Synthesis and evaluation of 3-halocyclophosphamides and analogous compounds as novel anticancer "pro-prodrugs".

abstract：:This study compares one of the previously studied formulations with commercial amoxicillin capsules. The results indicate that the percentage of the dose absorbed is similar in both formulations; nevertheless, the amoxicillin capsules present a higher absorption rate. The in vivo--in vitro correlations in terms of res...

journal_title：Journal of pharmaceutical sciences

authors： Llabrés M,Vila JL,Martínez-Pacheco R

更新日期：1982-08-01 00:00:00

abstract：:Dextran sulfate samples from different sources were examined by 1H and 13C NMR spectroscopy to differentiate the samples on the basis of extent and sites of sulfation. The anomeric (H-1) signal proved to be a good indicator ranging from no sulfation (as in dextran) to virtually complete sulfation at positions 2 and 3,...

journal_title：Journal of pharmaceutical sciences

authors： Neville GA,Rochon P,Rej RN,Perlin AS

更新日期：1991-03-01 00:00:00

abstract：:A colorimetric determination of chlorhexidine is described. The method is based on the formation of a yellow complex between the drug and bromcresol green. The absorption peak of this complex, extracted by chloroform, is at 410 nm, and linear response is obtained from 2.5 to 30 micrograms of chlorhexidine/ml. The accu...

journal_title：Journal of pharmaceutical sciences

authors： Andermann G,Buhler MO,Erhart M

更新日期：1980-02-01 00:00:00

abstract：:Midazolam (MDZ) is a benzodiazepine commonly administered in preanesthesia of children by oral or by sublingual routes. To mask its bitter taste and enhance its aqueous solubility, we already developed a 0.2% (w/v) MDZ oral solution containing γ-cyclodextrin (γ-CD), which proves to be better accepted by children in pe...

journal_title：Journal of pharmaceutical sciences

authors： Mathiron D,Marçon F,Dubaele JM,Cailleu D,Pilard S,Djedaïni-Pilard F

更新日期：2013-07-01 00:00:00

abstract：:The aim was to study a new method of dissolution in vitro, the "Bio-Dis" apparatus, and to compare it with the classical rotating bottle method. Several theophylline controlled-release drug dosage forms were studied. Dissolution testing was performed in increasing pH in standard conditions and after treatment with pea...

journal_title：Journal of pharmaceutical sciences

authors： Esbelin B,Beyssac E,Aiache JM,Shiu GK,Skelly JP

更新日期：1991-10-01 00:00:00

abstract：:The purpose of this work was to investigate the self-associating behavior observed in high concentration monoclonal antibody (MAb1) solutions at pH 6.0. Zeta potential measurements over the pH range (4.0-9.0) showed lower net charges present on the molecule at pH 6.0 and 7.0. The point of zero charge or crossover from...

journal_title：Journal of pharmaceutical sciences

authors： Yadav S,Liu J,Shire SJ,Kalonia DS

更新日期：2010-03-01 00:00:00

abstract：:Drug stability studies are expensive and time consuming. Multiple batches are studied to ensure that a product will consistently remain within specifications for its entire expiration dating period. Some of these studies involve the same drug products in similar packages or in multiple strengths. Application of sound ...

journal_title：Journal of pharmaceutical sciences

authors： Fairweather WR,Lin TY,Kelly R

更新日期：1995-11-01 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：:The assessment of provenance of heparin is becoming a major concern for the pharmaceutical industry and its regulatory bodies. Batch-specific [carbon (δ(13) C), nitrogen (δ(15) N), oxygen (δ(18) O), sulfur (δ(34) S), and hydrogen (δD)] stable isotopic compositions of five different animal-derived heparins were perform...

journal_title：Journal of pharmaceutical sciences

authors： Jasper JP,Zhang F,Poe RB,Linhardt RJ

更新日期：2015-02-01 00:00:00

abstract：:This study determines the enhancing effects of 2-n-nonyl-1,3-dioxolane on the penetration of econazole, an antifungal drug, into the deeper layers of the human nail where fungal infection resides. Aliquots (10 microL) of Econail lacquer formulation containing 0.45 mg of [(14)C]-econazole with 18% 2-n-nonyl-1,3-dioxola...

