Antibacterial activity of 6,8-disubstituted-quinolone-3-carboxylic acids.

abstract：:The development of sustained-release lithium (Li) tablets, intended to release the active principle at a rate of 1.0 mM/h for 10 h, was undertaken. The parameters used for the control of the release were the glyceril palmite-stearate content, the carboxypolymethylene content, and the compression force. The experimenta...

journal_title：Journal of pharmaceutical sciences

authors： Llabrés M,Fariña JB

更新日期：1991-11-01 00:00:00

abstract：:Three families of alloxan derivatives, 5-arylthiobarbituric, 5-aryliminobarbituric, and 5-aryldialuric acids, were prepared as prospective radioiodine-transporting radiopharmaceuticals for the delineation of pancreatic insulinomas. Members of each class were screened for effects on blood sugar levels in a rat glucose ...

journal_title：Journal of pharmaceutical sciences

authors： Adams WE,Heindel ND,Tutwiler G,Fawthrop H

更新日期：1984-03-01 00:00:00

abstract：:The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 14 2-(3-alkylaminoalkylamido)-pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, with seven showing comparable or greater activity than lidocaine. Most compounds also exhibite...

journal_title：Journal of pharmaceutical sciences

authors： Sowell JW Sr,Block AJ,Derrick ME,Freeman JJ,Kosh JW,Mubarak PF,Tenthorey PA

更新日期：1981-05-01 00:00:00

abstract：:Resveratrol trimethyl ether (trans-3,5,4'-trimethoxystilbene, RTE) is a naturally occurring and pharmacologically active resveratrol derivative. To evaluate its suitability as a drug candidate, a pharmacokinetic study was carried out in Sprague-Dawley rats with the emphasis to identify the impact of aqueous solubility...

journal_title：Journal of pharmaceutical sciences

authors： Lin HS,Ho PC

更新日期：2011-10-01 00:00:00

abstract：:We report a semiquantitative method for determining trace amounts (<1%) of thermodynamically stable forms in polymorphic mixtures, focusing on sample preparation effects on solid phase transitions. Tegafur [5-fluoro-1-(oxolan-2-yl)-1,2,3,4-tetrahydropyrimidine-2,4-dione] was used as a model material in this study. The...

journal_title：Journal of pharmaceutical sciences

authors： Bobrovs R,Actiņš A

更新日期：2012-12-01 00:00:00

abstract：:Three novel series of 4-oxoquinazoline derivatives were prepared and evaluated as potential antimicrobial agents. Evaluation of the antimicrobial activity of a variety of 4-substituted-1-thiosemicarbazides, 3,4-disubstituted thiazolines, and 3-substituted-5-thiazolidones reveals that the majority possess significant i...

journal_title：Journal of pharmaceutical sciences

authors： Habib NS,Khalil MA

更新日期：1984-07-01 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：:This article presents a theoretical model of transdermal drug delivery from an emulsion-type vehicle that addresses the vehicle heterogeneity and incorporates the prediction of drug transport parameters as function of the vehicle composition. The basic mass transfer model considers interfacial and diffusion resistance...

journal_title：Journal of pharmaceutical sciences

authors： Bernardo FP,Saraiva PM

更新日期：2008-09-01 00:00:00

abstract：:This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...

journal_title：Journal of pharmaceutical sciences

authors： Wang G,Wang JJ,Li F,To SS

更新日期：2016-04-01 00:00:00

abstract：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...

journal_title：Journal of pharmaceutical sciences

authors： Maniar ML,Kalonia DS,Simonelli AP

更新日期：1991-08-01 00:00:00

abstract：:Nadolol was extracted from tablet excipients with an acidic potassium chloride solution. The drug was oxidized with periodic acid, and the resulting aldehyde was reacted with 2,4-dinitrophenylhydrazine to form the corresponding hydrazone. Excess reagent was removed with a cupric chloride solution. The hydrazone was ex...

