Effect of the enantiomers of flurbiprofen, ibuprofen, and ketoprofen on intestinal permeability.

abstract：:A commercial dispersive Raman spectrometer operating at 785 nm with a CCD detector was used to acquire spectra of USP reference materials inside amber USP vials. The laser and collection beams were directed through the bottom of the vials, resulting in a 60% loss of signal. The Raman shift was calibrated with a 4-acet...

journal_title：Journal of pharmaceutical sciences

authors： McCreery RL,Horn AJ,Spencer J,Jefferson E

更新日期：1998-01-01 00:00:00

abstract：:Mixture response-surface methodology can be used as a technique to predict solubility in mixed solvent systems. The present report shows that if the intent is to predict solubility in nonideal solutions, mixture response-surface methodology is a better technique than one which assumes a particular mechanism to hold tr...

journal_title：Journal of pharmaceutical sciences

authors： Ochsner AB,Belloto RJ Jr,Sokoloski TD

更新日期：1985-02-01 00:00:00

abstract：:A new extraction-spectrophotometric method for the determination of hydralazine, based on its reaction with 2-hydroxy-1-naphthaldehyde at 25 degrees C, is described. The calibration curve was linear between 0.4 and 6 mg/mL of hydralazine. The molar absorbtivity of the product at 408 nm is 40,900 L.mol-1.cm-1. The meth...

journal_title：Journal of pharmaceutical sciences

authors： Mari-Buigues J,Mañes-Vinuesa J,Garcia-Domenech R,Pous-Miralles G

更新日期：1991-07-01 00:00:00

abstract：:The relationship between the lone tryptophan residue at position 214 and drug binding sites (Sites I and II) in human serum albumin (HSA) was studied by fluorescence energy transfer. The distance between the lone tryptophan residue and ligands bound to HSA was estimated by Förster's equation, taking into consideration...

journal_title：Journal of pharmaceutical sciences

authors： Kasai S,Horie T,Mizuma T,Awazu S

更新日期：1987-05-01 00:00:00

abstract：:We have previously reported the development of novel nanocapsules made of polyarginine (PArg) specifically designed for the delivery of small anticancer drugs into cells. Our goal, in this work, has been to investigate the potential of these nanocarriers for oral delivery of peptide anticancer drugs. To reach this obj...

journal_title：Journal of pharmaceutical sciences

authors： Lollo G,Gonzalez-Paredes A,Garcia-Fuentes M,Calvo P,Torres D,Alonso MJ

更新日期：2017-02-01 00:00:00

abstract：:Baclofen, a widely used antispastic agent, has been found to exist in two crystalline forms, the anhydrate and monohydrate. The aim of this study was (1) to identify and characterize these two solid phases of baclofen, and (2) to examine the processing-induced phase transformations associated with wet granulation of b...

journal_title：Journal of pharmaceutical sciences

authors： Mirza S,Miroshnyk I,Rantanen J,Aaltonen J,Harjula P,Kiljunen E,Heinämäki J,Yliruusi J

更新日期：2007-09-01 00:00:00

abstract：:Thymopentin (Tp5) was loaded in poly-butylcyanoacrylate (PBCA) nanoparticles (NP) in order to enhance the oral bioavailability of Tp5. PBCA-Tp5-NP was prepared by nanoprecipitation methods. Dialyzing membrane method was employed to examine the in vitro release of PBCA-Tp5-NP in PBS, and Tp5 samples in the release medi...

journal_title：Journal of pharmaceutical sciences

authors： He W,Jiang X,Zhang ZR

更新日期：2008-06-01 00:00:00

abstract：:The disposition kinetics of nicotine and cotinine enantiomers was determined in rabbits. The clearance of (R)-nicotine was similar to that of (S)-nicotine, but clearance of (R)-cotinine was twice that of (S)-cotinine. Fractional conversions of both enantiomers of nicotine to cotinine were approximately 50%. These resu...

