In the search for new anticancer drugs. 28. Synthesis and evaluation of highly active aminoxyl labeled amino acid derivatives containing the [N'-(2-chloroethyl)-N'-nitrosoamino]carbonyl group.

abstract：:Ascorbic acid has a unique role in the prevention and treatment of a large number of chronic diseases, including skin disorders but it can hardly penetrate the skin due to its solubility in water and its high instability. This study explored the formation of phosphatidylcholine-based vesicles upon addition of ascorbyl...

journal_title：Journal of pharmaceutical sciences

authors： Risaliti L,Ambrosi M,Calamante M,Bergonzi MC,Lo Nostro P,Bilia AR

更新日期：2020-10-01 00:00:00

abstract：:Quercetin had been shown to be effective in the management of arthritis. However, bioavailability of quercetin is a concern for such treatment. This work aims at the development of intra-articular drug delivery system by controlled release of quercetin (loaded in microspheres) for the management of rheumatoid arthriti...

journal_title：Journal of pharmaceutical sciences

authors： Natarajan V,Krithica N,Madhan B,Sehgal PK

更新日期：2011-01-01 00:00:00

abstract：:Injectable controlled-release formulations are of increasing interest for the treatment of chronic diseases. This study aims to develop and characterize a polymeric matrix for intramuscular or subcutaneous injection, consisting of two biocompatible polymers, particularly suitable for formulating poorly soluble drugs. ...

journal_title：Journal of pharmaceutical sciences

authors： Meeus J,Chen X,Scurr DJ,Ciarnelli V,Amssoms K,Roberts CJ,Davies MC,van Den Mooter G

更新日期：2012-09-01 00:00:00

abstract：:Corneal permeability data taken from the literature were analyzed for possible quantitative relationships with physicochemical properties. Although a parabolic relationship was obtained with good correlation between lipophilicity, as expressed by the 1-octanol-water partition coefficients, log Poctanol (or the distrib...

journal_title：Journal of pharmaceutical sciences

authors： Yoshida F,Topliss JG

更新日期：1996-08-01 00:00:00

abstract：:It is shown, using oxalic acid dihydrate as a model, that nonisothermal recrystallization of powders gives rise to particle size distributions which approach log-normality in many cases. The number of particles formed is, primarily, a function of the nucleation rate constants and the particle size distribution, i.e., ...

journal_title：Journal of pharmaceutical sciences

authors： Carstensen JT,Rodriguez-Hornedo N

更新日期：1985-12-01 00:00:00

abstract：:A new quantitative GLC method for analysis of lidamidine hydrochloride (I) was developed. The method was based on derivatization of I to 1-(2,6-dimethylphenyl)-4-methylamino-dihydro-1,3,5-triazin-2-one (II) using dimethylformamide dimethylacetal reagent. Compound II was synthesized and characterized by IR, NMR, mass s...

journal_title：Journal of pharmaceutical sciences

authors： Won CM,Zalipsky JJ,Patel DM,Grim WM

更新日期：1982-03-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:A heparin derivative sufficiently lipophilic to be bound to plastics, forming blood-compatible supports, or to be used as an anticoagulant by transdermal or oral routes would be of great pharmaceutical interest. For such applications, the functional groups within heparin's antithrombin III binding site, responsible fo...

journal_title：Journal of pharmaceutical sciences

authors： Liu J,Pervin A,Gallo CM,Desai UR,Van Gorp CL,Linhardt RJ

更新日期：1994-07-01 00:00:00

abstract：:The use of intravascular tyrosine (TYR) to enhance catecholamine release in hemorrhagic shock and other cardiovascular diseases, or as a constituent of nutrient mixtures used for total parenteral nutrition, is limited by the unusually poor solubility of the amino acid in water. We have thus examined the ability of var...

journal_title：Journal of pharmaceutical sciences

authors： Maher TJ,Kiritsy PJ,Moya-Huff FA,Casacci F,De Marchi F,Wurtman RJ

更新日期：1990-08-01 00:00:00

abstract：:Lipids were extracted from human stratum corneum and the remaining corneocytes were reaggregated with different lyotropic liquid crystals. Water transport through the reaggregated stratum corneum was determined using a diffusion chamber according to Smith and Blank. The permeability constant for the reaggregated strat...

