Particle Engineering for Enabling a Formulation Platform Suitable for Manufacturing Low-Dose Tablets by Direct Compression.

abstract：:The highly lipid soluble, free-base form of halofantrine (Hf base; approximately 50 mg/mL in triglyceride lipids), a highly lipophilic (calculated log P approximately 8.5) antimalarial, has recently been shown to undergo significant intestinal lymphatic transport (54% of administered dose) after postprandial administr...

journal_title：Journal of pharmaceutical sciences

authors： Khoo SM,Prankerd RJ,Edwards GA,Porter CJ,Charman WN

更新日期：2002-03-01 00:00:00

abstract：:Multidrug resistance (MDR) mediated by the overexpression of the drug efflux protein P-glycoprotein is one of the major obstacles to successful cancer chemotherapy. The development of safe and effective MDR-reversing agents is an important approach to addressing this problem clinically. In this study, we evaluated the...

journal_title：Journal of pharmaceutical sciences

authors： Liu R,Zhang Y,Chen Y,Qi J,Ren S,Xushi MY,Yang C,Zhu H,Xiong D

更新日期：2010-07-01 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：:Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher ...

journal_title：Journal of pharmaceutical sciences

authors： Bansal PC,Pitman IH,Higuchi T

更新日期：1981-08-01 00:00:00

abstract：:A representative series of hydroxy-5 beta-cholanyl-24-amines were tested both in vitro and in vivo with respect to their activity against the intestinal bacteria responsible for bile acid metabolism. For the in vitro studies, radiolabeled [14C]cholic acid was incubated with human stools both in aerobic and anaerobic c...

journal_title：Journal of pharmaceutical sciences

authors： Roda A,Bellini AM,Mencini E,Minutello A,Fini A,Guarneri M

更新日期：1992-03-01 00:00:00

abstract：:Unlike most organic compounds, both digoxin and digitoxin melted over a wide temperature range, with the widest range being 88 and 33 degrees for both compounds, respectively. Furthermore, the melting ranges varied markedly among several untriturated powders obtained from commercial sources and after recrystallization...

journal_title：Journal of pharmaceutical sciences

authors： Chiou WL,Kyle LE

更新日期：1979-10-01 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：:The germacranolide sesquiterpene lactones costunolide, parthenolide, and costunolide diepoxide were isolated from the leaves of Magnolia grandiflora L. Costunolide diepoxide might be, at least in part, an artifact derived from air oxidation of parthenolide. The root bark yielded only costunolide together with the two ...

journal_title：Journal of pharmaceutical sciences

authors： el-Feraly FS,Chan YM

更新日期：1978-03-01 00:00:00

abstract：:Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...

journal_title：Journal of pharmaceutical sciences

authors： Trapa PE,Belova E,Liras JL,Scott DO,Steyn SJ

更新日期：2016-02-01 00:00:00

abstract：:Econazole is a feasible alternative treatment in the management of fungal keratitis. Nevertheless, its low water solubility is considered the main limitation to the incorporation into ophthalmic formulations. In this work, econazole nitrate is solubilized by using cyclodextrins to achieve an optimum therapeutic concen...

journal_title：Journal of pharmaceutical sciences

authors： Díaz-Tomé V,Luaces-Rodríguez A,Silva-Rodríguez J,Blanco-Dorado S,García-Quintanilla L,Llovo-Taboada J,Blanco-Méndez J,García-Otero X,Varela-Fernández R,Herranz M,Gil-Martínez M,Lamas MJ,González-Barcia M,Otero-Espinar FJ,Fern

更新日期：2018-05-01 00:00:00

abstract：:A quantitative high-pressure liquid chromatographic method, using a reversed-phase column coupled to a fluorescence detector, was developed to determine salicylic acid in bulk aspirin and plain and buffered aspirin tablets. The aspirin was dissolved, filtered, and injected into the chromatograph; the fluorescence of t...

journal_title：Journal of pharmaceutical sciences

authors： Kirchhoefer RD,Juhl WE

更新日期：1980-05-01 00:00:00

abstract：:Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-i...

