Simple rapid method for the preparation of enteric-coated microspheres.

abstract：:Adequate protein solubility is an important prerequisite for development, manufacture, and administration of biotherapeutic drug candidates, especially for high-concentration protein formulations. A previously established method for determining the relative apparent solubility (thermodynamic activity) of proteins usin...

journal_title：Journal of pharmaceutical sciences

authors： Toprani VM,Joshi SB,Kueltzo LA,Schwartz RM,Middaugh CR,Volkin DB

更新日期：2016-08-01 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：:Aliphatic polyesters have great utility as temporary prosthetics and surgical aids, and in drug delivery systems. Knowledge of the mechanism and pathways of hydrolysis can form a basis for the design and selection of a controlled-release system. Because of the importance of hydrolysis to the properties of such a syste...

journal_title：Journal of pharmaceutical sciences

authors： Maniar ML,Kalonia DS,Simonelli AP

更新日期：1991-08-01 00:00:00

abstract：:6-Chloro-9-[2-(6-methyl-3-pyridyl)ethyl]-1,2,3,4-tetrahydrocarbazole-2-carboxylic acid hydrochloride lowered serum cholesterol, triglyceride, phospholipid, and free fatty acid levels in normal rats. The compound appeared to have a low toxicity and to be well tolerated in mice, adult and neonatal rats, and rabbits. At ...

journal_title：Journal of pharmaceutical sciences

authors： Dalton C,Pool WR

更新日期：1977-03-01 00:00:00

abstract：:In this study, the effects of structurally related organic impurities on the molecular dynamics of amorphous sulfamethazine were evaluated using thermal analysis. Sulfanilamide (SNA), sulfamerazine (SMR), and sulfadimethoxine were used as virtual impurities of sulfamethazine. The amorphous state was prepared in situ i...

journal_title：Journal of pharmaceutical sciences

authors： Hamada Y,Ono M,Ohara M,Yonemochi E

更新日期：2017-04-01 00:00:00

abstract：:Deflocculated suspensions of coarse powders tend to cake as the individual particles settle out and form compact, cohesive sediments. Limited flocculation results in looser sediments because the settled-out flocs incorporate large amounts of the liquid suspending medium. Controlled flocculation of bismuth subnitrate s...

journal_title：Journal of pharmaceutical sciences

authors： Schott H

更新日期：1976-06-01 00:00:00

abstract：:The present study pursued to profile the intestinal solubility of nine HIV protease inhibitors (PIs) in fasted- and fed-state human intestinal fluids (FaHIF, FeHIF) aspirated from four volunteers. In addition, the ability of fasted- and fed-state simulated intestinal fluids (FaSSIF, FeSSIF) to predict the intestinal s...

journal_title：Journal of pharmaceutical sciences

authors： Wuyts B,Brouwers J,Mols R,Tack J,Annaert P,Augustijns P

更新日期：2013-10-01 00:00:00

abstract：:The purpose of this study was to understand the combined effect of two polymers showing drug-polymer interactions on amorphous stabilization and dissolution enhancement of indomethacin (IND) in amorphous ternary solid dispersions. The mechanism responsible for the enhanced stability and dissolution of IND in amorphous...

journal_title：Journal of pharmaceutical sciences

authors： Prasad D,Chauhan H,Atef E

更新日期：2014-11-01 00:00:00

abstract：:Experimental solubilities are reported for anthracene in binary solvent mixtures containing p-dioxane with n-hexane, cyclohexane, n-heptane, methylcyclohexane, n-octane, cyclooctane, and isooctane at 25 degrees C. Results of these measurements, used in conjunction with the nearly ideal binary solvent (NIBS) model, ena...

journal_title：Journal of pharmaceutical sciences

authors： Procyk AD,Bissell M,Street KW Jr,Acree WE Jr

更新日期：1987-08-01 00:00:00

abstract：:Cytochrome P450 1B1 (CYP1B1) has been reported to have a major role in metabolizing arachidonic acid (AA) into cardiotoxic metabolites, mid-chain hydroxyeicosatetraenoic acids (HETEs). Recently, we have shown that fluconazole decreases the level of mid-chain HETEs in human liver microsomes. Therefore, the objectives o...

journal_title：Journal of pharmaceutical sciences

authors： Alammari AH,Shoieb SM,Maayah ZH,El-Kadi AOS

更新日期：2020-07-01 00:00:00

abstract：:Detection and quantification of the amorphous phase of etoricoxib bulk drug substances, a selective cycloogenase-2 inhibitor used for the treatment of osteoarthritis, rheumatoid arthritis, and dental pain, was carried out using modulated differential scanning calorimetry (MDSC), dynamic mechanical analysis (DMA), and ...