journal_title：Journal of pharmaceutical sciences

authors： Kayali I,Suhery T,Friberg SE,Simion FA,Rhein LD

更新日期：1991-05-01 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：:Angiogenesis, the sprouting of capillaries from preexisting ones, is essential for the sustained growth of solid tumors. In this study, we used SU5416, a hydrophobic molecule with potent tyrosine kinase inhibitor of type 2 receptor for vascular endothelial growth factor (VEGF), as PEGylated emulsion (SU5416-PE), and e...

journal_title：Journal of pharmaceutical sciences

authors： Ogawara K,Abe S,Un K,Yoshizawa Y,Kimura T,Higaki K

更新日期：2014-08-01 00:00:00

abstract：:A method is described for screening compounds that inhibit crystallization in solution to enable more accurate measurement of amorphous drug solubility. Three polymers [polyvinylpyrrolidone, hydroxypropyl methylcellulose, and hydroxypropyl methylcellulose acetate succinate (HPMCAS)] were screened for their ability to ...

journal_title：Journal of pharmaceutical sciences

authors： Murdande SB,Pikal MJ,Shanker RM,Bogner RH

更新日期：2011-10-01 00:00:00

abstract：:A series of gem-cichlorocyclopropyl and cyclopropyl analogs of stilbene congeners was synthesized and examined for estrogenic and antiestrogenic activity using the uterotropic assay in the immature mouse. The relative receptor affinity in vitro was determined by measuring [3H]estradiol displacement from the rat uterin...

journal_title：Journal of pharmaceutical sciences

authors： Stobaugh JF,Magarian RA,Pento JT

更新日期：1982-10-01 00:00:00

abstract：:The extent of formation of solasodiene from solasodine upon treatment with hydrochloric acid under various conditions was determined. The diene formed was assayed by using the characteristic extinction at 236 nm. Diene formation was effected by the acid concentration and the boiling point of the solvent used. Optimal ...

journal_title：Journal of pharmaceutical sciences

authors： Segal R,Breuer A,Milo-Goldzweig I

更新日期：1978-08-01 00:00:00

abstract：:During stability studies at high temperature (70 degrees C) and low relative humidity ( approximately 0%), the recovery of an asparagine containing hexapeptide (VYPNGA) and its known deamidation products from solid polyvinylpyrrolidone (PVP) matrices was incomplete. To determine the causes of this mass loss, formulati...

journal_title：Journal of pharmaceutical sciences

authors： D'Souza AJ,Schowen RL,Borchardt RT,Salsbury JS,Munson EJ,Topp EM

更新日期：2003-03-01 00:00:00

abstract：:The hydrophobic substituent parameter for a system of meta- and para-disubstituted benzenes, XC6H4Y, defined as pi X/PhY = log PXC6H4Y - log PC6H5Y, where P is the octanol-water partition coefficient and X and Y are variable and fixed substituents, respectively, varies from one system to another, according to the vari...

journal_title：Journal of pharmaceutical sciences

authors： Fujita T

更新日期：1983-03-01 00:00:00

abstract：:Neural networks (NN) are computational systems implemented in software or hardware that attempt to simulate the neurological processing abilities of biological systems. A synopsis is presented of the operational characteristics, structures, and applications of NN. The NN technology has primarily been aimed at recognit...

journal_title：Journal of pharmaceutical sciences

authors： Veng-Pedersen P,Modi NB

更新日期：1993-09-01 00:00:00

abstract：:The thiazide diuretic chlorothiazide is poorly metabolized, and is predominantly excreted via the kidneys. We have previously shown that chlorothiazide is transported by ATP-binding cassette transporter G2, suggesting a potential role for this transporter in apical efflux of chlorothiazide in the kidney. However, beca...

journal_title：Journal of pharmaceutical sciences

authors： Juhász V,Beéry E,Nagy Z,Bui A,Molnár E,Zolnerciks JK,Magnan R,Jani M,Krajcsi P