journal_title：Journal of pharmaceutical sciences

authors： Hui X,Chan TC,Barbadillo S,Lee C,Maibach HI,Wester RC

更新日期：2003-01-01 00:00:00

abstract：:A method is presented for determining the equilibrium solubility of a drug in a solid polymer at or near room temperature, which represents a typical storage temperature. The method is based on a thermodynamic model to calculate the Gibbs energy change ΔG(SS) associated with forming a binary drug-polymer solid solutio...

journal_title：Journal of pharmaceutical sciences

authors： Bellantone RA,Patel P,Sandhu H,Choi DS,Singhal D,Chokshi H,Malick AW,Shah N

更新日期：2012-12-01 00:00:00

abstract：:A convenient and sensitive analytical method for determination of plasma morphine and its metabolites in cancer patients was established using HPLC with a column-switching technique. Sample plasma which has been deproteinized with trichloroacetic acid is injected onto a precolumn, then the compounds of interest are pr...

journal_title：Journal of pharmaceutical sciences

authors： Konishi M,Hashimoto H

更新日期：1990-05-01 00:00:00

abstract：:This study is to prepare and evaluate Pluronics-modified mixed micelle (MM) to deliver polyphenolic myricetin (MYR) across the blood-brain barrier. MYR has been proven to be an effective anticancer agent against glioblastoma cells in our previous studies. However, the poor solubility of MYR limits its access to the br...

journal_title：Journal of pharmaceutical sciences

authors： Wang G,Wang JJ,Li F,To SS

更新日期：2016-04-01 00:00:00

abstract：:The pharmacologically active compound (33% reduction in rabbit intraocular pressure recovery rate assay) 1-ethyl-6-fluoro-1,2,3,4-tetrahydroquinoline (MC4), which showed ocular hypotensive action and had optimum physicochemical properties, was characterized for its ocular absorption and distribution properties to bett...

journal_title：Journal of pharmaceutical sciences

authors： Pamulapati CR,Schoenwald RD

更新日期：2011-12-01 00:00:00

abstract：:An isothermal chromatographic (GC) method employing an SE-30 column and flame-ionization detection has been developed for the simultaneous assay of methyl, ethyl, propyl, and butyl 4-hydroxybenzoates and 4-hydroxybenzoic acid in liquid antacid formulations. The method, which uses a silica column chromatographic cleanu...

journal_title：Journal of pharmaceutical sciences

authors： Schieffer GW,Palermo PJ,Pollard-Walker S

更新日期：1984-01-01 00:00:00

abstract：:Application of low-frequency ultrasound has been shown to enhance transdermal transport of drugs (low-frequency sonophoresis). In this paper, we show that the efficacy of low-frequency ultrasound in enhancing transdermal transport can be further increased by its combination with sodium lauryl sulfate (SLS), a well-kno...

journal_title：Journal of pharmaceutical sciences

authors： Mitragotri S,Ray D,Farrell J,Tang H,Yu B,Kost J,Blankschtein D,Langer R

更新日期：2000-07-01 00:00:00

abstract：:Systematic structural modifications were performed on the natural sesquiterpene lactone tenulin to define those groupings essential to, or significant in, its in vivo antitumor activity. Accordingly, the following tenulin analogs were prepared: dihydrotenulin, 2,3-epoxytenulin, isotenulin, dihydroisotenulin, 2,3-epoxy...

journal_title：Journal of pharmaceutical sciences

authors： Waddell TG,Austin AM,Cochran JW,Gerhart KG,Hall IH,Lee KH

更新日期：1979-06-01 00:00:00

abstract：:The plasma concentrations and urinary excretions of bisoprolol enantiomers in four Japanese male healthy volunteers after a single oral administration of 20 mg of racemic bisoprolol were evaluated. The AUC(infinity) and elimination half-life of (S)-(-)-bisoprolol were slightly larger than those of (R)-(+)-bisoprolol i...

journal_title：Journal of pharmaceutical sciences

authors： Horikiri Y,Suzuki T,Mizobe M

更新日期：1998-03-01 00:00:00

abstract：:The effect of dietary polyphenols on the intestinal glucuronidation and absorption of a model phenolic drug, alpha-naphthol (alpha-NA), was studied in isolated rat small intestine. (-)-Epicatechin significantly inhibited the glucuronidation of alpha-NA. Chrysin, (-)-epigallocatechin galleate (EGCG), and quercetin decr...