journal_title：Journal of pharmaceutical sciences

authors： Ivashikiv E

更新日期：1978-07-01 00:00:00

abstract：:A sensitive, simple, and rapid method for the quantitation of ibuprofen in plasma, using 1-(p-fluorobenzoyl)-5-methoxy-2-methylindole acetic acid as the internal standard, was developed. The method is based on reversed-phase high-pressure liquid chromatography with a mobile phase containing acetonitrile--0.1 M acetic ...

journal_title：Journal of pharmaceutical sciences

authors： Ali A,Kazmi S,Plakogiannis FM

更新日期：1981-08-01 00:00:00

abstract：:The complete pH-rate profile of the hydrolysis reaction of aspirin, requiring many experiments in the past, was obtained by a single variable-parameter kinetic experiment carried out by varying the hydrogen ion concentration. The experiment was carried out spectrophotometrically, reading automatically absorbance, pH, ...

journal_title：Journal of pharmaceutical sciences

authors： Alibrandi G,Coppolino S,Micali N,Villari A

更新日期：2001-03-01 00:00:00

abstract：:In our previous research, cocaine applied intranasally in rats diffused or was transported directly from the nasal cavity to the brain. However, the direct nose-brain cocaine transport only contributes to an initial increase in the relative cocaine brain exposure. In this study, we have determined the nose-brain trans...

journal_title：Journal of pharmaceutical sciences

authors： Chow HH,Anavy N,Villalobos A

更新日期：2001-11-01 00:00:00

abstract：:Samples of ethacrynic acid were treated with methanol-hydrochloric acid or with diazomethane. GLC and mass spectrometric analysis indicated that the methanol-hydrochloric acid reaction gave the expected methyl ester, whereas diazomethane treatment gave a compound containing an additional 14 mass units. Accurate mass m...

journal_title：Journal of pharmaceutical sciences

authors： Midha KK,Hubbard JW,Charette C,Jun HW

更新日期：1978-07-01 00:00:00

abstract：:The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...

journal_title：Journal of pharmaceutical sciences

authors： Sugano K,Terada K

更新日期：2015-09-01 00:00:00

abstract：:A general spectroscopic method is described that might be applied to validating amino acid sequences in peptides and protein fragments with a view to it becoming a routine procedure with which to characterize biotechnology drug products. The tripeptides are the L-enantiomers of GGA, GGH, GGI, GGL, GGF, GHG, LGG, and Y...

journal_title：Journal of pharmaceutical sciences

authors： Purdie N,Province DW,Johnson EA

更新日期：1999-07-01 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

authors： Ihara M,Tsuchiya Y,Sawasaki Y,Hisaka A,Takehana H,Tomimoto K,Yano M

更新日期：1989-07-01 00:00:00

abstract：:Nosocomial diarrhea and pseudomembranous colitis causing toxins A and B from Clostridium difficile were studied at pH 5-8 and over the temperature range of 10-85 degrees C. The proteins were crosslinked with formaldehyde to inactivate them to toxoid forms and permit their use as vaccines. Structural changes and aggreg...

journal_title：Journal of pharmaceutical sciences

authors： Salnikova MS,Joshi SB,Rytting JH,Warny M,Middaugh CR

更新日期：2008-09-01 00:00:00

abstract：:An emerging technology subtype that has been adopted by formulators to address low-solubility issues is the supersaturating drug delivery system; this system is based on the "spring" and "parachute" design elements, which have been applied to lipid-based formulations, S(M)EDDS, solid dispersions, nano-based systems, a...

journal_title：Journal of pharmaceutical sciences

authors： Augustijns P,Brewster ME

更新日期：2012-01-01 00:00:00

abstract：:The stability of therapeutic proteins formulated in prefilled syringes (PFS) may be negatively impacted by the exposure of protein molecules to silicone oil-water interfaces and air-water interfaces. In addition, agitation, such as that experienced during transportation, may increase the detrimental effects (i.e., pro...