journal_title：Journal of pharmaceutical sciences

authors： Jacob P 3rd,Benowitz NL,Copeland JR,Risner ME,Cone EJ

更新日期：1988-05-01 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：:The bioavailability of clofibric acid from formulations containing calcium clofibrate along and mixed with calcium carbonate (1:1 w/w) was compared to that from a standard clofibrate formulation in a crossover study in 12 human subjects. The 95% confidence intervals of bioavailability differences were such that they ...

journal_title：Journal of pharmaceutical sciences

authors： Taylor T,Chasseaud LF

更新日期：1977-11-01 00:00:00

abstract：:1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized. Compound 8 showed less potent beta-adrenergic blocking activity than betaxolol in an in vitro test with guinea pig tracheal ...

journal_title：Journal of pharmaceutical sciences

authors： Amlaiky N,Leclerc G

更新日期：1985-10-01 00:00:00

abstract：:An automated, stability-indicating, UV spectrophotometric assay for cefazolin is presented. The method employs a reaction with hydroxylamine and derives its stability-indicating power through comparison of reacted and unreacted aliquots of the sample. A double-probe sampling procedure is used. Good agreement with micr...

journal_title：Journal of pharmaceutical sciences

authors： Holl WW,O'Brien M,Filan J,Mazeika TR,Post A,Pitkin D,Actor P

更新日期：1975-07-01 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：:The placental and nonplacental clearances of metoclopramide were studied in nine chronically instrumented, near-term pregnant sheep using a two-compartment open model. Metoclopramide was administered to the ewe and fetus on separate occasions as an initial iv bolus loading dose followed by a constant-rate infusion, wi...

journal_title：Journal of pharmaceutical sciences

authors： Riggs KW,Rurak DW,Taylor SM,McErlane BA,McMorland GH,Axelson JE

更新日期：1990-12-01 00:00:00

abstract：:Though there is an advantage in using the higher solubility amorphous state in cases where low solubility limits absorption, physical instability poses a significant barrier limiting its use in solid oral dosage forms. Unlike chemical instability, where useful accelerated stability testing protocols are common, no met...

journal_title：Journal of pharmaceutical sciences

authors： Bhugra C,Pikal MJ

更新日期：2008-04-01 00:00:00

abstract：:Molecular interactions between iodine and disulfiram, clomethiazole, and tolnaftate were investigated by electron spectroscopy. Iodine forms charge transfer complexes with these molecules, with 1:1 stoichiometry and of the n-sigma type. The formation constants were compared with those obtained with antithyroid molecul...

journal_title：Journal of pharmaceutical sciences

authors： Buxeraud J,Absil AC,Raby C

更新日期：1984-12-01 00:00:00

abstract：:Application of ultrasound enhances transdermal transport of drugs (sonophoresis). The enhancement may result from enhanced diffusion due to ultrasound-induced skin alteration and/or from forced convection. To understand the relative roles played by these two mechanisms in low-frequency sonophoresis (LFS, 20 kHz), a th...

journal_title：Journal of pharmaceutical sciences

authors： Tang H,Mitragotri S,Blankschtein D,Langer R

更新日期：2001-05-01 00:00:00

abstract：:Colonic drug delivery is intended for local or systemic therapies. The lack of predictive in vitro or animal model leads to considerable time delays in colonic product development. The objective of this scintigraphic study was to provide "proof of concept" for a novel capsule-type colonic delivery system (Colon-Target...

journal_title：Journal of pharmaceutical sciences

authors： Ishibashi T,Pitcairn GR,Yoshino H,Mizobe M,Wilding IR

更新日期：1998-05-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:Tissue-specific ultrasonic enhancement can be used for the detection and characterization of atherosclerosis. We have previously demonstrated the generation of inherently echogenic (acoustically reflective) liposomes solely by varying lipid composition and controlling the method of production. In this study, echogenic...

