Usefulness of PBPK Modeling in Incorporation of Clinical Conditions in Personalized Medicine.

abstract：:The plasma protein binding of zomepirac, a new nonnarcotic analgesic, was studied using equilibrium dialysis. Experiments were performed using human plasma and plasma from mice, rats, and rhesus monkeys, all species of pharmacological or toxicological interest. At concentrations approximating those achieved in vivo, t...

journal_title：Journal of pharmaceutical sciences

authors： O'Neill PJ

更新日期：1981-07-01 00:00:00

abstract：:The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...

journal_title：Journal of pharmaceutical sciences

authors： Kobuchi S,Kita Y,Hiramatsu Y,Sasaki K,Uno T,Ito Y,Sakaeda T

更新日期：2021-02-01 00:00:00

abstract：:When heated at temperatures in excess of 100 degrees, the stability of neomycin in aqueous ophthalmic formulations was improved by the addition of edetate disodium (0.01%). As the exposure temperature was reduced, the degree of stability enhancement diminished until the effect was reversed, and addition of edetate dis...

journal_title：Journal of pharmaceutical sciences

authors： Hodges NA,Walton PG

更新日期：1981-08-01 00:00:00

abstract：:A rapid and sensitive GLC method was developed for the quantitative determination of methenamine in tablets. The method was shown to possess several advantages over the official NF assay. After dissolution of the whole tablet in absolute ethanol and addition of an internal standard (pentylenetetrazol), an aliquot was ...

journal_title：Journal of pharmaceutical sciences

authors： Strom JG Jr,Jun HW

更新日期：1977-04-01 00:00:00

abstract：:Oxidation of 7,8-dimethoxy-1,2,3,4-tetrahydroisoquinoline with potassium permanganate in acetone afforded 7,8-dimethoxy-3,4-dihydroisoquinoline as the primary product. Hence, oxidation of the appropriate secondary nonphenolic 7,8-dioxygenated tetrahydroisoquinoline alkaloid is thus a facile method for the generation o...

journal_title：Journal of pharmaceutical sciences

authors： el-Fishawy AM,Slatkin DJ,Knapp JE,Schiff PL Jr

更新日期：1984-11-01 00:00:00

abstract：:Three aspirin derivatives, aspirin phenylalanine ethyl ester, aspirin phenylalanine amide, and aspirin phenyllactic ethyl ester, were investigated with respect to their hydrolysis by alpha-chymotrypsin. Of the three compounds, aspirin phenylalanine ethyl ester was the best substrate, with kcat = 25 sec-1 and Km = 1.3 ...

journal_title：Journal of pharmaceutical sciences

authors： Banerjee PK,Amidon GL

更新日期：1981-12-01 00:00:00

abstract：:To preserve the positive effect of collagen on tissue regeneration and to locally deliver low molecular weight compounds for an extended time period, a composite for parenteral application was devised based on a collagen sponge with gentamicin-loaded PLGA microparticles incorporated. Antibiotic liberation from the par...

journal_title：Journal of pharmaceutical sciences

authors： Schlapp M,Friess W

更新日期：2003-11-01 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：:The application of a stable isotope coadministration technique for estimating the fraction (fm) of imipramine (IP) that is converted to desipramine (DMI) is described. Four healthy male subjects received 25 mg of IP-d4 hydrochloride orally with 25 mg of DMI hydrochloride. The plasma concentrations of IP-d4, DMI-d4, an...

journal_title：Journal of pharmaceutical sciences

authors： Sasaki Y,Shinohara Y,Baba S

更新日期：1990-02-01 00:00:00

abstract：:In iontophoresis, an electric field across the skin induces electromigration of exogenously applied and endogenously present ions. The approach can be used to improve dramatically drug delivery by elimination of competing co-ions in the externally applied formulation, as this maximizes the fraction of current carried ...

journal_title：Journal of pharmaceutical sciences

authors： Mudry B,Guy RH,Delgado-Charro MB

更新日期：2006-03-01 00:00:00

abstract：:Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the ...

journal_title：Journal of pharmaceutical sciences

authors： Hersey SJ,Jackson RT

更新日期：1987-12-01 00:00:00

abstract：:A physically based method for arriving at topological indexes is described. The derived indexes correlate with molecular surface areas and with the molecular connectivity index. The newly derived index seems to account better for the expected distinctions among primary, secondary, and tertiary alcohol aqueous solubili...

journal_title：Journal of pharmaceutical sciences

authors： Cammarata A

更新日期：1979-07-01 00:00:00

abstract：:A stability-indicating assay procedure for the determination of norethindrone on the surface of Red Delicious apple slices was developed. The apple slice is homogenized in pH 10 borate buffer solution and norethindrone is then partitioned into chloroform using a diffusion chamber that has a membrane that is permeable ...

journal_title：Journal of pharmaceutical sciences

authors： Mayberry DO,Kowblansky M,Lane PA,Wray PE

更新日期：1990-08-01 00:00:00

abstract：:The significance of factors such as drug solubility, polymer molecular weight, drug loading dose, compression force, and hydrodynamic conditions on drug release from a swellable hydrophilic delivery system was investigated. Hydroxypropyl methylcellulose (HPMC) and pectin were major polymeric constituents of the delive...

journal_title：Journal of pharmaceutical sciences

authors： Kim H,Fassihi R

更新日期：1997-03-01 00:00:00

abstract：:A method for establishing sampling plans for in-house limits that fix both the producer's and consumer's risks is presented for pharmaceutical systems in which both between-batch and within-batch variations are present. Such plans can always be constructed and require more or less sample assays depending on the variab...

