Formation of a cyclic derivative of ethacrynic acid with diazomethane.

abstract：:Flexible manufacturing technologies for solid oral dosage forms with a continuous adjustability of the manufactured dose strength are of interest for applications in personalized medicine. This study explored the feasibility of using microvalve technology for the manufacturing of different solid oral dosage form conce...

journal_title：Journal of pharmaceutical sciences

authors： Bonhoeffer B,Kwade A,Juhnke M

更新日期：2018-03-01 00:00:00

abstract：:The aim of this study was to characterize the metabolic pathways of 2-methoxyestradiol (2ME2), an investigational anticancer drug. In vitro metabolism studies were performed by incubation of 2ME2 with human liver microsomes under various conditions and metabolite identification was performed using liquid chromatograph...

journal_title：Journal of pharmaceutical sciences

authors： Lakhani NJ,Sparreboom A,Xu X,Veenstra TD,Venitz J,Dahut WL,Figg WD

更新日期：2007-07-01 00:00:00

abstract：:The objective of the present research was to investigate the stability of an amorphous drug, Delta(9)-tetrahydrocannabinol (THC) in polymer-based transmucosal systems. THC was incorporated in polyethylene oxide and hydroxypropylcellulose matrices by a hot-melt fabrication procedure, utilizing various processing aids. ...

journal_title：Journal of pharmaceutical sciences

authors： Munjal M,Stodghill SP,Elsohly MA,Repka MA

更新日期：2006-08-01 00:00:00

abstract：:While the number of clinical trials has continued to grow by about 20% in the past six months, no corresponding growth in product approval by the food and drug administration is seen or anticipated in the near future. Late-stage clinical failures due to lack of efficacy or toxicity continues to be a challenge. The opt...

journal_title：Journal of pharmaceutical sciences

authors： Ho RJ,Chien JY

更新日期：2009-06-01 00:00:00

abstract：:Supercritical fluid emulsion extraction is an innovative technology that uses supercritical carbon dioxide (SC-CO(2)) to extract the dispersed oily phase of an emulsion. This technology was used to produce poly-lactic-co-glycolic acid (PLGA) microspheres charged with two common NSAIDs: piroxicam (PX) and diclophenac s...

journal_title：Journal of pharmaceutical sciences

authors： Della Porta G,Falco N,Reverchon E

更新日期：2010-03-01 00:00:00

abstract：:The pre-equilibrium capillary zone electrophoretic (pre-eq CZE) method to determine association constants of active anionic forms of antithyroid drugs: 6-n-propyl-2-thiouracil (PTU), 6-methyl-2-thiouracil (MTU), 2-thiouracil (TU) with bovine serum albumin (BSA) under physiological pH 7.4 has been developed for the fir...

journal_title：Journal of pharmaceutical sciences

authors： Chernov'yants MS,Dolinkin AO,Chernyshev AV,Khohlov EV,Golovanova EG

更新日期：2010-03-01 00:00:00

abstract：:Even though gelatin is the most widely used polymeric excipient in pharmaceutical products, scant attention has been paid to its interaction with small organic molecules. The present work deals with the interaction of gelatin and four monosulfonated or monocarboxylated azo dyes having hydrocarbon moieties of different...

journal_title：Journal of pharmaceutical sciences

authors： Gautam J,Schott H

更新日期：1994-07-01 00:00:00

abstract：:The present study was carried out to investigate the blood-to-retina transport of nicotine across the inner blood-retinal barrier (BRB). Using the in vivo vascular injection method, the blood-to-retina influx clearance of nicotine across the BRB was determined as 131 μL/(min?g retina), which is much higher than that o...

journal_title：Journal of pharmaceutical sciences

authors： Tega Y,Kubo Y,Yuzurihara C,Akanuma S,Hosoya K

更新日期：2015-09-01 00:00:00

abstract：:The recently developed hydrogen-bonding propensity tool in the Cambridge Structural Database software package (Mercury) was tested to predict polymorphs. The compounds for the study were chosen from a list of approximately 300 pharmaceutically important compounds, for which multiple crystal forms had not been previous...

