Molecular complexing ability of quinoline and its simple derivatives.

abstract：:The S6-(N-alkyl-N-alkoxycarbonyl)aminomethyl-6-MP (6-CARB-6-MP) prodrugs 5-20 were synthesized from the reaction of 6-MP with N-alkyl-N-alkyoxycarbonylaminomethyl chlorides (4) in dimethyl sulfoxide in overall yields of 5-62%, depending on the N-alkyl and the alkoxy groups involved. The derivatives were fully characte...

journal_title：Journal of pharmaceutical sciences

authors： Siver KG,Sloan KB

更新日期：1990-01-01 00:00:00

abstract：:Continuing work on the interaction of inorganic additives with nonionic surfactants in aqueous solution dealt with their effect on the CMC and surface tension. The surfactants were octoxynol and polyoxyethylated oleyl alcohol, containing an average of 9.5 and 10 ethylene oxide units, respectively. Their CMC values wer...

journal_title：Journal of pharmaceutical sciences

authors： Schott H,Han SK

更新日期：1976-07-01 00:00:00

abstract：:Many active pharmaceutical ingredients exhibit a needle-like (acicular) crystal habit, which can significantly complicate their downstream processing. In this study, the acicular crystal habit of a model active pharmaceutical ingredient, 5-aminosalicylic acid (5-ASA), was modified by addition of selected organic solve...

journal_title：Journal of pharmaceutical sciences

authors： Pudasaini N,Parker CR,Hagen SU,Bond AD,Rantanen J

更新日期：2018-04-01 00:00:00

abstract：:A tetrazole ring is often used in drug discovery as a replacement for the carboxylic acid group. Previous work indicates that compounds containing a tetrazole moiety show asymmetric permeability in Caco-2 cells characteristic of an efflux transporter substrate. The aim of this study is to determine which transporters ...

journal_title：Journal of pharmaceutical sciences

authors： Young AM,Audus KL,Proudfoot J,Yazdanian M

更新日期：2006-04-01 00:00:00

abstract：:A general method for predicting the intestinal absorption of a wide range of drugs using multiple regression analysis of their physicochemical properties and the drug-membrane electrostatic interaction was developed. The absorption rates of tested drugs from rat jejunum were measured by the in situ single-pass perfusi...

journal_title：Journal of pharmaceutical sciences

authors： Sugawara M,Takekuma Y,Yamada H,Kobayashi M,Iseki K,Miyazaki K

更新日期：1998-08-01 00:00:00

abstract：:Chlorthalidone was analyzed in the concentration range of 0.1-3.0 microgram/ml with a precision of +/- 0.05 microgram/ml. Chlorthalidone inhibition of the enzymatic hydrolysis rate of p-nitrophenyl acetate by bovine erythrocyte carbonic anhydrase was used as a basis for the determination. The amount of p-nitrophenol f...

journal_title：Journal of pharmaceutical sciences

authors： Johnston MM,Li H,Mufson D

更新日期：1977-12-01 00:00:00

abstract：:This edition of the Journal of Pharmaceutical Sciences is dedicated to the wonderful career of Per Artursson from the Uppsala University. My Commentary focusses on Per's major contributions to the Caco-2 cell literature over the past 30 years. Two especially influential papers have been cited more than 1000 times out ...

journal_title：Journal of pharmaceutical sciences

authors： Brayden DJ

更新日期：2021-01-01 00:00:00

abstract：:Hard gelatin capsule (HGC) shells are widely used to encapsulate drugs for oral delivery but are vulnerable to gelatin cross-linking, which can lead to slower and more variable in vitro dissolution rates. Adding proteolytic enzymes to the dissolution medium can attenuate these problems, but this complicates dissolutio...

