Quantitative structure/property relationship analysis of Caco-2 permeability using a genetic algorithm-based partial least squares method.

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：:Dynamic imaging analysis instruments are used for sizing particles of different types that might appear in a biopharmaceutical. These instruments are calibrated using polystyrene latex microspheres in water, which is a significantly different system than the typical particles imaged in a formulation. We show how the i...

journal_title：Journal of pharmaceutical sciences

authors： Cavicchi RE,Ripple DC,Bioprocess Measurements Group.

更新日期：2020-01-01 00:00:00

abstract：:The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 00:00:00

abstract：:Water evaporation rates were measured from thin samples of a model layered structure of stratum corneum lipids with 32% water. A model with only free fatty acids present gave the lowest evaporation rates, while a model with only oleic acid gave values approximately 50% higher. Using the total lipid spectrum of stratum...

journal_title：Journal of pharmaceutical sciences

authors： Friberg SE,Kayali I

更新日期：1989-08-01 00:00:00

abstract：:An immune response for a nasal ovalbumin (OVA) powder formulation with an applied nasal delivery platform technology, consisting of a powdery nasal carrier and a device, was evaluated in monkeys with similar upper respiratory tracts and immune systems to those of humans, in order to assess the applicability to a vacci...

journal_title：Journal of pharmaceutical sciences

authors： Torikai Y,Sasaki Y,Sasaki K,Kyuno A,Haruta S,Tanimoto A

更新日期：2020-12-03 00:00:00

abstract：:This study explored the ability to conduct primary drying during lyophilization at product temperatures above the glass transition temperature of the maximally freeze-concentrated solution (Tg′) in amorphous formulations for four proteins from three different classes. Drying above Tg′ resulted in significant reduction...

journal_title：Journal of pharmaceutical sciences

authors： Depaz RA,Pansare S,Patel SM

更新日期：2016-01-01 00:00:00

abstract：:Tryptophan (Trp) oxidation in proteins leads to a number of events, including changes in color, higher order structure (HOS), and biological activity. We describe here a number of new findings through a comprehensive characterization of 6 monoclonal antibodies (mAbs) following selective oxidation of Trp residues by 2,...

journal_title：Journal of pharmaceutical sciences

authors： Barnett GV,Balakrishnan G,Chennamsetty N,Hoffman L,Bongers J,Tao L,Huang Y,Slaney T,Das TK,Leone A,Kar SR

更新日期：2019-06-01 00:00:00

abstract：:The ability to produce and isolate relatively pure amounts of relevant degradation products is key to several aspects of drug product development: (a) aid in the unambiguous structural identification of such degradation products, fulfilling regulatory requirements to develop safe formulations (International Conference...

journal_title：Journal of pharmaceutical sciences

authors： Nanda KK,Mozziconacci O,Small J,Allain LR,Helmy R,Wuelfing WP

更新日期：2019-04-01 00:00:00

abstract：:Previously, 1 mL of purified water (hyposmotic) or saline (isosmotic) which dissolved 200 μM of FITC-dextran (FD-4), a nonabsorbable marker, was orally administered to rats, and luminal concentration-time profile of FD-4 was directly measured. In this study, at first, luminal FD-4 concentration was measured after oral...

journal_title：Journal of pharmaceutical sciences

authors： Tanaka Y,Higashino H,Kataoka M,Yamashita S

更新日期：2020-06-01 00:00:00

abstract：:Three aspirin derivatives, aspirin phenylalanine ethyl ester, aspirin phenylalanine amide, and aspirin phenyllactic ethyl ester, were investigated with respect to their hydrolysis by alpha-chymotrypsin. Of the three compounds, aspirin phenylalanine ethyl ester was the best substrate, with kcat = 25 sec-1 and Km = 1.3 ...

journal_title：Journal of pharmaceutical sciences

authors： Banerjee PK,Amidon GL

更新日期：1981-12-01 00:00:00

abstract：:Angiogenesis--process of new blood-vessel growth from existing vasculature--is an integral part of both normal developmental processes and numerous pathologies such as cancer, ischemic diseases and chronic inflammation. Angiogenesis plays a crucial role facilitating tumour growth and the metastatic process, and it is ...