journal_title：Journal of pharmaceutical sciences

authors： Nauha E,Bernstein J

更新日期：2015-06-01 00:00:00

abstract：:The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...

journal_title：Journal of pharmaceutical sciences

authors： Nordström J,Alderborn G

更新日期：2015-06-01 00:00:00

abstract：:Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...

journal_title：Journal of pharmaceutical sciences

authors： Trapa PE,Belova E,Liras JL,Scott DO,Steyn SJ

更新日期：2016-02-01 00:00:00

abstract：:The pharmacokinetics of fluorouracil were examined after single 250-mg iv doses and 500-mg oral doses to female patients with breast cancer. In five patients who received intravenous fluorouracil, the mean peak plasma level of unchanged drug was 13.4 microgram/ml, the elimination half-life was 6.3 min, and the plasma ...

journal_title：Journal of pharmaceutical sciences

authors： Phillips TA,Howell A,Grieve RJ,Welling PG

更新日期：1980-12-01 00:00:00

abstract：:Local variations in compaction behaviour were investigated, for specimens of different shapes and thickness, comparing predictions from finite element (FE) modelling and results from a recently developed method using small-angle X-ray scattering (SAXS). Good agreement was generally obtained between these methods, in t...

journal_title：Journal of pharmaceutical sciences

authors： Laity PR,Han L,Elliott J,Cameron RE

更新日期：2010-10-01 00:00:00

abstract：:Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Schlich M,Cryan JF,O'Driscoll CM

更新日期：2017-12-01 00:00:00

abstract：:To study if electrostatic charge initially present in mannitol powder plays a role in the generation of aerosols, mannitol was unipolarly charged to varying magnitudes by tumbling the powder inside containers of different materials. The resulting charge in the powder was consistent with predictions from the triboelect...

journal_title：Journal of pharmaceutical sciences

authors： Adi H,Kwok PC,Crapper J,Young PM,Traini D,Chan HK

更新日期：2010-05-01 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：: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 geometry and structural features of the inclusion complexes of beta-cyclodextrin (beta-CD) with the chiral antiamnesic drugs (+/-)-1-benzyl-4-hydroxymethylpyrrolidin-2-one (WEB-1868). (+/-)-1-benzenesulfonyl-5-ethoxypyrrolidin-2-one (RU-35929), and (+/-)-1-(3-pyridinlysulfonyl)-5-ethoxypyrrolidin-2-one (RU-47010) ...

journal_title：Journal of pharmaceutical sciences

authors： Amato ME,Djedaïni F,Pappalardo GC,Perly B,Scarlata G

更新日期：1992-12-01 00:00:00

abstract：:A Bayesian approach was developed to determine an amikacin dosage regimen to achieve the desired plasma concentrations for each patient. Statistical characteristics of pharmacokinetic parameters were first evaluated in a group of patients (reference population), which when combined with three individual plasma concent...

journal_title：Journal of pharmaceutical sciences

authors： Garraffo R,Iliadis A,Cano JP,Dellamonica P,Lapalus P

更新日期：1989-09-01 00:00:00

abstract：:The survival of Staphylococcus aureus was studied in 30 oral administration liquid medicaments (15 syrups and 15 solutions) to determine the effectiveness of the preservatives, the influence of the culture medium used in the enumeration of the surviving microorganisms, and the loss of the enzyme coagulase, phosphatase...

journal_title：Journal of pharmaceutical sciences

authors： Vivar C,de la Rosa C,Mosso A

更新日期：1993-02-01 00:00:00

abstract：:The dependency of metformin in vivo disposition on the rate and extent of dissolution was studied. The analysis includes the use of fundamental principles of drug input, permeability, and intestinal transit time within the framework of a compartmental absorption transit model to predict key pharmacokinetic (PK) parame...

