Solvent influences on metastable polymorph lifetimes: real-time interconversions using energy dispersive X-ray diffractometry.

abstract：:The effect of calcium ions on the structure and stability of recombinant human DNase I (rhDNase) in the aqueous and solid (lyophilized) states was investigated. Fourier transform infrared (FTIR) spectroscopy was used to examine the overall secondary structure, while chemical stability was monitored in terms of deamida...

journal_title：Journal of pharmaceutical sciences

authors： Chen B,Costantino HR,Liu J,Hsu CC,Shire SJ

更新日期：1999-04-01 00:00:00

abstract：:In the present work, authors produced tablets of anhydrous sodium naproxen by wet granulation using a high-shear mixer-granulator. Drug hydrated to the tetrahydrated form, as observed by X-ray powder diffractometry. After wet granulation, authors then performed two different drying procedures, obtaining granules of di...

journal_title：Journal of pharmaceutical sciences

authors： Di Martino P,Malaj L,Censi R,Martelli S

更新日期：2008-12-01 00:00:00

abstract：:Alzheimer's disease (AD) is historically difficult to treat, in part because of the inaccessible nature of brain pathology. Amyloid beta and tau proteins drive pathology by forming toxic oligomers that eventually deposit as insoluble amyloid plaques and neurofibrillary tangles. Recent clinical studies suggest that eff...

journal_title：Journal of pharmaceutical sciences

authors： Vander Zanden CM,Chi EY

更新日期：2020-01-01 00:00:00

abstract：:Pyrimethamine, an antimalarial drug, was found to be able to inhibit both enzymes (DHFR-TS and PTR1) of the leishmanial folate pathway, although this effect in vivo appears only in relatively high concentrations. To reach the parasites inside macrophage cells, where they are sheltered, targeted drugs of pyrimethamine,...

journal_title：Journal of pharmaceutical sciences

authors： De Carvalho PB,Ramos DC,Cotrim PC,Ferreira EI

更新日期：2003-10-01 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：:Carbamazepine (CBZ) is a leading molecule in the management of epilepsy. Surveys have revealed that a sufficient lack of therapeutically efficient CBZ transbuccal formulation exists. Therefore, this investigation was directed toward designing multiparticulate composite construct (MCC) for the transbuccal delivery of C...

journal_title：Journal of pharmaceutical sciences

authors： Adeleke OA,Choonara YE,Du Toit LC,Pillay V

更新日期：2014-04-01 00:00:00

abstract：:The phase behavior of two series of phosphatidylcholines (PC) possessing carbamyloxy-linked fatty acids has been studied by differential scanning calorimetry. These non-natural phosphatidylcholines are of interest because they possess the capability of forming interlipid hydrogen bonds via the carbamyloxy function and...

journal_title：Journal of pharmaceutical sciences

authors： Curatolo W,Bali A,Gupta CM

更新日期：1985-12-01 00:00:00

abstract：:Phenytoin has been decreasingly used because of the high interindividual variability in drug concentration and the narrow therapeutic window. Despite such drawbacks, phenytoin is still essential as a second-line therapy for status epilepticus when patients are resistant to benzodiazepines. This study aimed to develop ...

journal_title：Journal of pharmaceutical sciences

authors： Guk J,Lee SG,Chae D,Kim JH,Park K

更新日期：2019-08-01 00:00:00

abstract：:Nephropathic cystinosis is a rare autosomal recessive disease characterised by raised lysosomal levels of cystine in the cells of all the organs. It is treated by the 6-h oral administration of the aminothiol, cysteamine, which has an offensive taste and smell. In an attempt to reduce this frequency and improve the tr...

journal_title：Journal of pharmaceutical sciences

authors： Buchan B,Kay G,Matthews KH,Cairns D

更新日期：2012-10-01 00:00:00

abstract：:The cyclopropyl amine moiety in GSK2879552 (1) degrades hydrolytically in high pH conditions. This degradation pathway was observed during long-term stability studies and impacted the shelf life of the drug product. This article describes the work to identify the degradation impurities, elucidate the degradation mecha...

