Steroidal thiourea and thiazoline derivatives: synthesis and in vitro effects on bovine pancreatic ribonuclease activity.

abstract：:The aim of this study was to characterize the in vitro hepatic uptake kinetics of sodium fluorescein (NaFluo) and identify the transporters involved. NaFluo exhibited saturable uptake kinetics in suspended rat and human hepatocytes as reflected by K(m) values of 22.5 and 14.1 µM, and V(max) values of 98.3 and 5.8 pmol...

journal_title：Journal of pharmaceutical sciences

authors： De Bruyn T,Fattah S,Stieger B,Augustijns P,Annaert P

更新日期：2011-11-01 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：:A high-performance liquid chromatographic method for the simultaneous determination of propranolol and 4-hydroxypropranolol in plasma is presented. The method involves plasma extraction at basic pH with ethyl column, and fluorescence detection. The within-run a reversed-phase column coefficient of variation were 3.0-7...

journal_title：Journal of pharmaceutical sciences

authors： Rosseel MT,Bogaert MG

更新日期：1981-06-01 00:00:00

abstract：:Employing the roots of Iris missouriensis, two known triterpenes, iso-iridogermanal and zeorin, were isolated and identified. As presently reported, they were found to demonstrate cytotoxic activity toward cultured P-388 cells (ED50 = 0.1 and 1.1 microgram/mL, respectively). Additionally, a new triterpene that demonst...

journal_title：Journal of pharmaceutical sciences

authors： Wong SM,Oshima Y,Pezzuto JM,Fong HH,Farnsworth NR

更新日期：1986-03-01 00:00:00

abstract：:Minitablets are an appealing option for an age-appropriate pediatric dosage form. In particular, for combination therapies where multiple active ingredients are dosed simultaneously, the use of minitablets will enable independent adjustments of each dose. The work presented describes the development of Compound A and ...

journal_title：Journal of pharmaceutical sciences

authors： Zhang D,Rumondor ACF,Zhu W,Colace T,Marota M,Mora J,Liu Z,Li Y

更新日期：2020-12-01 00:00:00

abstract：:The objective of this study was to determine the relative importance of metabolism by cytochrome P450 (CYP) enzymes versus efflux by P-glycoprotein (P-gp) in restricting the intestinal mucosal permeation of cyclic prodrugs (AOA-DADLE, CA-DADLE, OMCA-DADLE) of the opioid peptide DADLE (H-Tyr-D-Ala-Gly-Phe-D-Leu-OH). AO...

journal_title：Journal of pharmaceutical sciences

authors： Ouyang H,Chen W,Andersen TE,Steffansen B,Borchardt RT

更新日期：2009-01-01 00:00:00

abstract：:Granules prepared by the high shear wet granulation (HSWG) process commonly exhibit the problem of overgranulation, a phenomenon characterized by a severe loss of the ability to form adequately strong tablet. We hypothesize that the incorporation of brittle excipients promotes brittle fracture of granules during compa...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Yeboah F,Zhang M,Feng Y,Sun CC

更新日期：2014-08-01 00:00:00

abstract：:Phosphate is specifically adsorbed by aluminum hydroxycarbonate by anion ligand exchange. IR analysis indicated that phosphate exchanged with specifically adsorbed carbonate. Adsorption is favored by low pH and is inversely related to particle size. Adsorption of phosphate decreases the rate of acid neutralization of ...

journal_title：Journal of pharmaceutical sciences

authors： Liu JC,Feldkamp JR,White JL,Hem SL

更新日期：1984-10-01 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：:Simple assays for extraction and determination of the concentrations of the antibiotics oxytetracycline, oxolinic acid, and flumequine in a drug dosage form for farmed fish are described. HPLC with UV detection was used in the analyses. The recovery of all three drugs was approximately 100%, and the precision varied f...

journal_title：Journal of pharmaceutical sciences

authors： Rogstad A,Weng B

更新日期：1993-05-01 00:00:00

abstract：:A method for the measurement of a potential diuretic-antihypertensive agent, (+/-)-[[6,7-dichloro-2-(4-fluorophenyl)-2-methyl-1-oxo-5-indanyl] oxy]acetic acid, in biological fluids is described. The procedure involves the addition of a related internal standard to the specimens followed by extraction of the acids into...

journal_title：Journal of pharmaceutical sciences

authors： Weidner LL,Zacchei AG

更新日期：1984-02-01 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：:Cyclosporin A (CyA) is a good candidate for incorporation in colloidal carriers such as nanoparticles (NP) that would diminish the adverse effects associated with its use under conventional pharmaceutical dosage forms and improve bioavailability after oral administration. In this study a composite rotational experimen...

journal_title：Journal of pharmaceutical sciences

authors： Molpeceres J,Guzman M,Aberturas MR,Chacon M,Berges L

更新日期：1996-02-01 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：: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：:6-Chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid hydrochloride lowered serum cholesterol, triglyceride, phospholipid, and free fatty acid levels in normal rats. The compound appeared to have a low toxicity and to be well tolerated in mice, adult and neonatal rats, and rabbits. At ...

journal_title：Journal of pharmaceutical sciences

authors： Dalton C,Pool WR

更新日期：1977-03-01 00:00:00

abstract：:This work reports the measurement of the partition rate of a model drug, ibuprofen (IBU), from aqueous solutions into octanol in the absence and presence of common pharmaceutical excipients including glucose, lactose, maltoheptaose, hydroxypropyl methylcellulose, polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetat...

