A mechanistic and kinetic study of the beta-lactone hydrolysis of Salinosporamide A (NPI-0052), a novel proteasome inhibitor.

abstract：:The affinity chromatographic technique was used to study the interaction of bovine serum albumin and salicylic acid at 3.3 +/- 1.1 degrees. Beaded agarose gel, on which the albumin was immobilized by covalent linkage, was packed in a column as an affinity adsorbent. Frontal analysis was performed on this column to eva...

journal_title：Journal of pharmaceutical sciences

authors： Nakano NI,Oshio T,Fujimoto Y,Amiya T

更新日期：1978-07-01 00:00:00

abstract：:Hydrolytic degradation products of cefdinir were studied in acidic (pH 1), neutral (pH 6), and basic (pH 9) solutions. Seven major degradation products were isolated by preparative and/or high-performance liquid chromatography and characterized by UV, IR, 1H-NMR, and mass spectra. To clarify degradation pathways in ea...

journal_title：Journal of pharmaceutical sciences

authors： Okamoto Y,Kiriyama K,Namiki Y,Matsushita J,Fujioka M,Yasuda T

更新日期：1996-09-01 00:00:00

abstract：:From a consideration of the basic processes involved in drug elimination, the fraction of drug cleared by the gut and by the liver were described as functions of availability and hepatic clearance. For a drug given orally, a plot of the fraction of drug cleared by the gut or liver against alpha, a proportionality cons...

journal_title：Journal of pharmaceutical sciences

authors： Minchin RF,Ilett KF

更新日期：1982-04-01 00:00:00

abstract：:Understanding the effect of surfactant properties is critical when designing vesicular delivery systems. This review evaluates previous studies to explain the influence of surfactant properties on the behavior of lipid vesicular systems, specifically their size, charge, stability, entrapment efficiency, pharmacokineti...

journal_title：Journal of pharmaceutical sciences

authors： Bnyan R,Khan I,Ehtezazi T,Saleem I,Gordon S,O'Neill F,Roberts M

更新日期：2018-05-01 00:00:00

abstract：:Foam granulation is a relatively newer wet granulation process whereby foamed binder solutions are added to powders in a mixer. It is essential to understand the effect of powder substrate on foam drainage and half-life, which are relevant to nucleation and agglomeration during foam granulation. Hydroxypropyl methylce...

journal_title：Journal of pharmaceutical sciences

authors： Koo OM,Ji J,Li J

更新日期：2012-04-01 00:00:00

abstract：:Oil-frozen water-in-oil-in-water (W₁/O/W₂) double emulsions (DE) containing ethanol up to 40% (w/v) in the external aqueous W₂ phase exhibited external coalescence upon thawing of the oil phase, releasing up to 85% of the encapsulated protein of the internal aqueous phase. These emulsions were studied in vitro as pote...

journal_title：Journal of pharmaceutical sciences

authors： Jaimes-Lizcano YA,Lawson LB,Papadopoulos KD

更新日期：2011-04-01 00:00:00

abstract：:Co-amorphous drug-amino acid systems have gained growing interest as an alternative to common amorphous formulations which contain polymers as stabilizers. Several preparation methods have recently been investigated, including vibrational ball milling on a laboratory scale or spray drying in a larger scale. In this st...

journal_title：Journal of pharmaceutical sciences

authors： Lenz E,Löbmann K,Rades T,Knop K,Kleinebudde P

更新日期：2017-01-01 00:00:00

abstract：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

journal_title：Journal of pharmaceutical sciences

authors： Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

更新日期：2014-05-01 00:00:00

abstract：:A method for preparing polyanhydride granules of an injectable size was developed. The resulting granules permitted a nearly constant release of low-molecular-weight, water-soluble drugs without an initial burst. The polyanhydrides used were poly(fatty acid dimer), poly(sebacic acid), and their copolymers. The dyes ac...

journal_title：Journal of pharmaceutical sciences

authors： Tabata Y,Domb A,Langer R

更新日期：1994-01-01 00:00:00

abstract：:It is demonstrated that the fluid-phase thermodynamics theory conductor-like screening model for real solvents (COSMO-RS) as implemented in the COSMOtherm software can be used for accurate and efficient screening of coformers for active pharmaceutical ingredient (API) cocrystallization. The excess enthalpy, H(ex) , be...

