Novel potential anticancer agents derived from benzimidazole.

abstract：:A procedure for the simultaneous analysis of diphenylhydantoin and phenobarbital in plasma by high-pressure liquid chromatography was developed and evaluated. Separation is effected on a porous particle silicic acid column with chloroform dioxane-isopropanol-acetic acid (310:9.7:1.0:0.1 by volume) and is monitored at ...

journal_title：Journal of pharmaceutical sciences

authors： Atwell SH,Green VA,Haney WG

更新日期：1975-05-01 00:00:00

abstract：:The binding of Cu2+ and Ni2+ to bovine, dog, and human serum albumin has been studied by the 35Cl NMR probe technique. The number of primary copper sites were estimated to be 1.3 for human serum albumin, 3.1 for bovine serum albumin, and 6.6 for dog serum albumin. A similar number of primary nickel sites was determine...

journal_title：Journal of pharmaceutical sciences

authors： Mohanakrishnan P,Chignell CF,Cox RH

更新日期：1985-01-01 00:00:00

abstract：:N-linked glycosylation is an important post translational modification that occurs on Asparagine 297 residue or a homologous position on the Fc portion of monoclonal antibodies (mAbs). mAb Fc glycans play important roles in antibody structure, stability, and function including effector function and pharmacokinetics. T...

journal_title：Journal of pharmaceutical sciences

authors： Voruganti S,Xu J,Li X,Balakrishnan G,Singh SM,Kar SR,Das TK

更新日期：2021-02-01 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 aim of the present work was to prepare and characterize chitosan-stearic acid conjugate nanomicelles for encapsulation of amphotericin B (AmB) and to evaluate the in vitro nebulization of the formulations. Water soluble chitosan was grafted to stearic acid (SA) chains via 1-ethyl-3-(3-dimethylaminopropyl)carbodiim...

journal_title：Journal of pharmaceutical sciences

authors： Gilani K,Moazeni E,Ramezanli T,Amini M,Fazeli MR,Jamalifar H

更新日期：2011-01-01 00:00:00

abstract：:Gender and immune status can considerably impact on the pharmacokinetics (PK) of macromolecular and small molecule drugs. However, these effects are often not considered in drug development. We aimed to quantitatively evaluate effects of gender and immune status on the PK of PEGylated interferon in frequently used mur...

journal_title：Journal of pharmaceutical sciences

authors： Landersdorfer CB,Caliph SM,Shackleford DM,Ascher DB,Kaminskas LM

更新日期：2015-05-01 00:00:00

abstract：:Diazepam (1), a hypnotic and anxiolytic drug in worldwide use, formed an intermediate product in a mixture of ethanol and sodium hydroxide ([NaOH] > or = 1 M). The intermediate product slowly decomposed to form 2-(methylamino)-5-chlorobenzophenone imine (2) and 2-(methylamino)-5-chlorobenzophenone (3). The amount of 2...

journal_title：Journal of pharmaceutical sciences

authors： Yang SK,Tang R,Yang TJ,Pu QL,Bao Z

更新日期：1996-07-01 00:00:00

abstract：:Sodium salicylate improves the rectal absorption of drugs which exhibit molecular self-association; it is suggested that salicylate may improve drug bioavailability by altering the drug self-association pattern. Methylene blue was chosen as a model molecule for investigating the interference of salicylate with drugs u...

journal_title：Journal of pharmaceutical sciences

authors： Touitou E,Fisher P

更新日期：1986-04-01 00:00:00

abstract：:A number of isomeric benzoylpyrroleacetic acids (1-6) were prepared and tested in vitro for rat lenses aldose reductase activity. These pyrrole derivatives are structurally related to the acidic nonsteroidal anti-inflammatory drugs. Therefore, their anti-inflammatory properties were also evaluated in the carrageenan-i...