journal_title：Journal of pharmaceutical sciences

authors： Campbell JM,Lee M,Clawson J,Kennedy-Gabb S,Bethune S,Janiga A,Kindon L,Leach KP

更新日期：2019-09-01 00:00:00

abstract：:Local variations in compaction behaviour were investigated, for specimens of different shapes and thickness, comparing predictions from finite element (FE) modelling and results from a recently developed method using small-angle X-ray scattering (SAXS). Good agreement was generally obtained between these methods, in t...

journal_title：Journal of pharmaceutical sciences

authors： Laity PR,Han L,Elliott J,Cameron RE

更新日期：2010-10-01 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：:A novel method for creating water soluble prodrugs of cisplatin analogues bearing chelating diamines is introduced. When 2-(amino-methyl)aniline is reacted with K2PtCl4 between a pH of 6 and 7, the neutral chelated complex [2-(aminomethyl)aniline)dichloroplatinum(II) (1) is isolated. On the other hand, when the comple...

journal_title：Journal of pharmaceutical sciences

authors： Köckerbauer R,Bednarski PJ

更新日期：1995-07-01 00:00:00

abstract：:Jet-milling as the common way for micronization of drugs shows several disadvantages. Drug powder properties are decisive for pulmonary use because, besides a small particle size, a good deagglomeration behavior is required. In this study, several anti-inflammatory drugs [beclomethasone-17,21-dipropionate (BDP), betam...

journal_title：Journal of pharmaceutical sciences

authors： Rasenack N,Steckel H,Müller BW

更新日期：2003-01-01 00:00:00

abstract：:The use of pharmacological responses such as pupil diameter for dosage individualization, bioavailability, and pharmacokinetic analyses is becoming more widespread. Attempts to use pupil diameter to assess morphine bioavailability illuminate the fact that multiple responses, nonlinearities, and the condition of the su...

journal_title：Journal of pharmaceutical sciences

authors： Kramer PA

更新日期：1977-04-01 00:00:00

abstract：:In this study, the influence of the preparation technique (ball milling, spray drying, and film casting) of a supersaturated amorphous dispersion on the quality of solubility determinations of indomethacin in polyvinylpyrrolidone was investigated by means of statistical analysis. After annealing of the amorphous dispe...

journal_title：Journal of pharmaceutical sciences

authors： Knopp MM,Olesen NE,Holm P,Löbmann K,Holm R,Langguth P,Rades T

更新日期：2015-01-01 00:00:00

abstract：:The intrinsic absorption of salbutamol in different intestinal segments of the rat was measured and related with the corresponding intestinal P-glycoprotein (P-gp) expression levels. The apparent absorption rate constants (k(a), h(-1)) observed in each fraction by means of the "in situ" rat gut absorption method after...

journal_title：Journal of pharmaceutical sciences

authors： Valenzuela B,Nácher A,Ruiz-Carretero P,Martín-Villodre A,López-Carballo G,Barettino D

更新日期：2004-06-01 00:00:00

abstract：:Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dep...

journal_title：Journal of pharmaceutical sciences

authors： Singh SP,Ali B,Auyong TK,Parmar SS,De Boer B

更新日期：1976-03-01 00:00:00

abstract：:4-Fluoroisoleucine was produced by ammonolysis of 2-bromo-4-fluoro-3-methylpentanoic acid, which resulted from the bromofluorination of 4-methyl-2-pentenoic acid. It did not inhibit Plasmodium berghei in mice at 640 mg/kg and was not toxic to the animals. The fluoroamino acid inhibited Aspergillus niger, Trichoderma v...

journal_title：Journal of pharmaceutical sciences

authors： Gershon H,Shanks L,Clarke DD

更新日期：1978-05-01 00:00:00

abstract：:The particle sizing performance of a Next Generation Pharmaceutical Impactor (NGI) was compared to that of an Andersen cascade impactor (ACI). A single lot of Vanceril MDIs containing beclomethasone dipropionate (BDP) was used throughout. MDIs were sampled into NGI and ACI in accordance with USP recommendations, at 30...

