Water/n-octanol partition coefficients of 1,2-dithiole-3-thiones.

abstract：:Interest in the 5-, 6-, and 7-trifluoromethyl-substituted 2,3-bis(4-methoxyphenyl)indoles as potent, orally active anti-inflammatory agents required a method for their determination in serum, urine, and feces to permit studies of their absorption, metabolism, and excretion. A simple, rapid, sensitive, and specific pro...

journal_title：Journal of pharmaceutical sciences

authors： Kaiser DG,Liggett WF,Forist AA

更新日期：1976-12-01 00:00:00

abstract：:The pharmaceutical preparation, chromatography, and biological distribution of a series of new chemical analogs of palmitic acid and diethylenetriaminepentaacetic acid, ethylenediaminetetraacetic acid, or diethylenetriamine are described. The biological distribution in rabbits 30 min after intravenous administration o...

journal_title：Journal of pharmaceutical sciences

authors： Karesh SM,Eckelman WC,Reba RC

更新日期：1977-02-01 00:00:00

abstract：:Brain cancers are among the most lethal tumors due to their rapid development and poor prognosis. Despite the existing potential of novel therapeutic strategies for the treatment of brain cancer, the major remaining challenge associated with clinical translation is the lack of effective and safe delivery strategies to...

journal_title：Journal of pharmaceutical sciences

authors： Guo J,Schlich M,Cryan JF,O'Driscoll CM

更新日期：2017-12-01 00:00:00

abstract：:A study of the pH of saliva produced by humans sucking hard candy lozenges containing zinc gluconate and citric acid demonstrated the probability that the formulation delivered an insignificant amount of the contained zinc as Zn2+. This could account for the negative results of several clinical studies of this lozenge...

journal_title：Journal of pharmaceutical sciences

authors： Zarembo JE,Godfrey JC,Godfrey NJ

更新日期：1992-02-01 00:00:00

abstract：:Simulated intestinal media (SIM) containing bile salt (BS) and phospholipids (PL) with and without medium chain lipolytic products (MC-LP) or long chain lipolytic products (LC-LP) were developed to study the solubility of seocalcitol. Both MC-LP and LC-LP were studied in order to investigate the influence of fatty aci...

journal_title：Journal of pharmaceutical sciences

authors： Grove M,Pedersen GP,Nielsen JL,Müllertz A

更新日期：2005-08-01 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 crossover experiment was utilized to compare the pharmacokinetics of a 1-g dose of cephalexin tablets, cephalexin capsules, or cephradine capsules in nine normal human volunteers. These antibiotics were administered as three formulations: two 500-mg capsulin every 6 hr for five doses, and one 1000-mg tablet of cepha...

journal_title：Journal of pharmaceutical sciences

authors： Finkelstein E,Quintiliani R,Lee R,Bracci A,Nightingale CH

更新日期：1978-10-01 00:00:00

abstract：:Poor water solubility leads to low dissolution rate and consequently, it can limit bioavailability. Solid dispersions, where the drug is dispersed into an inert, hydrophilic polymer matrix can enhance drug dissolution. Solid dispersions were prepared using phenacetin and phenylbutazone as model drugs with polyethylene...

journal_title：Journal of pharmaceutical sciences

authors： Khan S,Batchelor H,Hanson P,Perrie Y,Mohammed AR

更新日期：2011-10-01 00:00:00

abstract：:A GLC method for the determination of procainamide in biological fluids is presented. By using a dipropyl analog of procainamide as an internal standard, both compounds can be chromatographed directly, yielding linear calibration curves and a sensitivity that allows quantitative determination of concentrations as low ...

journal_title：Journal of pharmaceutical sciences

authors： Simons KJ,Levy RH

更新日期：1975-12-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 00:00:00

abstract：:The polymorphism of rac-5,6-diisobutyryloxy-2-methylamino-1,2,3,4-tetrahydro-naphthalene hydrochloride (CHF 1035) was investigated. Three different crystal forms (Form I, Form II, and Form III) were obtained by recrystallization procedures from common organic solvents. The polymorphs were characterized by Raman and ca...

journal_title：Journal of pharmaceutical sciences

authors： Giordano F,Rossi A,Moyano JR,Gazzaniga A,Massarotti V,Bini M,Capsoni D,Peveri T,Redenti E,Carima L,Dagli Alberi M,Zanol M

更新日期：2001-08-01 00:00:00

abstract：:An aqueous solution of trimedoxime bromide, atropine, and benactyzine hydrochloride was formulated to have maximum stability as an antidote in organophosphorus poisoning. The stability of the mixture in glass and plastic cartridges was determined. Glass cartridges were more desirable than plastic; there was less vapor...

journal_title：Journal of pharmaceutical sciences

authors： Zvirblis P,Ellin RI

更新日期：1982-03-01 00:00:00

abstract：:To gain further insight into the effect of molecular mobility on the crystallization rate of amorphous drugs, the mean relaxation times of amorphous nifedipine and phenobarbital were calculated based on the Adam-Gibbs-Vogel (AGV) equation, using the parameters D, T(0), and T(f), derived from the heating rate dependenc...

journal_title：Journal of pharmaceutical sciences

authors： Aso Y,Yoshioka S,Kojima S

更新日期：2001-06-01 00:00:00

abstract：:The health effects of green tea are associated with catechins: (-)-epigallocatechin-3-O-gallate (EGCG), (-)-epigallocatechin, (-)-epicatechin-3-O-gallate, and (-)-epicatechin. An understanding of compound absorption, distribution, metabolism, excretion, and toxicity characteristics is essential for explaining its biol...

