2-(methylamino)-5-chlorobenzophenone imine: a novel product formed in base-catalyzed hydrolysis of diazepam.

abstract：:Ambrisentan is a nonsulfonamide, ET(A)-selective endothelin receptor antagonist (ERA) approved for the treatment of pulmonary arterial hypertension (PAH), and tadalafil is a phosphodiesterase type 5 (PDE-5) inhibitor under investigation for treatment of PAH. Due to the potential combination use, the pharmacokinetic (P...

journal_title：Journal of pharmaceutical sciences

authors： Spence R,Mandagere A,Harrison B,Dufton C,Boinpally R

更新日期：2009-12-01 00:00:00

abstract：:A modification of wet agglomeration technique is developed and demonstrated by agglomerative crystallization process for a nonapeptide (ABT-510) to improve processing of needle like crystals. Our procedure involves exploiting partial miscibility of the crystallization solvent system for in situ generation of a wetting...

journal_title：Journal of pharmaceutical sciences

authors： Sheikh AY,Pal A,Viswanath S,Tolle JC

更新日期：2008-03-01 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：:Glycerol stabilizes cyanocob(III)alamin (vitamin B12) against anaerobic photolysis by a high-intensity UV light source or a low-intensity fluorescent light source. The likely mechanism for stabilization by viscosigens is a decrease in diffusion and an enhancement of radical-pair recombination. Glycerol (25% or greater...

journal_title：Journal of pharmaceutical sciences

authors： Grissom CB,Chagovetz AM,Wang Z

更新日期：1993-06-01 00:00:00

abstract：:A sensitive, specific, high-performance liquid chromatographic procedure was developed for the measurement of plasma tiflamizole levels. Acidic plasma samples were extracted with three volumes of ether. The ether extracts were combined and evaporated to dryness. The residue was dissolved in acetonitrile, washed with h...

journal_title：Journal of pharmaceutical sciences

authors： Rakestraw DC,Whitney CC Jr

更新日期：1984-12-01 00:00:00

abstract：:A new High-performance liquid chromatographic (HPLC) method for the assay of sodium fusidate (I) or fusidic acid in dosage forms was developed and compared to a microbiological assay. A linear relationship was obtained between absolute peak area and amount of I(r = 0.99+) in the 50-1000-microgram/ml range. In the micr...

journal_title：Journal of pharmaceutical sciences

authors： Hikal AH,Shibl A,El-Hoofy S

更新日期：1982-11-01 00:00:00

abstract：:The adsorption of cimetidine on selected pharmaceuticals including kaolin, activated charcoal, talc, and nonsystemic antacids was determined at pH 5.0 and 25 degrees. The Langmuir and Freundlich adsorption isotherms showed that cimetidine adsorption was significant with activated charcoal, kaolin, talc, and magnesium ...

journal_title：Journal of pharmaceutical sciences

authors： Ganjian F,Cutie AJ,Jochsberger T

更新日期：1980-03-01 00:00:00

abstract：:Acyclovir is an antiviral drug poorly absorbed in the gastrointestinal tract due to its hydrophilicity, with low oral bioavailability (~20%). Although acyclovir is prescribed in the management of herpes simplex encephalitis (HSE), the disease has a poor prognosis, particularly if the treatment is delayed, reaching mor...

journal_title：Journal of pharmaceutical sciences

authors： Gurgel Assis MS,Fernandes Pedrosa TC,de Moraes FS,Caldeira TG,Pereira GR,de Souza J,Ruela ALM

更新日期：2021-01-13 00:00:00

abstract：:The transdermal delivery of 2 fluorescent probes with similar molecular weight but different lipophilicity, into and through the skin from 2 commercially available transdermal bases, pluronic lecithin organogel, and Lipoderm® has been evaluated. First, in vitro penetration of fluorescein sodium and fluorescein (free a...