journal_title：Journal of pharmaceutical sciences

authors： Bolton S

更新日期：1983-04-01 00:00:00

abstract：:The aims of this study were to evaluate the pharmacokinetics of doripenem (Finibax®, Doribax®, S-4661), a parenteral carbapenem antibiotic, in pediatric patients based on concentrations of doripenem in plasma after administration of 20 mg/kg 2 or 3 times daily and to evaluate the dosing regimens by using Monte-Carlo p...

journal_title：Journal of pharmaceutical sciences

authors： Matsuo Y,Ishibashi T,Matsumoto S,Katsube T,Wajima T

更新日期：2019-09-01 00:00:00

abstract：:A recirculation technique was used to study the first-order kinetics of intestinal absorption of un-ionized sulfadiazine, sulfamerazine, and sulfamethazine in rats in situ at 32, 35, and 38 degrees C. The absorption rate constant (Kab) of each sulfonamide increased with increase in temperature and, at each temperature...

journal_title：Journal of pharmaceutical sciences

authors： Chow SL,Nagwekar JB

更新日期：1993-12-01 00:00:00

abstract：:The dissolution characteristics of dicumarol were markedly enhanced by preparing dispersions of drug in polyethylene glycol 4000. Solid dispersions of varying weight fractions were formed by a melt method without measurable drug degradation or evaporation. There were no significant differences in dissolution rates amo...

journal_title：Journal of pharmaceutical sciences

authors： Ravis WR,Chen CY

更新日期：1981-12-01 00:00:00

abstract：:Therapeutic antibodies and antibody derivatives comprise the majority of today's biotherapeutics. Routine methods to generate novel antibodies, such as immunization and phage-display, often give rise to several candidates with desired functional properties. On the contrary, resource-intense steps such as the developme...

journal_title：Journal of pharmaceutical sciences

authors： Jarasch A,Koll H,Regula JT,Bader M,Papadimitriou A,Kettenberger H

更新日期：2015-06-01 00:00:00

abstract：:Peptide-Fc fusion proteins (or peptibodies) are chimeric proteins generated by fusing a biologically active peptide with the Fc-domain of immunoglobulin G. In this review, we describe recent studies that have evaluated the absorption, distribution, metabolism, and excretion characteristics of peptibodies. Key features...

journal_title：Journal of pharmaceutical sciences

authors： Wu B,Sun YN

更新日期：2014-01-01 00:00:00

abstract：:We previously reported nonaqueous silicone elastomer gels (SEGs) for sustained vaginal administration of the CCR5-targeted entry inhibitor maraviroc (MVC). Here, we describe chemically modified SEGs (h-SEGs) in which the hydrophobic cyclomethicone component was partially replaced with relatively hydrophilic silanol-te...

journal_title：Journal of pharmaceutical sciences

authors： Forbes CJ,McCoy CF,Murphy DJ,Woolfson AD,Moore JP,Evans A,Shattock RJ,Malcolm RK

更新日期：2014-05-01 00:00:00

abstract：:The synthesis of some substituted 7-hydroxy-5H-1,3,4-oxadiazolo [3,2-a]pyrimidin-5-ones, a class of bicyclics with unexplored pharmacotoxicological properties, is described. Reacting the 2-phenyl derivative with bis(2,4,5-trichlorophenyl)benzylmalonate afforded a linear pyrano-oxadiazolopyrimidinedione. The assigned s...

journal_title：Journal of pharmaceutical sciences

authors： Soliman FS,Shafik RM,Darwish M

更新日期：1982-02-01 00:00:00

abstract：:Statistical assessment of bioavailability and bioequivalence of drug products is generally carried out with a univariate analysis by independently comparing each relevant parameter [such as, area under the drug concentration curve (AUC) and peak drug concentration (Cmax)] of the test and reference products. The assump...

journal_title：Journal of pharmaceutical sciences

authors： Hsu HC,Lu HL,Chan KK

更新日期：1995-06-01 00:00:00

abstract：:Deiodination of diatrizoic acid, an anionic radiopaque, was found to be catalyzed by Cu(II). Through a detailed study of o-iodobenzoic acid, a model compound, the copper-catalyzed SN1 mechanism was established based on observations of common ion, salt, and pH effects. Meta- and para-iodobenzoic acids were unreactive. ...

journal_title：Journal of pharmaceutical sciences

authors： Wang YC

更新日期：1980-06-01 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：:Anionic surfactants compromise skin's barrier function by damaging stratum corneum lipids and proteins. The objective of this study was to examine anionic surfactant-induced changes in the skin's polar and transcellular pathways and the resulting impact on surfactant penetration into the skin. Three anionic surfactant...

journal_title：Journal of pharmaceutical sciences

authors： Morris SAV,Ananthapadmanabhan KP,Kasting GB

更新日期：2019-11-01 00:00:00

abstract：:This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...

journal_title：Journal of pharmaceutical sciences

authors： Connolly BD,Le L,Patapoff TW,Cromwell MEM,Moore JMR,Lam P

更新日期：2015-12-01 00:00:00

abstract：:The deamidation of asparagine into aspartate and isoaspartate moieties is a major pathway for the chemical degradation of monoclonal antibodies (mAbs). It can affect the shelf life of a therapeutic antibody that is not formulated or stored appropriately. A new approach to detect deamidation using ion exchange chromato...

journal_title：Journal of pharmaceutical sciences

authors： Pace AL,Wong RL,Zhang YT,Kao YH,Wang YJ

更新日期：2013-06-01 00:00:00

abstract：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...

journal_title：Journal of pharmaceutical sciences

authors： Liebner R,Meyer M,Hey T,Winter G,Besheer A

更新日期：2015-02-01 00:00:00

abstract：:In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...

journal_title：Journal of pharmaceutical sciences

authors： Krueger AB,Carnell P,Carpenter JF

更新日期：2016-04-01 00:00:00