journal_title：Journal of pharmaceutical sciences

authors： Demopoulos VJ,Rekka E

更新日期：1995-01-01 00:00:00

abstract：:Previously, we reported that repeated oral treatment with etoposide (ETP) increased ileal membrane localization of P-glycoprotein (P-gp) and that this was possibly mediated by increased expression of the ezrin/radixin/moesin (ERM)/phosphorylated ERM (p-ERM) via activation of RhoA/ROCK. These changes caused decreases i...

journal_title：Journal of pharmaceutical sciences

authors： Kobori T,Harada S,Nakamoto K,Tokuyama S

更新日期：2013-05-01 00:00:00

abstract：:This whitepaper highlights current challenges and opportunities associated with continuous synthesis, workup, and crystallization of active pharmaceutical ingredients (drug substances). We describe the technologies and requirements at each stage and emphasize the different considerations for developing continuous proc...

journal_title：Journal of pharmaceutical sciences

authors： Baxendale IR,Braatz RD,Hodnett BK,Jensen KF,Johnson MD,Sharratt P,Sherlock JP,Florence AJ

更新日期：2015-03-01 00:00:00

abstract：:In spite of the recent advances in technology to optimize the absorption, distribution, metabolism and elimination (ADME) properties of new and promising medicinal products to reduce clinical failures, the investigation of drug disposition in the pediatric and elderly populations continues to be under evaluated. With ...

journal_title：Journal of pharmaceutical sciences

authors： Chien JY,Ho RJ

更新日期：2011-01-01 00:00:00

abstract：:Various complex mechanisms and their multifactorial pathways decisively provoke low-grade local and systemic inflammation in β-cells of pancreatic islets and peripheral tissues to induce β-cells' dysfunction and apoptosis, insulin resistance, and ultimately, overt type 2 diabetes mellitus (T2DM). Conventional antidiab...

journal_title：Journal of pharmaceutical sciences

authors： Akash MS,Shen Q,Rehman K,Chen S

更新日期：2012-05-01 00:00:00

abstract：:The crystal structure of zolpidem hemitartrate hemihydrate (I, Form E) has been solved from high-resolution laboratory powder diffraction data. It crystallizes in the orthorhombic P2(1)2(1)2(1) space group with a = 22.4664(6) A, b = 26.0420(7) A, and c = 7.4391(1) A. Protonation of zolpidem molecules could not be unam...

journal_title：Journal of pharmaceutical sciences

authors： Halasz I,Dinnebier RE

更新日期：2010-02-01 00:00:00

abstract：:Acetylcarnitine, a naturally occurring compound found in high concentration in heart and skeletal muscle of vertebrates, bears structural resemblance to acetylcholine, and studies have shown that it has slight cholinergic properties. Acetylcarnitine was subjected to conformational analysis by extended Hückel theory (E...

journal_title：Journal of pharmaceutical sciences

authors： Reed KW,Murray WJ,Roche EB

更新日期：1980-09-01 00:00:00

abstract：:Terbinafine is an allylamine antifungal agent that is highly lipophilic and keratophilic. The aim of this study was to investigate terbinafine distribution in peripheral and visceral tissues after intravenous administration to rats. Terbinafine, 6 mg/kg, was administered to 33 male Sprague-Dawley rats via a jugular ve...

journal_title：Journal of pharmaceutical sciences

authors： Hosseini-Yeganeh M,McLachlan AJ

更新日期：2001-11-01 00:00:00

abstract：:Mixing Fungizone with a fat emulsion used for nutritional purpose (Intralipid or Lipofundin ) was reported to decrease Amphotericin B (AmB) toxicity in clinical use. In an effort to understand the reason for this phenomenon, spectral and morphological analyses were done for the Fungizone and Fungizone /Lipofundin admi...

journal_title：Journal of pharmaceutical sciences

authors： Egito ES,Araújo IB,Damasceno BP,Price JC

更新日期：2002-11-01 00:00:00

abstract：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 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：:This article discusses the evaluation of drug candidates as hepatic transporter substrates. Recently, research on the applications of hepatic transporters in the pharmaceutical industry has improved to meet the requirements of the regulatory guidelines for the evaluation of drug interactions. To identify the risk of t...