journal_title：Journal of pharmaceutical sciences

authors： Crison JR,Timmins P,Keung A,Upreti VV,Boulton DW,Scheer BJ

更新日期：2012-05-01 00:00:00

abstract：:(-)-1-Cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo [a,d]cyclohepten-5-ylidene)piperidine (MK-160) was extracted from human plasma and urine with petroleum ether and quantitated by GLC using a nitrogen-sensitive detector. A homologue of the drug served as the internal standard. The method is specific for the d...

journal_title：Journal of pharmaceutical sciences

authors： Hucker HB,Hutt JE

更新日期：1983-07-01 00:00:00

abstract：:The aminoxyl (nitroxyl) labeled (2-chloroethyl)nitrosocarbamoyl (CNC) derivatives of amino acids, i.e., N-[[N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl]-A-(1-oxy-2,2,6,6- tetramethylpiperidin-4-yl)amides, A = glycyl (10a), A = L-alanyl (10b), A = L-valyl (10c), A = L-phenylalanyl (10d), were synthesized and evaluated ...

journal_title：Journal of pharmaceutical sciences

authors： Sosnovsky G,Baysal M,Erciyas E

更新日期：1994-07-01 00:00:00

abstract：:A sensitive, specific and reproducible high-performance liquid chromatographic procedure, using the normal phase and radial compression system, is described for the simultaneous determination of corticosterone, hydrocortisone, and dexamethasone in plasma, with prednisolone as the internal standard. Samples were extrac...

journal_title：Journal of pharmaceutical sciences

authors： Alvinerie M,Toutain PL

更新日期：1982-07-01 00:00:00

abstract：:The tissue penetration and distribution of antibiotics is of great importance, since most of the infections occur in the tissue. At the infection site, the free, unbound fraction of the antibiotic is responsible for the antiinfective effect. These free extracellular concentrations can be measured by microdialysis. It ...

journal_title：Journal of pharmaceutical sciences

authors： Nolting A,Costa TD,Vistelle R,Rand KH,Derendorf H

更新日期：1996-04-01 00:00:00

abstract：:The presence of subvisible particles in formulations of therapeutic proteins is a risk factor for adverse immune responses. Although the immunogenic potential of particulate contaminants likely depends on particle structural characteristics (e.g., composition, size, and shape), exact structure-immunogenicity relations...

journal_title：Journal of pharmaceutical sciences

authors： Daniels AL,Randolph TW

更新日期：2018-05-01 00:00:00

abstract：:The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

journal_title：Journal of pharmaceutical sciences

authors： Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

更新日期：2004-06-01 00:00:00

abstract：:Plasma levels were determined frequently after single doses of perfluorooctyl bromide were administered to beagle dogs at doses of either 30.8 g/kg po or 3.9 g/kg intratracheally. The apparent first-order half-life during the terminal elimination phase was about 1 day after oral medication and about 7 days after intra...

journal_title：Journal of pharmaceutical sciences

authors： Lee FH,Scrime M,Edelson J

更新日期：1978-07-01 00:00:00

abstract：:The influence of commonly used excipients, spray-dried lactose (SDL), microcrystalline cellulose (MCC), and partially pregelatinized maize starch (Starch 1500) on drug release from hydroxypropyl methylcellulose (HPMC, hypromellose) matrix system has been investigated. A model formulation contained 30%w/w drug, 20%w/w ...

journal_title：Journal of pharmaceutical sciences

authors： Levina M,Rajabi-Siahboomi AR

更新日期：2004-11-01 00:00:00

abstract：:Tuberculosis (TB) is a serious infectious disease that affects more than new 10 million patients each year. Many of these cases are resistant to first-line drugs so second-line ones, like fluoroquinolones, need to be incorporated into the therapeutic. Ofloxacin (OF) is a fluoroquinolone which demonstrates high antibio...

journal_title：Journal of pharmaceutical sciences

authors： Ceschan NE,Rosas MD,Olivera ME,Dugour AV,Figueroa JM,Bucalá V,Ramírez-Rigo MV

更新日期：2020-09-01 00:00:00