journal_title：Journal of pharmaceutical sciences

authors： Djekic L,Martinovic M,Stepanović-Petrović R,Tomić M,Micov A,Primorac M

更新日期：2015-08-01 00:00:00

abstract：:The objective of this study was to determine if a high Tg polymer (Eudragit(®) S100) could be used to stabilize amorphous domains of polyethylene oxide (PEO) and hence improve the stability of binary polymer systems containing celecoxib (CX). We propose a novel method of stabilizing the amorphous PEO solid dispersion ...

journal_title：Journal of pharmaceutical sciences

authors： Jones DS,Tian Y,Li S,Yu T,Abu-Diak OA,Andrews GP

更新日期：2016-10-01 00:00:00

abstract：:The pharmacokinetics and tissue distribution of methotrexate (MTX) were investigated following intra-articular injection of either MTX solution or controlled release MTX loaded microspheres in healthy rabbit joints. MTX solution or MTX loaded microspheres (size 30-100 mum) (10 mg MTX) was injected into the right knee ...

journal_title：Journal of pharmaceutical sciences

authors： Liang LS,Wong W,Burt HM

更新日期：2005-06-01 00:00:00

abstract：:Evidence is provided for the existence of a second discrete chemical form of meropenem at clinically relevant concentrations prepared from the marketed formulation of the drug. Proton and carbon-13 NMR spectra in D2O, coupled with tandem mass spectroscopy (MS/MS) and cross polarization/magic angle spinning (CP-MAS) NM...

journal_title：Journal of pharmaceutical sciences

authors： Almarsson O,Kaufman MJ,Stong JD,Wu Y,Mayr SM,Petrich MA,Williams JM

更新日期：1998-05-01 00:00:00

abstract：:A consistent account of the assumptions of the well-stirred perfusion limited model leads to the equation for the organ tissue that does not coincide with that often presented in books and papers. The difference in pharmacokinetic profiles calculated by the valid and the commonly used equations could be quite signific...

journal_title：Journal of pharmaceutical sciences

authors： Berezhkovskiy LM

更新日期：2010-01-01 00:00:00

abstract：:(14)N nuclear quadrupole resonance (NQR) in two known polymorphs of famotidine was measured. At room temperature, seven quadrupolar sets of transition frequencies (ν(+), ν(-), and ν(0)) corresponding to seven different nitrogen sites in the crystal structure of each of the two polymorphs were found. This confirms the ...

journal_title：Journal of pharmaceutical sciences

authors： Luźnik J,Pirnat J,Jazbinšek V,Lavrič Z,Žagar V,Srčič S,Seliger J,Trontelj Z

更新日期：2014-09-01 00:00:00

abstract：:Stability testing of morphine sulfate formulated with nonpareil sugar seeds (consisting of sucrose and starch) and fumaric acid revealed the formation of the three impurities 5-(hydroxymethyl)-2-furfural, 10-hydroxymorphine and 10-oxomorphine. 5-(Hydroxymethyl)-2-furfural was isolated via semipreparative HPLC utilizin...

journal_title：Journal of pharmaceutical sciences

authors： Kelly SS,Glynn PM,Madden SJ,Grayson DH

更新日期：2003-03-01 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：:A simple, reliable, and user friendly system was established to cultivate Caco-2 cell monolayer for epithelial transport studies. After an initial growth period of 1 week in a CO(2) incubator, Caco-2 cells were cultivated in an automated continuous perfusion system (Minucells and Minutissue, Germany). Medium was const...

journal_title：Journal of pharmaceutical sciences

authors： Masungi C,Borremans C,Willems B,Mensch J,Van Dijck A,Augustijns P,Brewster ME,Noppe M

更新日期：2004-10-01 00:00:00

abstract：:The kinetics of acetylation of alcohols by acetyl chloride and acetic anhydride, with N-methylimidazole as the catalyst, were studied in acetonitrile solution at 25 degrees; some measurements were also made with 4-dimethylaminopyridine as the catalyst. The acetic anhydride-N-methylimidazole system proceeds entirely by...