journal_title：Journal of pharmaceutical sciences

authors： Gerhardt A,Mcgraw NR,Schwartz DK,Bee JS,Carpenter JF,Randolph TW

更新日期：2014-06-01 00:00:00

abstract：:Complex dosing regimens simulated in the literature using a universal dosing regimen were calculated with a general dosing program developed using the program CONSAM. The program provides a rapid method of calculating nonuniform dosing regimens for up to n = 3 compartments for any linear model. Subject data can also b...

journal_title：Journal of pharmaceutical sciences

authors： Jackson AJ,Zech LA

更新日期：1991-04-01 00:00:00

abstract：:Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...

journal_title：Journal of pharmaceutical sciences

authors： Almarsson O,Kaufman MJ,Stong JD,Wu Y,Mayr SM,Petrich MA,Williams JM

更新日期：1998-05-01 00:00:00

abstract：:The dielectric constant of a solid substance in the dissolved state may be found by using a solvent with a dielectric constant that remains invariable when the solid substance is dissolved. The slope values obtained from dielectric constant versus concentration plots of the solid substance in two solvents with differe...

journal_title：Journal of pharmaceutical sciences

authors： Cavé G,Puisieux F,Carstensen JT

更新日期：1979-04-01 00:00:00

abstract：:Dolasetron mesilate (Anzemet) ((2 alpha, 6 alpha, 8 alpha, 9a beta)-octahydro-3-oxo-2,6-methano-2H-quinolizin-8-yl-1 H-indole-3-carboxylate monomethane-sulfonate) is a 5-HT3 receptor antagonist, which is in development for the treatment of chemotherapy-induced emesis. The ketone moiety of dolasetron is rapidly reduced...

journal_title：Journal of pharmaceutical sciences

authors： Dow J,Francesco GF,Berg C

更新日期：1996-07-01 00:00:00

abstract：:A Modified Crisp Equation, describing the differential Gibbs free energy of the adsorption process, is being proposed, which considers multiple sites available on the surface for adsorption and their relative fractions. The differential Gibbs free energy can be calculated by the van't Hoff Equation, which depends on t...

journal_title：Journal of pharmaceutical sciences

authors： Yu P,Wurster DE

更新日期：2018-04-01 00:00:00

abstract：:Aerosolized medicine is one of the fastest growing areas in the pharmaceutical industry. Dry powder aerosols of pharmaceutical compounds are particularly attractive for the prevention and treatment of respiratory diseases but are also emerging as a treatment option for systemic diseases. Engineering particles in dry p...

journal_title：Journal of pharmaceutical sciences

authors： El-Gendy N,Selvam P,Soni P,Berkland C

更新日期：2012-09-01 00:00:00

abstract：:AZD1175 and AZD2207 are 2 highly lipophilic compounds with a significant risk of not achieving therapeutic plasma concentrations due to solubility-limited absorption. The compounds have the same molecular weight and minimal structural differences. The aim of the present work was to investigate whether salts could be a...

journal_title：Journal of pharmaceutical sciences

authors： Tannergren C,Karlsson E,Sigfridsson K,Lindfors L,Ku A,Polentarutti B,Carlert S

更新日期：2016-11-01 00:00:00

abstract：:The analysis of corticosteroid prodrugs in pharmacokinetic (PK) studies poses the risk of overestimation of corticosteroid concentrations due to in vitro hydrolysis of prodrugs after sample collection. This study tests the effectiveness of enzyme inhibitors as stabilizers for betamethasone sodium phosphate (BSP) in pr...

journal_title：Journal of pharmaceutical sciences

authors： Samtani MN,Schwab M,Nathanielsz PW,Jusko WJ

更新日期：2004-03-01 00:00:00

abstract：:Development of high-throughput release and characterization assays is critical for the effective support of the rapidly growing biologics pipeline for biotherapeutics. Clipping of polypeptide chains is commonly monitored during process optimization, formulation development, and stability studies. A reduced capillary e...

journal_title：Journal of pharmaceutical sciences

authors： Stackhouse N,Miller AK,Gadgil HS

更新日期：2011-12-01 00:00:00