journal_title：Journal of pharmaceutical sciences

authors： Likar MD,Carroll SC,Colgan ST,Yeoh T,MacDonald BC,Johnson GM,Space JS

更新日期：2018-12-01 00:00:00

abstract：:Modifications of antibacterial activity have been demonstrated using combinations of two antibacterials from trimethoprim, sulfonamides (sulfadiazine, sulfamerazine, and silver sulfadiazine), silver nitrate, and dibromopropamidine isethionate, either formulated in a cream base or dissolved in peptone water. The creams...

journal_title：Journal of pharmaceutical sciences

authors： Richards RM,Taylor RB,Xing DK

更新日期：1991-09-01 00:00:00

abstract：:A thermodynamic analysis of the energy transformations occurring within pharmaceutical tablets during the unloading phase of compaction was performed on Avicel, calcium phosphate, acetaminophen, and calcium oxalate. This analysis was based on viscoelastic stress data collected using an instrumented rotary press and wa...

journal_title：Journal of pharmaceutical sciences

authors： Hoag SW,Rippie EG

更新日期：1994-06-01 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

abstract：:The role of particle size and surface modification on biodistribution of nanocarriers is widely reported. We report for the first time the role of nanoparticle shape on biodistribution. Our study demonstrates that irregular shaped polymer lipid nanoparticles (LIPOMER) evade kupffer cells and localize in the spleen. We...

journal_title：Journal of pharmaceutical sciences

authors： Devarajan PV,Jindal AB,Patil RR,Mulla F,Gaikwad RV,Samad A

更新日期：2010-06-01 00:00:00

abstract：:This work compares the conformational stability, backbone flexibility, and aggregation propensity of monomer and dimer fractions of an IgG1 monoclonal antibody (mAb) generated on UVA light exposure for up to 72 h collected by preparative size-exclusion chromatography, compared with unstressed control. UVA light exposu...

journal_title：Journal of pharmaceutical sciences

authors： Bommana R,Chai Q,Schöneich C,Weiss WF 4th,Majumdar R

更新日期：2018-06-01 00:00:00

abstract：:5-Methyl-2-[(4-methyl-2-nitrophenyl)amino]-3-thiophenecarbonitrile is an example of conformational and color polymorphism. The compound crystallizes in red (R), dark red (DR), light red (LR), and orange (O) modifications. There are two specific goals for this study. One is to characterize the complex thermodynamic rel...

journal_title：Journal of pharmaceutical sciences

authors： He X,Griesser UJ,Stowell JG,Borchardt TB,Byrn SR

更新日期：2001-03-01 00:00:00

abstract：:Amorphous nifedipine (NFD), which has a smooth surface immediately after preparation, was shown to have structures resembling clusters of curling and branching fibers approximately 1 μm wide by atomic force microscopy (AFM) after storage at 25°C. The size of the cluster-like structures increased with storage over time...

journal_title：Journal of pharmaceutical sciences

authors： Miyazaki T,Aso Y,Kawanishi T

更新日期：2011-10-01 00:00:00

abstract：:A procedure is described for TLC detection and differentiation of the butyrophenone-diphenylbutylpiperidine group and phenothiazine derivatives at the microgram level. A two-dimensional TLC method to separate butyrophenone and diphenylbutylpiperidine compounds is reported. A variety of possible detection reagents were...

journal_title：Journal of pharmaceutical sciences

authors： Pluym A

更新日期：1979-08-01 00:00:00

abstract：:A new parameter, the kinetic ratio, is suggested for estimating product potency during storage under ambient warehouse temperatures. Actual warehouse temperature data were integrated using Arrhenius kinetics, and the resulting potency errors, due both to the integration method and to temperature averaging, were evalua...

journal_title：Journal of pharmaceutical sciences

authors： Scher M

更新日期：1980-03-01 00:00:00

abstract：:Most of the global healthcare issues facing us--from expanding access to care, to providing medical and dental care in the aftermath of disasters--are far too complex for any single sector to successfully solve. Industry, the healthcare profession, government, academia and non-governmental organizations (NGOs) are all...