journal_title：Journal of pharmaceutical sciences

authors： Mizuma T,Awazu S

更新日期：2004-09-01 00:00:00

abstract：:It is hypothesized that ferrocene (FC)-loaded nanocarriers (FC-NCs) are safe label-free contrast agents for cochlear biodistribution study by transmission electron microscopy (TEM). To test this hypothesis, after engineering, the poly(epsilon-caprolactone)/polyglycolide NCs are tested for stability with various types ...

journal_title：Journal of pharmaceutical sciences

authors： Youm I,Musazzi UM,Gratton MA,Murowchick JB,Youan BC

更新日期：2016-10-01 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：:A high-performance liquid chromatographic method with spectrofluorometric detection has been developed for the analysis of a new substituted benzamide and its metabolite in body fluids. The detection was performed at 270 nm for excitation, and 370 nm for emission. The proposed technique is selective, reliable, and sen...

journal_title：Journal of pharmaceutical sciences

authors： Bressolle F,Bres J,Moulin A

更新日期：1990-06-01 00:00:00

abstract：:Vitamin E tocopherol polyethylene glycol succinate (TPGS) is a non-ionic surface active agent, known to enhance the bioavailability of lipophilic compounds via wettability, solubility, and in some cases permeability enhancement. MK-0536 is an anti-retroviral drug with poor wettability and solubility and a high dose. B...

journal_title：Journal of pharmaceutical sciences

authors： Tatavarti A,Kesisoglou F

更新日期：2015-11-01 00:00:00

abstract：:The combined clearance of endogenous 6β-hydroxycortisol and 6β-hydroxycortisone is suggested biomarker for in vivo cytochrome P450 3A (CYP3A) activity. We aimed to determine whether the combined clearance of these two markers together with information of biopharmaceutics classification system (BCS) of drugs could be u...

journal_title：Journal of pharmaceutical sciences

authors： Luo X,Zheng L,Cai N,Liu Q,Yang S,He X,Cheng Z

更新日期：2015-10-01 00:00:00

abstract：:The thermodynamic relationship between FI and FII of ethyl 4-aminobenzoate (benzocaine) has been investigated. Slurry conversion experiments show that the transition temperature below which FI is stable is located between 302 K-303 K (29 °C-30 °C). The polymorphs FI and FII have been characterised by infrared spectros...

journal_title：Journal of pharmaceutical sciences

authors： Cheuk D,Svärd M,Rasmuson ÅC

更新日期：2020-11-01 00:00:00

abstract：:Aggregation of therapeutic monoclonal antibodies has a potential risk of immunogenicity, requiring minimization of aggregate formation. We have developed a fitting formula for antibody aggregation at 40°C based on physicochemical parameters, including colloidal and conformational stabilities. An IgG1 monoclonal antibo...

journal_title：Journal of pharmaceutical sciences

authors： Oyama H,Koga H,Tadokoro T,Maenaka K,Shiota A,Yokoyama M,Noda M,Torisu T,Uchiyama S

更新日期：2020-01-01 00:00:00

abstract：:Nitroglycerin is rapidly lost from solution when incubated with red blood cells or whole blood. The assumption that the loss is enzymatic in nature may not be true, since no major metabolite is detected during this incubation. Explanation on the basis of a chemical reaction is also difficult, since the products of the...

journal_title：Journal of pharmaceutical sciences

authors： Sokoloski TD,Wu CC,Wu LS,Burkman AM

更新日期：1983-04-01 00:00:00

abstract：:The solvent-free melt electrospinning (MES) method was developed to prepare a drug delivery system with fast release of carvedilol (CAR), a drug with poor water solubility. To the authors knowledge, this is the first report for preparing drug-loaded melt electrospun fibers. Cationic methacrylate copolymer of Eudragit®...

journal_title：Journal of pharmaceutical sciences

authors： Nagy ZK,Balogh A,Drávavölgyi G,Ferguson J,Pataki H,Vajna B,Marosi G

更新日期：2013-02-01 00:00:00

abstract：:Two previously reported but unidentified phenylburazone degradation products were isolated from a tablet that was stored at 60 degrees for 203 days. The compounds, alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene and alpha-hydroxy-alpha-(N-phenylcarbamoyl)-N-caproylhydrazobenzene, were isolated by chromatography, ide...

journal_title：Journal of pharmaceutical sciences

authors： Matsui F,Robertson DL,Poirier MA,Lovering EG

更新日期：1980-04-01 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