journal_title：Journal of pharmaceutical sciences

authors： Mauriz JL,González-Gallego J

更新日期：2008-10-01 00:00:00

abstract：:The correlation between dynamic surface properties of drug molecules and drug absorption in two common in vitro models of the intestinal wall (Caco-2 monolayers and rat intestinal segments) has been investigated. A homologous series of beta-adrenoreceptor antagonists were used as model compounds. Dynamic molecular sur...

journal_title：Journal of pharmaceutical sciences

authors： Palm K,Luthman K,Ungell AL,Strandlund G,Artursson P

更新日期：1996-01-01 00:00:00

abstract：:It is shown, using oxalic acid dihydrate as a model, that nonisothermal recrystallization of powders gives rise to particle size distributions which approach log-normality in many cases. The number of particles formed is, primarily, a function of the nucleation rate constants and the particle size distribution, i.e., ...

journal_title：Journal of pharmaceutical sciences

authors： Carstensen JT,Rodriguez-Hornedo N

更新日期：1985-12-01 00:00:00

abstract：:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of C...

journal_title：Journal of pharmaceutical sciences

authors： Adeleke OA,Choonara YE,Du Toit LC,Pillay V

更新日期：2014-04-01 00:00:00

abstract：:A high-performance liquid chromatographic (HPLC) method for the simultaneous determination of pralidoxime chloride (I) and its major decomposition products in an injectable formulation is described. I and its decomposition products were detected and quantitated by their UV absorbances at 270 nm, after being separated ...

journal_title：Journal of pharmaceutical sciences

authors： Prue DG,Johnson RN,Kho BT

更新日期：1983-07-01 00:00:00

abstract：:An HPLC method for the simultaneous determination of safrole (S), dihydrosafrole (DHS), and chloromethyldihydrosafrole (CM-DHS) in piperonyl butoxide, with fluorimetric detection and elution gradient, is described. Samples with internal standard (piperonyl isobutyrate) are adsorbed on silica cartridges, then eluted wi...

journal_title：Journal of pharmaceutical sciences

authors： Schreiber-Deturmeny EM,Pauli AM,Pastor JL

更新日期：1993-08-01 00:00:00

abstract：:A series of 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-2-acetic acids (3a-e) and 3-substituted indeno[1,2-c]pyrazol-4(1H)-one-1-acetic acids (4a-e) were synthesized as semirigid analogues of tolmetin (1). These compounds were evaluated for their anti-inflammatory action by investigating their ability to block arachi...

journal_title：Journal of pharmaceutical sciences

authors： Lemke TL,Abebe E,Moore PF,Carty TJ

更新日期：1989-04-01 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

authors： Chan J,Lee KH

更新日期：1975-07-01 00:00:00

abstract：:Crystallization of drugs in metastable, supersaturated adhesive polymeric matrices in transdermal drug delivery devices can be avoided by determination of the solubility of the drug in the adhesive polymer. A novel method is described to determine the solubility of the drug in polymeric matrices. Unlike existing metho...

journal_title：Journal of pharmaceutical sciences

authors： Jasti BR,Berner B,Zhou SL,Li X

更新日期：2004-08-01 00:00:00

abstract：:An equation was developed which enables blood level data to be utilized for determining whether or not the first-order absorption and elimination rate constants are equal in the one-compartment open model. This equation was tested using simulated data with excellent results. ...

journal_title：Journal of pharmaceutical sciences

authors： Macheras PE

更新日期：1985-05-01 00:00:00

abstract：:Stable protein nanostructured particles, produced by spray freezing into liquid (SFL) nitrogen, were encapsulated uniformly into microspheres to reduce the burst release over the first 24 h. The denaturation and aggregation of these bovine serum albumin (BSA) high-surface area particles were minimal due to ultra-rapid...