journal_title：Journal of pharmaceutical sciences

authors： Okudaira N

更新日期：2017-09-01 00:00:00

abstract：:In relation to drug release properties the lateral and rotational mobility of two drugs and one drug mimic in photopolymerized poly(ethylene glycol) diacrylate (PEGDA) networks were investigated by nuclear magnetic resonance as a function of the network cross-link density and temperature. The network mesh size affects...

journal_title：Journal of pharmaceutical sciences

authors： Tomić K,Veeman WS,Boerakker M,Litvinov VM,Dias AA

更新日期：2008-08-01 00:00:00

abstract：:Oxidative-reductive interconversion of the methylthiomethyl ester of aspirin and the corresponding sulfoxide and sulfone derivatives can be detected in rat liver homogenate, in addition to the extremely facile hydrolysis of these esters. The methylthiomethyl and methylsulfinylmethyl 2-acetoxybenzoates penetrate freshl...

journal_title：Journal of pharmaceutical sciences

authors： Loftsson T,Bodor N

更新日期：1981-07-01 00:00:00

abstract：:The bioavailability of three different brands and three different dosage forms of doxycycline was studied in normal subjects. Single doses, equivalent to 200 mg of doxycycline, were administered to six subjects in a crossover design as the innovator's intravenous solution given orally (Treatment A), the innovator's ca...

journal_title：Journal of pharmaceutical sciences

authors： Antal EJ,Jaffe JM,Poust RI,Colaizzi JL

更新日期：1975-12-01 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：:To reduce the risk of immunogenicity that may be caused by therapeutic protein products, it is important to properly characterize subvisible particles and to develop strategies to reduce the levels of particles delivered to patients. In the present study, by using state-of-the-art methods to quantify particle levels, ...

journal_title：Journal of pharmaceutical sciences

authors： Ueda T,Nakamura K,Abe Y,Carpenter JF

更新日期：2019-01-01 00:00:00

abstract：:The plasma nitroglycerin levels obtained after intracardial (0.7 mg/kg), oral (7 mg/kg), and topical (7--14 mg/kg) doses of nitroglycerin in rats are reported. Nitroglycerin followed essentially one-compartment kinetics after intracardial administration, showing a mean half-life of about 4 min and a mean apparent volu...

journal_title：Journal of pharmaceutical sciences

authors： Yap PS,Fung HL

更新日期：1978-04-01 00:00:00

abstract：:Thymoquinone (TQ) is the main bioactive component isolated from Nigella sativa essential oil and seeds and has been used for the treatment of inflammations, liver disorders, arthritis, and is of great importance as a promising therapeutic drug for different diseases including cancer. This paper reports the first exper...

journal_title：Journal of pharmaceutical sciences

authors： Lupidi G,Camaioni E,Khalifé H,Avenali L,Damiani E,Tanfani F,Scirè A

更新日期：2012-07-01 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：:The binding of representative chemical classes of nonsteroidal anti-inflammatory drugs (NSAIDs) to human serum albumin (HSA) was investigated by equilibrium dialysis. Warfarin enantiomers were used as specific markers in displacement studies. Data were analyzed by a computerized nonlinear least squares approach design...

journal_title：Journal of pharmaceutical sciences

authors： Li KL,Thakur AK,Kapoor AL

更新日期：1988-03-01 00:00:00

abstract：:Insulin-degrading enzyme (IDE) has been implicated in the intracellular degradation of insulin in insulin target cells. Knowledge of the existence of this enzyme in the intestine will be beneficial to the achievement of clinical oral efficacy of insulin. A comparative study was conducted with rat intestine, human colo...

journal_title：Journal of pharmaceutical sciences

authors： Chang LL,Stout LE,Wong WD,Buls JG,Rothenberger DA,Shier WT,Sorenson RL,Bai JP

更新日期：1997-01-01 00:00:00