journal_title：Journal of pharmaceutical sciences

authors： Clas SD,Lalonde K,Khougaz K,Dalton CR,Bilbeisi R

更新日期：2012-02-01 00:00:00

abstract：:Solvent influences on the crystallization of polymorph and hydrate forms of the nootropic drug piracetam (2-oxo-pyrrolidineacetamide) were investigated from water, methanol, 2-propanol, isobutanol, and nitromethane. Crystal growth profiles of piracetam polymorphs were constructed using time-resolved diffraction snapsh...

journal_title：Journal of pharmaceutical sciences

authors： DeMatos LL,Williams AC,Booth SW,Petts CR,Taylor DJ,Blagden N

更新日期：2007-05-01 00:00:00

abstract：:Two multisample laboratory powder diffractometers have been evaluated for the purpose of pattern indexing in the context of physical form screening. Both diffractometers utilise foil transmission geometry, primary monochromated radiation, and a position-sensitive detector. Data collected from six compounds (sotalol hy...

journal_title：Journal of pharmaceutical sciences

authors： Florence AJ,Baumgartner B,Weston C,Shankland N,Kennedy AR,Shankland K,David WI

更新日期：2003-09-01 00:00:00

abstract：:A general method for predicting the intestinal absorption of a wide range of drugs using multiple regression analysis of their physicochemical properties and the drug-membrane electrostatic interaction was developed. The absorption rates of tested drugs from rat jejunum were measured by the in situ single-pass perfusi...

journal_title：Journal of pharmaceutical sciences

authors： Sugawara M,Takekuma Y,Yamada H,Kobayashi M,Iseki K,Miyazaki K

更新日期：1998-08-01 00:00:00

abstract：:Using quantitative structure-retention relationships (QSRR) methodologies the Kovats gas chromatographic retention indices for both apolar (DB-1) and polar (DB-Wax) columns for 48 compounds from Ylang-Ylang essential oil were empirically predicted from calculated and experimental data on molecular structure. Topologic...

journal_title：Journal of pharmaceutical sciences

authors： Olivero J,Gracia T,Payares P,Vivas R,Díaz D,Daza E,Geerlings P

更新日期：1997-05-01 00:00:00

abstract：:High-throughput lyophilization process was designed and developed for protein formulations using a single-step drying approach at a shelf temperature (Ts) of ≥40°C. Model proteins were evaluated at different protein concentrations in amorphous-only and amorphous-crystalline formulations. Single-step drying resulted in...

journal_title：Journal of pharmaceutical sciences

authors： Pansare SK,Patel SM

更新日期：2019-04-01 00:00:00

abstract：:An F(ab')2 fragment of an IgG has been spray-dried on a bench-top machine to examine the presence of insoluble particulates in the redissolved powder product. Preliminary experiments showed that treatment of the F(ab')2 in aqueous solution in a water bath at 65°C for 1 h produced fragmentation and also insoluble parti...

journal_title：Journal of pharmaceutical sciences

authors： Lassner P,Adler M,Lee G

更新日期：2014-04-01 00:00:00

abstract：:Isoperibol calorimetry was used to evaluate protein/carbohydrate interactions after freeze drying. rh-DNase, rh-GH, rh-MetGH, and rh-IGF-I were freeze dried with either mannitol, sucrose, trehalose, or dextran at concentrations ranging from 0% to 100% (w/w). Enthalpies of solution for both freeze-dried and physical mi...

journal_title：Journal of pharmaceutical sciences

authors： Souillac PO,Costantino HR,Middaugh CR,Rytting JH

更新日期：2002-01-01 00:00:00

abstract：:Different approaches for the colorimetric determination of acetaminophen, based on its coupling with diazotized o-nitroaniline, are described. Copper(II) chelation with the coupled compound makes the method highly selective. Sensitivity is increased when the acetaminophen assay is carried out indirectly through the de...

journal_title：Journal of pharmaceutical sciences

authors： Belal S,Elsayed MA,El-Waliely A,Abdine H

更新日期：1979-06-01 00:00:00

abstract：:Solid solutions of felodipine with EUDRAGIT E and EUDRAGIT E/NE were shown to dramatically increase the dissolution rate of felodipine in biorelevant media. Of the two polymer systems, extrudates containing 5% EUDRAGIT NE showed a faster dissolution rate and less recrystallization (no precipitation within 2 h). Althou...