journal_title：Journal of pharmaceutical sciences

authors： Demos SM,Onyüksel H,Gilbert J,Roth SI,Kane B,Jungblut P,Pinto JV,McPherson DD,Klegerman ME

更新日期：1997-02-01 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 present studies were undertaken to describe the dynamic nature of the degradation and absorption of insulin in the subcutaneous injection site and to develop agents which would stabilize this dosage form. [125I]Insulin with 0.2-U/kg of unlabeled insulin in 10 microliters of aqueous solution was injected subcutaneo...

journal_title：Journal of pharmaceutical sciences

authors： Hori R,Komada F,Okumura K

更新日期：1983-04-01 00:00:00

abstract：:An analysis of the disintegration-dissolution sequence of drug release from a tablet leads to a mathematical expression relating disintegration to the dissolution profile of the tablet and the dissolution rate of the primary drug particles in the tablet. The equation describing the disintegration of an acetaminophen t...

journal_title：Journal of pharmaceutical sciences

authors： Nelson KG,Wang LY

更新日期：1978-01-01 00:00:00

abstract：:Single crystal X-ray diffraction (SCXRD), powder X-ray diffraction (PXRD), and solid-state NMR (SSNMR) techniques are used to analyze the structures of two nonsolvated polymorphs of {4-(4-chloro-3-fluorophenyl)-2-[4-(methyloxy)phenyl]-1,3-thiazol-5-yl} acetic acid. These polymorphs are enantiotropically-related with a...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Katrincic LM,Long ST,Mueller RL,Carlton RA,Sun YT,Johnson MN,Copley RC,Light ME

更新日期：2008-11-01 00:00:00

abstract：:A roadmap for the selection of a pharmaceutical salt form for a development candidate is presented. The free base of the candidate did not have sufficient chemical stability for development. The initially selected salt form turned out to be undevelopable because it was unstable during scale-up synthesis and storage. T...

journal_title：Journal of pharmaceutical sciences

authors： He Y,Orton E,Yang D

更新日期：2018-01-01 00:00:00

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：:Bouvardin is a cyclic hexapeptide antitumor agent which undergoes two major microbial transformation reactions. Screening with 220 cultures revealed 17 different strains capable of producing O-desmethylbouvardin in good yield. O-Desmethylbouvardin was isolated and characterized from preparative scale incubations with ...

journal_title：Journal of pharmaceutical sciences

authors： Petroski RJ,Bates RB,Linz GS,Rosazza JP

更新日期：1983-11-01 00:00:00

abstract：:The reaction of UICEL-A/102, a cellulose II powder recently prepared from Avicel(R) PH-102 by treatment with an aqueous sodium hydroxide solution, with glutaraldehyde in 0.01 N HCl has been investigated to improve its binder properties, without adversely affecting the rapid disintegration characteristic. The results s...

journal_title：Journal of pharmaceutical sciences

authors： de la Luz Reus Medina M,Kumar V

更新日期：2007-02-01 00:00:00

abstract：:Quality-by-design (QbD) is a systematic approach to drug development, which begins with predefined objectives, and uses science and risk management approaches to gain product and process understanding and ultimately process control. The concept of QbD can be extended to analytical methods. QbD mandates the definition ...

journal_title：Journal of pharmaceutical sciences

authors： Vogt FG,Kord AS

更新日期：2011-03-01 00:00:00

abstract：:A new polymorphic form of Alprazolam (Xanax), 8-chloro-1-methyl-6-phenyl-4H-[1,2,4]triazolo-[4,3-alpha][1,4]benzodiazepine, C(17)H(13)ClN(4), has been investigated by means of X-ray powder diffraction (XRPD), single crystal X-ray diffraction, and differential scanning calorimetry (DSC). This polymorphic form (form III...

journal_title：Journal of pharmaceutical sciences

authors： de Armas HN,Peeters OM,Van den Mooter G,Blaton N

更新日期：2007-05-01 00:00:00