeze-dried products was determined using different pycnometric methodologies and gases [helium (He), nitr...

journal_title：Journal of pharmaceutical sciences

authors： Stange U,Scherf-Clavel M,Gieseler H

更新日期：2013-11-01 00:00:00

abstract：:Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...

journal_title：Journal of pharmaceutical sciences

authors： Wu B,Sun YN

更新日期：2014-01-01 00:00:00

abstract：:The objective was to examine the influence of Pluronic block-copolymers on the interaction between the drug efflux transporter, P-glycoprotein and HIV-1 protease inhibitors (PIs). The ATPase assay determined the effect of various Pluronics on PI-stimulated P-gp ATPase activity. Cellular accumulation studies were condu...

journal_title：Journal of pharmaceutical sciences

authors： Shaik N,Pan G,Elmquist WF

更新日期：2008-12-01 00:00:00

abstract：:A rapid, sensitive, and accurate reversed-phase HPLC method has been developed for the analysis and quantification of pharmaceutical formulations containing tyrothricin (1), an antibiotic used in antiseptic buccal compressed tablets for local application. The assay has been carried out under isocratic conditions, usin...

journal_title：Journal of pharmaceutical sciences

authors： Caraballo I,Fernandez-Arevalo M,Holgado MA,Vela MT,Rabasco AM

更新日期：1994-08-01 00:00:00

abstract：:Single-dose oral administration of a commercial polychlorinated biphenyl product containing 54% chlorine provided data with which to plot the time course of total polychlorinated biphenyl and individual components in the blood of swine and sheep. Pharmacokinetic parameters describing absorption from the gut and elimin...

journal_title：Journal of pharmaceutical sciences

authors： Borchard RE,Welborn ME,Wiekhorst WB,Wilson DW,Hansen LG

更新日期：1975-08-01 00:00:00

abstract：:3-Fluoro-, 3-chloro-, and 3-bromocyclophosphamide were prepared from the reaction of trifluoromethylhypofluorite, sodium hypochlorite, and bromine with the anticancer drug cyclophosphamide. Treatment of cis- and trans-4-phenylcyclophosphamide and 5,6-benzocyclophosphamide with sodium hypochlorite afforded cis- and tra...

journal_title：Journal of pharmaceutical sciences

authors： Zon G,Ludeman SM,Ozkan G,Chandrasegaran S,Hammer CF,Dickerson R,Mizuta K,Egan W

更新日期：1983-06-01 00:00:00

abstract：:In recent years, biotechnologically derived peptide and protein-based drugs have developed into mainstream therapeutic agents. Peptide and protein drugs now constitute a substantial portion of the compounds under preclinical and clinical development in the global pharmaceutical industry. Pharmacokinetic and exposure/r...

journal_title：Journal of pharmaceutical sciences

authors： Tang L,Persky AM,Hochhaus G,Meibohm B

更新日期：2004-09-01 00:00:00

abstract：:The direct photoisomerization of (E)-4-(1-imidazoylmethyl)-cinnamic acid (IMC), a thromboxane synthetase inhibitor, to its (Z)-isomer at pH 2.0 was decelerated by beta-cyclodextrin (beta-CyD) and heptakis(2,6-di-O-methyl)-beta-cyclodextrin (DM-beta-CyD). The photostationary composition [(Z)-isomer:IMC ratio] was shift...

journal_title：Journal of pharmaceutical sciences

authors： Hirayama F,Utsuki T,Uekama K,Yamasaki M,Harata K

更新日期：1992-08-01 00:00:00

abstract：:This work establishes a predictive model that explicitly recognizes microstructural parameters in the description of the overall mass uptake and local gradients of moisture into tablets. Model equations were formulated based on local tablet geometry to describe the transient uptake of moisture. An analytical solution ...

journal_title：Journal of pharmaceutical sciences

authors： Klinzing GR,Zavaliangos A

更新日期：2016-08-01 00:00:00

abstract：:Aqueous solubilities for some guanine derivatives were estimated by semiempirical equations developed by Yalkowsky and Valvani1 using the data for partition coefficient and melting temperature. It was shown that in the case of guanine derivatives examined in this study, the solubility values could not be estimated ade...

journal_title：Journal of pharmaceutical sciences

authors： Kristl A

更新日期：1999-01-01 00:00:00

abstract：:The utility of inhaled protein therapeutics to treat lung-resident diseases is limited by protein degradation in the lungs and rapid clearance. This study therefore aimed to evaluate the impact of PEGylation on the lung and systemic exposure of interferon (IFN) α2 after intratracheal administration to rats. An inverse...

journal_title：Journal of pharmaceutical sciences

authors： Mcleod VM,Chan LJ,Ryan GM,Porter CJ,Kaminskas LM

更新日期：2015-04-01 00:00:00

abstract：:Terbinafine is an allylamine antifungal agent that is highly lipophilic and keratophilic. The aim of this study was to investigate terbinafine distribution in peripheral and visceral tissues after intravenous administration to rats. Terbinafine, 6 mg/kg, was administered to 33 male Sprague-Dawley rats via a jugular ve...

journal_title：Journal of pharmaceutical sciences

authors： Hosseini-Yeganeh M,McLachlan AJ

更新日期：2001-11-01 00:00:00

abstract：:A precursor-dependent model of indirect pharmacodynamic response which can describe tolerance and rebound was characterized in terms of the effects of changes in the fundamental properties of the drug on its response profiles. The model extends previous models by considering inhibition or stimulation of production of ...

journal_title：Journal of pharmaceutical sciences

authors： Sharma A,Ebling WF,Jusko WJ

更新日期：1998-12-01 00:00:00