journal_title：Journal of pharmaceutical sciences

authors： Matić S,Jadrijević-Mladar Takač M,Barbarić M,Lučić B,Gall Trošelj K,Stepanić V

更新日期：2018-11-01 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：:Mathematical relationships describing the delivery of drug to a target organ after intra-arterial, intravenous, and oral administration are presented. This discussion clearly demonstrates that administration into a blood vessel leading to the target organ often is superior to intravenous administration. However, this ...

journal_title：Journal of pharmaceutical sciences

authors： Oie S,Huang JD

更新日期：1981-12-01 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：:Apparent micellar molecular weights were determined with the antibiotic fusidate sodium by ultracentrifugation in varying counterion concentrations (Na+). The effects of buffer salts, pH, sodium chloride concentration, and drug concentration were studied. The results strongly support the concept of the formation of pr...

journal_title：Journal of pharmaceutical sciences

authors： Richard AJ

更新日期：1975-05-01 00:00:00

abstract：:The intracellular delivery of small interfering RNA (siRNA) is a therapeutic strategy to transiently block gene expression. Two silencing RNA strategies utilize either synthetic double stranded RNA or plasmid DNA encoding a short hairpin RNA (shRNA). In the present study, we have quantitatively compared the potency of...

journal_title：Journal of pharmaceutical sciences

authors： McAnuff MA,Rettig GR,Rice KG

更新日期：2007-11-01 00:00:00

abstract：:Two polymorphs of the 1:1 fumarate salt of 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester, developed for the treatment of cognitive symptoms of schizophrenia and Alzheimer disease, have been characterized. The 2 crystal structures have been solved, and their phase relationships have been establish...

journal_title：Journal of pharmaceutical sciences

authors： Robert B,Perrin MA,Barrio M,Tamarit JL,Coquerel G,Ceolin R,Rietveld IB

更新日期：2016-01-01 00:00:00

abstract：:Regional permeability coefficients of 19 drugs with different physicochemical properties were determined using excised segments from three regions of rat intestine: jejunum, ileum, and colon. The results are discussed in relation to the characteristics of the drug, i.e., MW (range 113-1071 Da), pKa, log D (octanol/wat...

journal_title：Journal of pharmaceutical sciences

authors： Ungell AL,Nylander S,Bergstrand S,Sjöberg A,Lennernäs H

更新日期：1998-03-01 00:00:00

abstract：:Pepsin adsorbed on gibbsite or boehmite, non-acid-reactive forms of aluminum hydroxide, had a significantly lower activity than pepsin in solution. IR and desorbed pepsin activity studies showed that the reduced activity of adsorbed pepsin was not due to denaturation of pepsin on adsorption. Steric occlusion of the ac...

journal_title：Journal of pharmaceutical sciences

authors： Sepelyak RJ,Feldkamp JR,Regnier FE,White JL,Hem SL

更新日期：1984-11-01 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：:Plasma and various organ concentrations of canrenone, canrenoate, and total 3H-activity were measured following single doses of 20 mg of 3H-canrenoate/kg iv to rabbits. Organs studied included heart, lungs, brain, kidneys, liver, adrenal glands, and spleen. Canrenoate was shown to be in rapid equilibrium with canrenon...

journal_title：Journal of pharmaceutical sciences

authors： Finn AM,Brown R,Sadée W

更新日期：1977-02-01 00:00:00

abstract：:Ethyl, n-dodecyl, and n-hexadecyl esters of urocanic acid (4-imidazoleacrylic acid) were prepared from 4-imidazolecarboxaldehyde in satisfactory yields via the Wittig reaction. ...

journal_title：Journal of pharmaceutical sciences

authors： Honda K,Nishijima Y

更新日期：1981-01-01 00:00:00

abstract：:Optical crystallographic data were determined on a variety of newer USP drugs for which data had not been previously obtained. The ingredients in an unknown sample can be identified by polarized light microscopy by mounting small amounts of the material in successive specific refractive index liquids and determining r...

journal_title：Journal of pharmaceutical sciences

authors： Jordan DD

更新日期：1993-12-01 00:00:00

abstract：:Some coated aspirin tablet formulations were evaluated by relating their properties to disintegrating force development patterns. The treatment of disintegrating force-time curves was effected using the Weibull distribution as proposed for dissolution. Such parameters as the maximum disintegrating force developed, the...

journal_title：Journal of pharmaceutical sciences

authors： Colombo P,Conte U,Caramella C,Geddo M,La Manna A

更新日期：1984-05-01 00:00:00

abstract：:A number of arylidene derivatives of alicyclic ketones and some corresponding oximes, oxime esters, and related compounds were prepared as candidate cytotoxic agents. All of the compounds were evaluated against murine L1210 lymphoid leukemia cells. In general, cytotoxicity was greatest with the alpha,beta-unsaturated ...

journal_title：Journal of pharmaceutical sciences

authors： Dimmock JR,Sidhu KK,Chen M,Li J,Quail JW,Allen TM,Kao GY

更新日期：1994-06-01 00:00:00

abstract：:This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

journal_title：Journal of pharmaceutical sciences

authors： Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

更新日期：2009-01-01 00:00:00

abstract：:There is a recognized need for new approaches to understand unit operations with pharmaceutical relevance. A method for analyzing complex interactions in experimental data is introduced. Higher-order interactions do exist between process parameters, which complicate the interpretation of experimental results. In this ...

journal_title：Journal of pharmaceutical sciences

authors： Naelapää K,Allesø M,Kristensen HG,Bro R,Rantanen J,Bertelsen P

更新日期：2009-05-01 00:00:00