journal_title：Journal of pharmaceutical sciences

authors： Zhang Q,Song Y,Page SW,Garg S

更新日期：2018-02-01 00:00:00

abstract：:NMR was used to study the binding of acetylcholine, atropine, and physostigmine to acetylcholinesterase. Changes in the linewidth of the N-methyl resonance of acetylcholine, resulting from association with the enzyme during hydrolysis, were utilized to study the enzyme-substrate interaction. Physostigmine inhibited th...

journal_title：Journal of pharmaceutical sciences

authors： Kato G

更新日期：1975-03-01 00:00:00

abstract：:The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

journal_title：Journal of pharmaceutical sciences

authors： Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

更新日期：1989-01-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00

abstract：:The purpose of this study was to evaluate the therapeutic efficacy of a new calcium phosphate (CaP)-based formulation in improving the bone mineral deficiency in ovariectomized (OVX) rats. The ions release experiments for CaP preparations (G2: 0.46% Mg, 5.78% Zn, and 2.5% F; G3:3.1% Mg, 0.03% Zn, and 3.01% F; G4: 1.25...

journal_title：Journal of pharmaceutical sciences

authors： Otsuka M,Oshinbe A,Legeros RZ,Tokudome Y,Ito A,Otsuka K,Higuchi WI

更新日期：2008-01-01 00:00:00

abstract：:The correlation of log P (in octanol--water) with the nonempirical, topologically dependent, calculated molecular connectivity index (1chiv) delineates substituted hydroxyureas into two families of linearly related groups of compounds. The first group, composed of the 3-substituted ethyl, n-propyl, and n-butyl analogs...

journal_title：Journal of pharmaceutical sciences

authors： Parker GR

更新日期：1978-04-01 00:00:00

abstract：:An extension of the Bischoff-Dedrick pharmacokinetic model is presented. This model is derived from basic considerations of drug distrubition with physiological and anatomical meaning. The Bischoff-Dedrick model can simultaneously predict drug distribution with time in blood, organs, and tissues of pharmacological int...

journal_title：Journal of pharmaceutical sciences

authors： Chen CN,Andrade JD

更新日期：1976-05-01 00:00:00

abstract：:The influences of 1-ethyl-, 1-butyl-, 1-hexyl-, and 1-octyl-2-pyrrolidone in their saline solutions on the transport of beta-estradiol, corticosterone, and hydrocortisone across hairless mouse skin under in vitro conditions have been investigated by the physical model approach. The experimental data were interpreted w...

journal_title：Journal of pharmaceutical sciences

authors： Yoneto K,Ghanem AH,Higuchi WI,Peck KD,Li SK

更新日期：1995-03-01 00:00:00

abstract：:The pKa values of benzoic acid, p-methylbenzoic, and p-aminobenzoic acid (PABA) were determined by potentiometric titration in mixtures of 0-0.5 volume fractions of various cosolvents and water. The differences between the aqueous and semiaqueous pKa values were similar for the three solutes at a particular cosolvent-...

journal_title：Journal of pharmaceutical sciences

authors： Rubino JT,Berryhill WS

更新日期：1986-02-01 00:00:00

abstract：:An electron-capture GLC method was developed for measuring pindolol in human plasma and urine. The unchanged drug was extracted with benzene from alkalinized plasma or urine using propranolol as the internal standard. Both compounds subsequently were back-extracted into 0.1 M HCl and then into benzene. After evaporati...

journal_title：Journal of pharmaceutical sciences

authors： Guerret M,Lavene D,Kiechel JR

更新日期：1980-10-01 00:00:00

abstract：:A sensitive (10 ng/mL) and specific high-performance liquid chromatographic (HPLC) assay, with electrochemical (EC) detection, for the geometric isomers of 3-hydroxy-N-(2-phenyl-2-(2-thienyl)ethenyl-5-(trifluoromethyl)benzo(b) thiophene-2-carboxamide in dog and human plasma has been developed. Both isomers strongly ab...