journal_title：Journal of pharmaceutical sciences

authors： Leach WT,Simpson DT,Val TN,Anuta EC,Yu Z,Williams RO 3rd,Johnston KP

更新日期：2005-01-01 00:00:00

abstract：:Alginate-based polyelectrolyte complexes (PECs) and hydrogel were engineered as platforms for local bevacizumab (BVZ) therapy. This study provides deep comprehension on the microstructures of such systems, and their correlation with drug-release patterns. PECs and hydrogel were characterized using Fourier transform in...

journal_title：Journal of pharmaceutical sciences

authors： Ferreira NN,Caetano BL,Boni FI,Sousa F,Magnani M,Sarmento B,Ferreira Cury BS,Daflon Gremião MP

更新日期：2019-04-01 00:00:00

abstract：:Gold nanoparticles through nucleation of Au clusters have been extensively studied. However, due to low potency, prolonged tissue retention, and irreversible accumulation, the safety considerations have limited their therapeutic and diagnostic applications. Novel gold nanostructures with retained physical properties a...

journal_title：Journal of pharmaceutical sciences

authors： Gao Y,Mu Q,Zhu L,Li Z,Ho RJY

更新日期：2020-05-01 00:00:00

abstract：:A commercial dispersive Raman spectrometer operating at 785 nm with a CCD detector was used to acquire spectra of USP reference materials inside amber USP vials. The laser and collection beams were directed through the bottom of the vials, resulting in a 60% loss of signal. The Raman shift was calibrated with a 4-acet...

journal_title：Journal of pharmaceutical sciences

authors： McCreery RL,Horn AJ,Spencer J,Jefferson E

更新日期：1998-01-01 00:00:00

abstract：:The plasma protein binding of drugs has been shown to have significant effects on the quantitative relationship between clinical pharmacokinetics and pharmacodynamics. In many clinical situations, measurement of the total drug concentration does not provide the needed information concerning the unbound fraction of dru...

journal_title：Journal of pharmaceutical sciences

authors： Musteata FM,Pawliszyn J,Qian MG,Wu JT,Miwa GT

更新日期：2006-08-01 00:00:00

abstract：:A method that accurately indicates the end-point of precipitation reactions by the measurement of the relative intensity of the scattered light in the titrate is presented. A new nephelometric titrator with an internal nephelometric sensor has been devised. The work of the titrator including the sensor and change in t...

journal_title：Journal of pharmaceutical sciences

authors： Zhan X,Li C,Li Z,Yang X,Zhong S,Yi T

更新日期：2004-02-01 00:00:00

abstract：:A series of 2-(alpha-hydroxyacetyl)pyridine thiosemicarbazones was synthesized as potential antimalarial and antibacterial agents. Their synthesis was achieved by the condensation of N4-mono- or N4,N4-disubstituted thiosemicarbazides with 2-(alpha-hydroxyacetyl)pyridine. The latter was prepared by selective bromine ox...

journal_title：Journal of pharmaceutical sciences

authors： Klayman DL,Lin AJ,Hoch JM,Scovill JP,Lambros C,Dobek AS

更新日期：1984-12-01 00:00:00

abstract：:Vehicle effects may be caused by thermodynamic effects and by specific (penetration enhancing) effects. To investigate the effects of various lipophilic vehicles on drug penetration, an in vivo permeability study was conducted with methyl nicotinate as the model drug. The drug was dissolved in the respective vehicles ...

journal_title：Journal of pharmaceutical sciences

authors： Leopold CS,Lippold BC

更新日期：1995-02-01 00:00:00

abstract：:Inhibition of endogenous prostacyclin and thromboxane biosynthesis by aspirin is critically dose-dependent in humans. Gastrointestinal and hepatic hydrolysis may limit systemic availability of aspirin, especially in low doses, perhaps contributing to the biochemical selectivity of aspirin. Existing analytical methods ...

journal_title：Journal of pharmaceutical sciences

authors： Pedersen AK,FitzGerald GA

更新日期：1985-02-01 00:00:00

abstract：:Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...

journal_title：Journal of pharmaceutical sciences

authors： McConnell EL,Murdan S,Basit AW

更新日期：2008-09-01 00:00:00