journal_title：Journal of pharmaceutical sciences

authors： Xu H,Wang W,Shi Y,Gao P

更新日期：2019-01-01 00:00:00

abstract：:The dissolution rates of a number of drug-urethan solid-state dispersion systems were studied. A marked enhancement of the initial dissolution rates of several poorly water-soluble drugs was found when they were incorporated into a urethan matrix by heat fusion. These differences were considerable when pure substances...

journal_title：Journal of pharmaceutical sciences

authors： Maulding HV

更新日期：1978-03-01 00:00:00

abstract：:High pressure liquid chromatography using reversed-phase and/or ion-pair techniques was used to optimize resolution of aspirin-containing muscle relaxant mixtures as well as other therapeutic agents commonly found in muscle relaxant-analgesic mixtures. The compounds were chromatographed on an octadecylsilane column us...

journal_title：Journal of pharmaceutical sciences

authors： Stewart JT,Honigberg IL,Coldren JW

更新日期：1979-01-01 00:00:00

abstract：:Although displacement from plasma protein binding (dPB) is usually of little clinical significance, it should be taken into account when interpreting changes in total plasma concentrations of drugs subject to metabolically based drug-drug interactions (mDDI). The aim of this study was to develop an approach to predict...

journal_title：Journal of pharmaceutical sciences

authors： Christensen H,Baker M,Tucker GT,Rostami-Hodjegan A

更新日期：2006-12-01 00:00:00

abstract：:The dissolution rates of the two polymorphic forms of sulfathiazole containing polyethylene glycol 4000 were significantly different in water. The effect of agitation on the dissolution rates also was studied. At higher stirring speeds, the dissolution rates of the stable form were affected more than the metastable fo...

journal_title：Journal of pharmaceutical sciences

authors： Niazi S

更新日期：1976-02-01 00:00:00

abstract：:The adsorption of quinidine onto kaolin was studied as a function of pH in aqueous solutions in which the ionic strength was adjusted to 0.1. The interaction of quinidine with pectin also was investigated in water and in phosphate buffer; the buffer pH and ionic strength were adjusted to 6.5 and 0.1, respectively. The...

journal_title：Journal of pharmaceutical sciences

authors： Bucci AJ,Myre SA,Tan HS,Shenouda LS

更新日期：1981-09-01 00:00:00

abstract：:Die filling is a critical process step during tablet production as it defines the tablet weight. Achieving die fill consistency during production of mini-tablets, tablets with diameters ≤6 mm, is considerably more challenging. Although die filling in rotary presses had been studied in relation to the feed paddle desig...

journal_title：Journal of pharmaceutical sciences

authors： Goh HP,Sia Heng PW,Liew CV

更新日期：2019-03-01 00:00:00

abstract：:Aqueous solutions of several ionizable substances were stored in plastic infusion bags and the sorption of the substances monitored with time. The substances used were p-nitrophenol, p-toluidine, warfarin sodium [3-(alpha-acetonylbenzyl)-4-hydroxycoumarin sodium salt] and trifluoperazine hydrochloride (10-[3-(4-methyl...

journal_title：Journal of pharmaceutical sciences

authors： Kowaluk EA,Roberts MS,Polack AE

更新日期：1986-06-01 00:00:00

abstract：:The central compartment of an n-compartment mammillary model was concatenated with a gradient compartment (i.e., venous sampling compartment) and with a conventional effect compartment to model arterial-venous drug concentration gradients and the arterial drug concentration vs effect relationship, respectively. To mod...

journal_title：Journal of pharmaceutical sciences

authors： Jacobs JR,Nath PA

更新日期：1995-03-01 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：:There is a growing interest in developing inhibitors of the neonatal Fc-receptor, FcRn, for use in the treatment for humoral autoimmune conditions. We have developed a new physiologically based pharmacokinetic model that is capable of characterizing the pharmacokinetics and pharmacodynamics of anti-FcRn monoclonal ant...

journal_title：Journal of pharmaceutical sciences

authors： Li T,Balthasar JP

更新日期：2019-01-01 00:00:00

abstract：:Since its inception in the 1930s, disintegration testing has become an important quality control (QC) test in pharmaceutical industry, and disintegration test procedures for various dosage forms have been described by the different pharmacopoeias, with harmonization among them still not quite complete. However, becaus...

journal_title：Journal of pharmaceutical sciences

authors： Al-Gousous J,Langguth P

更新日期：2015-09-01 00:00:00

abstract：:The use of second generation cationic liposomes to deliver cytotoxic drugs to solid tumors is a rational and promising therapeutic approach, given the natural affinity of cationic carrier molecules for the tumor microvasculature. Cationic liposomal therapeutics are effective in the treatment of cancers that are resist...

journal_title：Journal of pharmaceutical sciences

authors： Campbell RB,Ying B,Kuesters GM,Hemphill R

更新日期：2009-02-01 00:00:00

abstract：:The objective of this study was to determine reasons behind the low oral (p.o.) bioavailability of glucosamine. By using male Sprague-Dawley rats, the movement of glucosamine through everted gut, the effect of dose and glucose, and inhibition of a glucose transporter (GLUT2) by quercetin were studied. Glucosamine phar...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim A,Gilzad-kohan MH,Aghazadeh-Habashi A,Jamali F

更新日期：2012-07-01 00:00:00