journal_title：Journal of pharmaceutical sciences

authors： Abramov YA,Loschen C,Klamt A

更新日期：2012-10-01 00:00:00

abstract：:The aim of this study was to evaluate a new experimental protocol utilizing isolated frog intestinal sacs for the assessment of intestinal drug permeability in humans. Segments of approximately 5.0 cm in length were used for these experiments. The intestinal sacs were filled with a solution of the appropriate drug in ...

journal_title：Journal of pharmaceutical sciences

authors： Trapani G,Franco M,Trapani A,Lopedota A,Latrofa A,Gallucci E,Micelli S,Liso G

更新日期：2004-12-01 00:00:00

abstract：:To reduce the inherent variability in serum uric acid levels of animals allowed ad libitum exposure to food containing potassium oxonate and uric acid, male Sprague-Dawley rats were trained to eat their daily food allotment in a 1.25-hr period each morning. After training the rats were fed a food mixture containing 5%...

journal_title：Journal of pharmaceutical sciences

authors： Newburger J,Hsu TF,Combs AB

更新日期：1979-05-01 00:00:00

abstract：:A new method for determining a quaternary mixture of vitamins B6, B1, and B12 and uridine 5'-triphosphate (UPT) using second-derivative spectrophotometry is described. Calibration graphs were linear up to 30 micrograms/mL of vitamin B6 at 307 nm (r = 0.9999) and vitamin B1 at 282.7 nm (r = 0.9997) and up to 35 microgr...

journal_title：Journal of pharmaceutical sciences

authors： Morelli B

更新日期：1995-01-01 00:00:00

abstract：:Corneal penetration studies were conducted in unanesthetized albino rabbits using various organic compounds representing both polar and nonpolar species. Very low molecular weight compounds demonstrate rapid uptake into the aqueous humor despite the lipid-like barrier imposed by the corneal epithelium. Evidence that t...

journal_title：Journal of pharmaceutical sciences

authors： Grass GM,Robinson JR

更新日期：1988-01-01 00:00:00

abstract：:The acidic, neutral, and alkaline degradations of six therapeutically useful cephalosporins (cephalothin, cephaloridine, cephaloglycin, cephalexin, cephradine, and cefazolin), 7-amino-cephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and some 7-substituted derivatives were followed by high-pressure liquid ch...

journal_title：Journal of pharmaceutical sciences

authors： Yamana T,Tsuji A

更新日期：1976-11-01 00:00:00

abstract：:Release of drug from a single-layer film containing dispersed drug follows a diffusion-controlled matrix model, where the quantity released per unit area is proportional to the square root of time. The kinetics may be made linear with time (zero order) by laminating a second film without drug to the releasing side of ...

journal_title：Journal of pharmaceutical sciences

authors： Borodkin S,Tucker FE

更新日期：1975-08-01 00:00:00

abstract：:The United States Food and Drug Administration recommends pilot dose duration-response and pivotal bioequivalence studies to be conducted using reflectance colorimetry for assessment of the in vivo bioequivalence of topical dermatologic corticosteroids. The major objectives of the present studies were to examine the a...

journal_title：Journal of pharmaceutical sciences

authors： Tsai JC,Cheng CL,Tsai YF,Sheu HM,Chou CH

更新日期：2004-01-01 00:00:00

abstract：:The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of the tongue, to investigate the mechanisms of glucose uptake. The uptake of D-glucose was much larger in cells of the dorsum of the tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-...

journal_title：Journal of pharmaceutical sciences

authors： Oyama Y,Yamano H,Ohkuma A,Ogawara K,Higaki K,Kimura T

更新日期：1999-08-01 00:00:00

abstract：:In this study, we attempted to improve the oral absorption of ceftriaxone (CTX) by using an absorption carrier and the CTX complex together. After the CTX-Ca-carrageenan gel complex was prepared, several kinds of compounds (Capmul MCM C10, Gelucire 44/14, glycyrrhizin) were screened as potential oral enhancers for our...

journal_title：Journal of pharmaceutical sciences

authors： Cho SW,Lee JS,Choi SH

更新日期：2004-03-01 00:00:00

abstract：:Levemopamil was solubilized by varying the concentration of hydroxypropyl-beta-cyclodextrin (HPbetaCD) and by the alteration of pH. The drug molecule has two sites for possible complexation with HPbetaCD, creating the possibility of either 1:1 or 1:2 complexation. The solubility as a function of HPbetaCD concentration...