journal_title：Journal of pharmaceutical sciences

authors： Matuszewski BK,Kanovsky SM,Constanzer ML,Yeh KC,Bayne WF

更新日期：1988-10-01 00:00:00

abstract：:Melanotan-II (1) is a cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH) which tans the skin and is currently being evaluated for the prevention of sunlight-induced skin cancers. The dissociation constants of 1 were determined using potentiometric titration and ultraviolet spectrophotomet...

journal_title：Journal of pharmaceutical sciences

authors： Lan EL,Ugwu SO,Blanchard J,Fang X,Hruby VJ,Sharma S

更新日期：1994-08-01 00:00:00

abstract：:Intranasal delivery of flurazepam, midazolam, and triazolam was studied in a dog model as a possible alternate route of drug administration for treatment of insomnia. Four beagles received each hypnotic by both intranasal and oral routes on two separate occasions. Plasma concentrations for each hypnotic after dosing w...

journal_title：Journal of pharmaceutical sciences

authors： Lui CY,Amidon GL,Goldberg A

更新日期：1991-12-01 00:00:00

abstract：:99mTc-N-(3-bromo-2,4,6-trimethylacetanilide)iminodiacetat e (I) and 99mTc-N-pyridoxyl-5-methyl-tryptophan (II) have been described as having optimal properties as hepatobiliary radiopharmaceuticals. This study compared specificity for hepatobiliary excretion, blood disappearance, rates of biliary appearance, and pharm...

journal_title：Journal of pharmaceutical sciences

authors： Fritzberg AR,Bloedow DC,Eshima D,Johnson DL

更新日期：1984-12-01 00:00:00

abstract：:The purpose of this study was to investigate the feasibility of delivering sinomenine hydrochloride (SH) transdermally using composite dissolving microneedles (DM) which integrated with liquid crystals (H2). The fabricated SH-loaded composite DM was evaluated for their appearance, mechanical strength, irritation, and ...

journal_title：Journal of pharmaceutical sciences

authors： Gui Z,Wu X,Wang S,Cao Y,Wan J,Shan Q,Yang Z,Zhang J,Gui S

更新日期：2017-12-01 00:00:00

abstract：:The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...

journal_title：Journal of pharmaceutical sciences

authors： Wuyts B,Brouwers J,Mols R,Tack J,Annaert P,Augustijns P

更新日期：2013-10-01 00:00:00

abstract：:Sol-to-gel systems of ciprofloxacin hydrochloride were prepared utilizing the phase transition properties of hydroxy propyl methyl cellulose K 15 M grade (HPMC) and carbopol 934. The sol-to-gel systems were sterilized by gamma radiation and/or filtration. The sol-to-gel systems were evaluated for rheological character...

journal_title：Journal of pharmaceutical sciences

authors： Charoo NA,Kohli K,Ali A

更新日期：2003-02-01 00:00:00

abstract：:Review of the current literature on racial differences in pharmacokinetics of drugs supports the premise that only pharmacokinetic processes which are biologically or biochemically mediated have the potential to exhibit differences between racial or ethnic groups. Thus, the pharmacokinetic factors which can be expecte...

journal_title：Journal of pharmaceutical sciences

authors： Johnson JA

更新日期：1997-12-01 00:00:00

abstract：:Two high-performance liquid chromatographic (HPLC) assay procedures were developed for the determination of salicylamide and its metabolites in serum, urine, and saliva. One method involves reverse-phase ion-pair chromatography and UV detection, and is used to determine salicylamide, salicylamide glucuronide, and sali...

journal_title：Journal of pharmaceutical sciences

authors： Morris ME,Levy G

更新日期：1983-06-01 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：:Literature data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the marketing authorization of immediate-release, solid oral dosage forms containing enalapril maleate are reviewed. Enalapril, a prodrug, is hydrolyzed by carboxylesterases to the active angiotensin-converting enzyme inhi...

journal_title：Journal of pharmaceutical sciences

authors： Verbeeck RK,Kanfer I,Löbenberg R,Abrahamsson B,Cristofoletti R,Groot DW,Langguth P,Polli JE,Parr A,Shah VP,Mehta M,Dressman JB

更新日期：2017-08-01 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