journal_title：Journal of pharmaceutical sciences

authors： Pandit NK,Connors KA

更新日期：1982-05-01 00:00:00

abstract：:The survival of Staphylococcus aureus was studied in 30 oral administration liquid medicaments (15 syrups and 15 solutions) to determine the effectiveness of the preservatives, the influence of the culture medium used in the enumeration of the surviving microorganisms, and the loss of the enzyme coagulase, phosphatase...

journal_title：Journal of pharmaceutical sciences

authors： Vivar C,de la Rosa C,Mosso A

更新日期：1993-02-01 00:00:00

abstract：:Chromatographic gel filtration matrixes used in various separation techniques are subject to microbial contamination. The need for a microbe-free column is critical when preparing materials that require a low or zero microbial count. This report proposes two alternative washing systems: 0.02 N HCl containing 0.81% NaC...

journal_title：Journal of pharmaceutical sciences

authors： Wen LF,Bohannon T,Crabb A,Mamaril F

更新日期：1980-02-01 00:00:00

abstract：:2,2'-Anhydro-1-beta-D-arabinofuranosylcytosine (I) is a more potent and less toxic antineoplastic agent than is cytarabine (1-beta-D-arabinofuranosylcytosine) (II). The anhydronucleoside (I) was found to be readily transformed by hydrogen peroxide into 2,2'-anhydro-5-hydroxy-1-beta-D-arabinofuranosylcytosine (III) by ...

journal_title：Journal of pharmaceutical sciences

authors： Kikugawa K

更新日期：1975-03-01 00:00:00

abstract：:In the present study, a previously described sulfenamide prodrug of a basic antidiabetic drug, metformin, was evaluated further. This sulfenamide prodrug was designed to improve the permeability and consequently the oral absorption and bioavailability (F) of the highly water-soluble metformin. Bioactivation of the pro...

journal_title：Journal of pharmaceutical sciences

authors： Huttunen KM,Leppänen J,Vepsäläinen J,Sirviö J,Laine K,Rautio J

更新日期：2012-08-01 00:00:00

abstract：:Abbott-232 is a chemically stable, highly water soluble non-hygroscopic compound selected for development as a potent uroselective alpha(1A) agonist. An anhydrate, a monohydrate, and an amorphous phase were isolated. The anhydrate was chosen for formulation development based on solid-state characterization. Excipients...

journal_title：Journal of pharmaceutical sciences

authors： Wardrop J,Law D,Qiu Y,Engh K,Faitsch L,Ling C

更新日期：2006-11-01 00:00:00

abstract：:Single-walled carbon nanotubes (SWCNTs) attract great interest in biomedical applications including drug and gene delivery. In this study, we developed a novel delivery system using SWCNTs associated with designed polycationic and amphiphilic peptides. Wrapping of SWCNTs with H-(-Lys-Trp-Lys-Gly-)7-OH [(KWKG)7] result...

journal_title：Journal of pharmaceutical sciences

authors： Ohta T,Hashida Y,Yamashita F,Hashida M

更新日期：2016-09-01 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

abstract：:Recent studies have clearly demonstrated that Fourier transform IR spectroscopy can be a powerful tool for the study of protein stabilization during freeze-drying and for optimizing approaches to prevent lyophilization-induced protein aggregation. The purpose of the current review is to provide an overview of these to...

journal_title：Journal of pharmaceutical sciences

authors： Dong A,Prestrelski SJ,Allison SD,Carpenter JF

更新日期：1995-04-01 00:00:00

abstract：:The kinetics and pathways for degradation of (+/-)-4'-ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride (HY-770; 1), a newly developed muscle-relaxing agent, and its analogues were studied in aqueous solution at 50 degrees C, ionic strength 0.5 M, and pH 8.0-12.0. Compound 1 and its four analogues followed ...

journal_title：Journal of pharmaceutical sciences

authors： Nagata O,Terasaki T,Yada E,Sato H,Tamai I,Tsuji A

更新日期：1989-01-01 00:00:00