journal_title：Journal of pharmaceutical sciences

authors： McCandless R,Yalkowsky SH

更新日期：1998-12-01 00:00:00

abstract：:The influence of ferric ions, EDTA, and visible light on the oxidation of methionine and the covalent reducible and nonreducible dimerization in human Insulin-like Growth Factor I (hIGF-I) in aqueous (1 mM) phosphate buffer solution were studied. A reduced factorial experiment with two levels of each factor was used. ...

journal_title：Journal of pharmaceutical sciences

authors： Fransson JR

更新日期：1997-09-01 00:00:00

abstract：:Drug transporters expressed in liver and kidney play a critical role in the elimination of a wide range of drugs and xenobiotics and inhibition of these transporters may therefore cause clinically significant drug-drug interactions (DDIs). Currently, in vitro transporter inhibition data are used to assess the risk tha...

journal_title：Journal of pharmaceutical sciences

authors： Chu X,Chan GH,Evers R

更新日期：2017-09-01 00:00:00

abstract：:Lysosomes are acidic intracellular organelles that can extensively sequester basic lipophilic drugs due to pH and membrane partitioning, and therefore may significantly influence subcellular drug concentrations. Current in vitro methods for lysosomal drug sequestration evaluation typically lack the ability to accurate...

journal_title：Journal of pharmaceutical sciences

authors： Francis L,Harrell A,Hallifax D,Galetin A

更新日期：2020-09-01 00:00:00

abstract：:Although several mathematical models have been reported for the estimation of human plasma concentration profiles of drug substances after dermal application, the successful cases that can predict human pharmacokinetic profiles are limited. Therefore, the aim of this study is to investigate the prediction of human pla...

journal_title：Journal of pharmaceutical sciences

authors： Yamamoto S,Karashima M,Arai Y,Tohyama K,Amano N

更新日期：2017-09-01 00:00:00

abstract：:The disposition of 8-methyl-8-azabicyclo[3,2,1]octan-3-yl 3,5-dichlorobenzoate (MDL 72,222; 1), a potent 5-hydroxytryptamine antagonist, and its N-demethylated and N-oxide metabolites was studied in dogs and monkeys. After single, intravenous doses of 1 at 5 mg/kg, the mean terminal half-lives of 1 in plasma were 2.6 ...

journal_title：Journal of pharmaceutical sciences

authors： Cheng H,Larsen DL,Ragner JA,Sproles GD,Gordon WP

更新日期：1992-04-01 00:00:00

abstract：:A sucrose-lactose-starch granulation was used to study particulate motion and attrition in a fluid bed dryer. There is some classification of material in the dryer as drying proceeds; fine particles are dried faster and become less dense, and the less dry but denser large particles show some (although not great) accum...

journal_title：Journal of pharmaceutical sciences

authors： Zoglio MA,Streng WH,Carstensen JT

更新日期：1975-11-01 00:00:00

abstract：:Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanopartic...

journal_title：Journal of pharmaceutical sciences

authors： Tsai MJ,Huang YB,Wu PC,Fu YS,Kao YR,Fang JY,Tsai YH

更新日期：2011-02-01 00:00:00

abstract：:The critical micellar concentration (cmc) values of some mixed systems containing two bile salts were determined by a maximum pressure bubble method and compared with those derived from a theoretical model developed for nonionic surfactants to assess the applicability of this model to such systems. Some assumptions on...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Cerré C,Fini A,Sipahi AM,Baraldini M

更新日期：1995-05-01 00:00:00

abstract：:An important part of pharmacokinetic research is fitting models to observed data and estimating the parameters in the model. In general, parameter estimation in pharmacokinetics is a subset of the general problem of nonlinear regression or parameter estimation in nonlinear regression models. The same criteria, algorit...

journal_title：Journal of pharmaceutical sciences

authors： Metzler CM

更新日期：1987-07-01 00:00:00

abstract：:A simple solution model that has lead to successful predictive equations for the partial molar excess properties of a solute in simple binary solvent mixtures containing only nonspecific interactions is extended to include association between the solute and one of the solvent components. An expression is derived and t...

journal_title：Journal of pharmaceutical sciences

authors： Acree WE Jr,McHan DR,Rytting JH

更新日期：1983-08-01 00:00:00