journal_title：Journal of pharmaceutical sciences

authors： Nollenberger K,Gryczke A,Meier Ch,Dressman J,Schmidt MU,Brühne S

更新日期：2009-04-01 00:00:00

abstract：:The ability to successfully formulate and manufacture therapeutic protein dosage forms requires a thorough understanding of their physico-chemical properties. Proteins are inherently dynamic molecules of marginal stability. These properties present unique challenges to the pharmaceutical scientist attempting to develo...

journal_title：Journal of pharmaceutical sciences

authors： Kamerzell TJ,Middaugh CR

更新日期：2008-09-01 00:00:00

abstract：:A rotating-basket apparatus for dissolution testing of veterinary bolus tablets was designed and constructed. Sulfamethazine boluses containing different disintegrating agents were evaluated in vitro and by blood level data following administration to cattle. The dissolution t50 and various pharmacokinetic parameters ...

journal_title：Journal of pharmaceutical sciences

authors： Frazier WF,Nuessle NO

更新日期：1976-12-01 00:00:00

abstract：:In pharmacokinetic evaluation of mice, using serial sampling methods rather than a terminal blood sampling method could reduce the number of animals needed and lead to more reliable data by excluding individual differences. In addition, using serial sampling methods can be valuable for evaluation of the drug-drug inte...

journal_title：Journal of pharmaceutical sciences

authors： Watanabe A,Watari R,Ogawa K,Shimizu R,Tanaka Y,Takai N,Nezasa K,Yamaguchi Y

更新日期：2015-03-01 00:00:00

abstract：:The aim of this study was to investigate the bioavailability enhancement of the biopharmaceutics classification system class II compound ezetimibe loaded in ordered mesoporous silica (OMS) in dogs. The OMS was characterized as highly ordered mesoporous material with a narrow pore size distribution. Ezetimibe was loade...

journal_title：Journal of pharmaceutical sciences

authors： Kiekens F,Eelen S,Verheyden L,Daems T,Martens J,Van Den Mooter G

更新日期：2012-03-01 00:00:00

abstract：:Three novel series of 4-oxoquinazoline derivatives were prepared and evaluated as potential antimicrobial agents. Evaluation of the antimicrobial activity of a variety of 4-substituted-1-thiosemicarbazides, 3,4-disubstituted thiazolines, and 3-substituted-5-thiazolidones reveals that the majority possess significant i...

journal_title：Journal of pharmaceutical sciences

authors： Habib NS,Khalil MA

更新日期：1984-07-01 00:00:00

abstract：:Chitosan salts are being investigated as materials for bacterially triggered colonic drug delivery, via the oral route, based on the assumption that they will be degraded by the enzymes produced by the human colonic bacteria. The actual susceptibility of chitosan to these enzymes is, however, unclear. The digestion of...

journal_title：Journal of pharmaceutical sciences

authors： McConnell EL,Murdan S,Basit AW

更新日期：2008-09-01 00:00:00

abstract：:Development of high-throughput release and characterization assays is critical for the effective support of the rapidly growing biologics pipeline for biotherapeutics. Clipping of polypeptide chains is commonly monitored during process optimization, formulation development, and stability studies. A reduced capillary e...

journal_title：Journal of pharmaceutical sciences

authors： Stackhouse N,Miller AK,Gadgil HS

更新日期：2011-12-01 00:00:00

abstract：:This article presents a theoretical model of transdermal drug delivery from an emulsion-type vehicle that addresses the vehicle heterogeneity and incorporates the prediction of drug transport parameters as function of the vehicle composition. The basic mass transfer model considers interfacial and diffusion resistance...

journal_title：Journal of pharmaceutical sciences

authors： Bernardo FP,Saraiva PM

更新日期：2008-09-01 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：:Disintegration performance was measured by analysing both water ingress and tablet swelling of pure microcrystalline cellulose (MCC) and in mixture with croscarmellose sodium using terahertz pulsed imaging (TPI). Tablets made from pure MCC with porosities of 10% and 15% showed similar swelling and transport kinetics: ...

journal_title：Journal of pharmaceutical sciences

authors： Yassin S,Goodwin DJ,Anderson A,Sibik J,Ian Wilson D,Gladden LF,Axel Zeitler J

更新日期：2015-10-01 00:00:00