更新日期：2013-05-01 00:00:00

abstract：:The applicability of bioavailability assessment at quasi- and nonsteady state is illustrated with data from a study comparing two formulations of amitriptyline hydrochloride in humans. Relative bioavailability as a function of the observed mean plasma concentrations may be expressed in closed form, provided the affect...

journal_title：Journal of pharmaceutical sciences

authors： Bondi JV,Hucker HB,Yeh KC,Kwan KC

更新日期：1976-11-01 00:00:00

abstract：:Determining the aggregation propensity of protein-based biotherapeutics is an important step in the drug development process. Typically, a great deal of data collected over a large period of time is needed to estimate the aggregation propensity of biotherapeutics. Thus, candidates cannot be screened early on for aggre...

journal_title：Journal of pharmaceutical sciences

authors： Lauer TM,Agrawal NJ,Chennamsetty N,Egodage K,Helk B,Trout BL

更新日期：2012-01-01 00:00:00

abstract：:The promoting efficacies of N-acyl derivatives of amino acids on the rectal absorption of sodium ampicillin were investigated using the rat rectal loop technique. N-Acyl derivatives with longer carbon chains in the acyl moiety showed a greater promoting potency. The promoting potencies of N-acyl derivatives of phenylg...

journal_title：Journal of pharmaceutical sciences

authors： Wu WM,Murakami T,Higashi Y,Yata N

更新日期：1987-07-01 00:00:00

abstract：:Clinical lots of recombinant human platelet-activating factor acetylhydrolase (rhPAF-AH) were prepared in a lyophilized formulation. After reconstitution with sterile water for injection to form an aqueous solution (10 mM sodium citrate, 7.5 w/v% sucrose, and 0.1 w/v% Pluronic-F68, pH 6.5), a few visible, slowly growi...

journal_title：Journal of pharmaceutical sciences

authors： Chi EY,Weickmann J,Carpenter JF,Manning MC,Randolph TW

更新日期：2005-02-01 00:00:00

abstract：:Cosalane is a potent inhibitor of HIV replication with multiple sites of action. The purposes of this study were to (a) determine the extent and nature of cosalane binding to mucin, alpha(1)-acid glycoprotein (AAG), plasma, and human (HSA) and bovine serum (BSA) albumin, and (b) determine the primary site(s) of cosala...

journal_title：Journal of pharmaceutical sciences

authors： Kuchimanchi KR,Ahmed MS,Johnston TP,Mitra AK

更新日期：2001-05-01 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：: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：:The reaction kinetics of blue tetrazolium with selected arylhydrazines were investigated under pseudo-first-order conditions. The reaction rate constants were obtained at various temperatures, and the enthalpy (8.4-11.2 kcal/mole) and entropy (-38--45 eu) of activations were calculated. A Hammett plot yielded a straig...

journal_title：Journal of pharmaceutical sciences

authors： Biehl ER,Wooten R,Kenner CT,Graham RE

更新日期：1978-07-01 00:00:00

abstract：:A titration method was developed for the determination of diphenhydramine, quinine, neostigmine, sparteine, strychnine, homatropine, atropine, physostigmine, and procaine in aqueous solution. Tetraphenylborate was used as a titrant with tetrabromophenolphthalein ethyl ester as an indicator in the presence of organic s...

journal_title：Journal of pharmaceutical sciences

authors： Tsubouchi M,Mitsushio H,Yamasaki N,Matsuoka K

更新日期：1981-11-01 00:00:00

abstract：:With the introduction of Quality by Design (QbD) to the pharmaceutical industry, there has been an increased focus on understanding the nature of particles and composites, with the aim of understanding and modeling how they interact in complex systems, leading to robust dosage forms. Particle characterization tools ha...

journal_title：Journal of pharmaceutical sciences

authors： Gamble JF,Tobyn M,Hamey R

更新日期：2015-05-01 00:00:00

abstract：:A mathematical model based on convective diffusion was developed to describe the rate of dissolution form the surface of a compressed compact. Experimental studies were carried out to test the model. The basic experimental apparatus consisted of a modified rotating-filter-stationary basket dissolution test apparatus. ...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Shah AC

更新日期：1975-04-01 00:00:00