journal_title：Journal of pharmaceutical sciences

authors： Bergman SM

更新日期：2008-12-01 00:00:00

abstract：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing metronidazole are reviewed. Metronidazole can be assigned to Biopharmaceutics Classification System Class I. Most BE studies that were identifi...

journal_title：Journal of pharmaceutical sciences

authors： Rediguieri CF,Porta V,G Nunes DS,Nunes TM,Junginger HE,Kopp S,Midha KK,Shah VP,Stavchansky S,Dressman JB,Barends DM

更新日期：2011-05-01 00:00:00

abstract：:Metronidazole and four derivatives were studied in vitro to investigate the differences in the extent of their binding to plasma proteins. Modification at the terminal portion of the alkyl side chain resulted in wide differences in the extent of binding. Molecular orbital calculations were performed by the CNDO and MI...

journal_title：Journal of pharmaceutical sciences

authors： Sanvordeker DR,Chien YW,Lin TK,Lambert HJ

更新日期：1975-11-01 00:00:00

abstract：:For development and optimization of protein formulation sensitive analytical tools are required to follow both aggregation and changes in protein structure. The latter can be seen as the beginning of physical instability leading to aggregation. The focus of this work laid on the development of a novel analysis simulta...

journal_title：Journal of pharmaceutical sciences

authors： Printz M,Friess W

更新日期：2012-02-01 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：:We investigated the effect of cytochrome P450 (CYP) 2C9 polymorphism on the inhibition of methylhydroxylation activity of tolbutamide, a typical CYP2C9 substrate, by triazole antifungal agents, fluconazole and voriconazole. Although the Michaelis constants (Km), maximal velocities (Vmax), and Vmax/Km values for CYP2C9...

journal_title：Journal of pharmaceutical sciences

authors： Niwa T,Hata T

更新日期：2016-03-01 00:00:00

abstract：:The transport rate constant of a drug partitioned in a two-phase system from an aqueous to an organic phase (k1obs) and vice versa (k2obs) is a function of the partition coefficient P and of a solvent system-dependent parameter beta. Drug transport is shown to be independent of molecular structure for a number of arbi...

journal_title：Journal of pharmaceutical sciences

authors： van de Waterbeemd H,van Bakel P,Jansen A

更新日期：1981-09-01 00:00:00

abstract：:This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electr...

journal_title：Journal of pharmaceutical sciences

authors： Jong T,Li J,Morton DA,Zhou QT,Larson I

更新日期：2016-03-01 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：: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：:Volunteers were injected im with 100 mg of tripelennamine (pyribenzamine).HCl dissolved in saline. Timed urine was collected. Tripelennamine and its metabolites were identified by GC/MS. Amounts of free tripelennamine excreted in the 0-2-, 2-4-, 4-8-, 8-12-, and 12-24-h urine samples were found to be 0.30, 0.56, 0.17,...

journal_title：Journal of pharmaceutical sciences

authors： Yeh SY

更新日期：1991-09-01 00:00:00

abstract：:Chitosan microspheres were evaluated for sustained-release of recombinant human interleukin-2 (rIL-2) in this study. In addition, the effects of different formulation factors, such as chitosan and protein concentrations, the volume of sodium sulfate solution, addition technique of rIL-2, and presence of glutaraldehyde...

journal_title：Journal of pharmaceutical sciences

authors： Ozbaş-Turan S,Akbuğa J,Aral C

更新日期：2002-05-01 00:00:00

abstract：:New butyrate derivatives were synthesized to investigate the residence time of potent butyric acid in vivo. These derivatives were triglycerides in which one, two, or three butyric acid molecules were bound to glycerol or to mono- and dipalmitic esters of glycerol. Pharmacokinetic studies showed that a constant plasma...

journal_title：Journal of pharmaceutical sciences

authors： Planchon P,Pouillart P,Ronco G,Villa P,Pieri F

更新日期：1993-10-01 00:00:00