journal_title：Journal of pharmaceutical sciences

authors： Kamiya A,Sakagami M,Hindle M,Byron PR

更新日期：2004-07-01 00:00:00

abstract：:Maintaining good content uniformity (CU) is a significant challenge for low-dose oral tablets in particular when using direct compression (DC). Using 6 model active pharmaceutical ingredients, we show that a platform DC tablet formulation suitable for developing low-dose API with excellent CU can be developed. This pl...

journal_title：Journal of pharmaceutical sciences

authors： Sun WJ,Aburub A,Sun CC

更新日期：2017-07-01 00:00:00

abstract：:Several controlled ice nucleation techniques have been developed to increase the efficiency of the freeze-drying process as well as to improve the quality of pharmaceutical products. Owing to the reduction in ice surface area, these techniques have the potential to reduce the degradation of proteins labile during free...

journal_title：Journal of pharmaceutical sciences

authors： Fang R,Tanaka K,Mudhivarthi V,Bogner RH,Pikal MJ

更新日期：2018-03-01 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：:The aim of this study was to determine the sensitivity of transgenic immune tolerant mice for the type and level of aggregation of recombinant human interferon alpha2b (rhIFNalpha2b). RhIFNalpha2b was aggregated by metal-catalyzed oxidation or by incubation at elevated temperature and various pHs. Native rhIFNalpha2b ...

journal_title：Journal of pharmaceutical sciences

authors： Hermeling S,Schellekens H,Maas C,Gebbink MF,Crommelin DJ,Jiskoot W

更新日期：2006-05-01 00:00:00

abstract：:Flightless I (Flii) is an actin remodeling protein important for cytoskeletal regulation and cellular processes including migration, proliferation, and adhesion. Previous studies have clearly identified Flii as a novel therapeutical target for improved wound repair and have demonstrated Flii regulation using Flii neut...

journal_title：Journal of pharmaceutical sciences

authors： Haidari H,Zhang Q,Melville E,Kopecki Z,Song Y,Cowin AJ,Garg S

更新日期：2017-07-01 00:00:00

abstract：:First-order rate constants (k) were determined for the hydrolysis of ceftazidime in the pH range of 0.5 to 8.5 at 45, 55, and 65 degrees C by a stability-indicating HPLC assay. In the absence of buffer effects, the pH-rate expression was k = kH1f1(aH+) + kH2f2(aH+) + kH3f3(aH+) + kSf3 + kOHf3(aOH-), where KH and KOH a...

journal_title：Journal of pharmaceutical sciences

authors： Zhou M,Notari RE

更新日期：1995-05-01 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：: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：:The purpose of this study was to evaluate the therapeutic efficacy of a new calcium phosphate (CaP)-based formulation in improving the bone mineral deficiency in ovariectomized (OVX) rats. The ions release experiments for CaP preparations (G2: 0.46% Mg, 5.78% Zn, and 2.5% F; G3:3.1% Mg, 0.03% Zn, and 3.01% F; G4: 1.25...

journal_title：Journal of pharmaceutical sciences

authors： Otsuka M,Oshinbe A,Legeros RZ,Tokudome Y,Ito A,Otsuka K,Higuchi WI

更新日期：2008-01-01 00:00:00

abstract：:The pathogenic bacterium Staphylococcus aureus can penetrate host cells. However, intracellular S. aureus is not considered during antimicrobial agent selection in clinical chemotherapy because of the lack of information about drug transportability into cells in vivo. We focused on agents used to treat methicillin-res...

journal_title：Journal of pharmaceutical sciences

authors： Kobuchi S,Kita Y,Hiramatsu Y,Sasaki K,Uno T,Ito Y,Sakaeda T

更新日期：2021-02-01 00:00:00