Enabling tablet product development of 5-fluorocytosine through integrated crystal and particle engineering.

abstract：:Bisphosphonates are widely used for the treatment of bone diseases, including hypercalcemia and osteoporosis. However, the bioavailability (BA) of orally administered bisphosphonates is low, at approximately 0.9%-1.8%. In addition, the oral administration of bisphosphonates is associated with mucosal damage, including...

journal_title：Journal of pharmaceutical sciences

authors： Katsumi H,Takashima M,Sano J,Nishiyama K,Kitamura N,Sakane T,Hibi T,Yamamoto A

更新日期：2011-09-01 00:00:00

abstract：:From a consideration of the basic processes involved in drug elimination, the fraction of drug cleared by the gut and by the liver were described as functions of availability and hepatic clearance. For a drug given orally, a plot of the fraction of drug cleared by the gut or liver against alpha, a proportionality cons...

journal_title：Journal of pharmaceutical sciences

authors： Minchin RF,Ilett KF

更新日期：1982-04-01 00:00:00

abstract：:One of the challenges with predictive modeling is how to quantify the reliability of the models' predictions on new objects. In this work we give an introduction to conformal prediction, a framework that sits on top of traditional machine learning algorithms and which outputs valid confidence estimates to predictions ...

journal_title：Journal of pharmaceutical sciences

authors： Alvarsson J,Arvidsson McShane S,Norinder U,Spjuth O

更新日期：2021-01-01 00:00:00

abstract：:Small particles of two steroids, cholesteryl acetate and beta-sitosterol, were prepared by the following technique. The steroid was dissolved in an organic solvent, which was emulsified in water in the presence of surfactant, thus giving a water-continuous emulsion. As the organic solvent was evaporated, the steroid p...

journal_title：Journal of pharmaceutical sciences

authors： Sjöström B,Bergenståhl B,Kronberg B

更新日期：1993-06-01 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：:Contraceptive natural steroids, such as progesterone and estradiol, are ineffective when administered orally because of extensive metabolism in the gastrointestinal (GI) tract during absorption and first-pass metabolism. Consequently, highly potent and potentially harmful synthetic steroids are now being used in oral...

journal_title：Journal of pharmaceutical sciences

authors： Hussain AA,Hirai S,Bawarshi R

更新日期：1981-04-01 00:00:00

abstract：:Resveratrol trimethyl ether (trans-3,5,4'-trimethoxystilbene, RTE) is a naturally occurring and pharmacologically active resveratrol derivative. To evaluate its suitability as a drug candidate, a pharmacokinetic study was carried out in Sprague-Dawley rats with the emphasis to identify the impact of aqueous solubility...

journal_title：Journal of pharmaceutical sciences

authors： Lin HS,Ho PC

更新日期：2011-10-01 00:00:00

abstract：:Modifications of antibacterial activity have been demonstrated using combinations of two antibacterials from trimethoprim, sulfonamides (sulfadiazine, sulfamerazine, and silver sulfadiazine), silver nitrate, and dibromopropamidine isethionate, either formulated in a cream base or dissolved in peptone water. The creams...

journal_title：Journal of pharmaceutical sciences

authors： Richards RM,Taylor RB,Xing DK

更新日期：1991-09-01 00:00:00

abstract：:Adsorption of proteins to solid-fluid interfaces is often empirically found to promote formation of soluble aggregates and larger, subvisible, and visible particles, but key stages in this process are often difficult to probe directly. Aggregation mediated by adsorption to water-silicon oxide (SiOx) interfaces, akin t...

journal_title：Journal of pharmaceutical sciences

authors： Perevozchikova T,Nanda H,Nesta DP,Roberts CJ

更新日期：2015-06-01 00:00:00

abstract：:Anthrax remains a serious threat worldwide as a bioterror agent. A second-generation anthrax vaccine currently under clinical evaluation consists of a recombinant Protective Antigen (rPA) of Bacillus anthracis. We have previously demonstrated that complete protection against inhalational anthrax can be achieved in a r...

journal_title：Journal of pharmaceutical sciences

authors： Jiang G,Joshi SB,Peek LJ,Brandau DT,Huang J,Ferriter MS,Woodley WD,Ford BM,Mar KD,Mikszta JA,Hwang CR,Ulrich R,Harvey NG,Middaugh CR,Sullivan VJ

更新日期：2006-01-01 00:00:00

abstract：:The purpose of this study was to develop quantitative structure-activity/pharmacokinetic relationships (QSAR/QSPKR) for 11 selected corticosteroids in man. Multiple linear regression analysis with an automatic forward step-wise inclusion algorithm was used to construct QSAR/QSPKR models from molecular and submolecular...

journal_title：Journal of pharmaceutical sciences

authors： Mager DE,Jusko WJ

更新日期：2002-11-01 00:00:00

abstract：:The objectives of this study were to identify the key process parameters during steam granulation of disordered mesoporous silica material Syloid® 244 FP (244) and to compare two different binders: polyvinylpyrrolidone (PVP) K25 and hydroxypropylmethyl cellulose (HPMC). Itraconazole (ITZ) was selected as the model com...

journal_title：Journal of pharmaceutical sciences

authors： Vialpando M,Albertini B,Passerini N,Vander Heyden Y,Rombaut P,Martens JA,Van Den Mooter G

更新日期：2013-11-01 00:00:00

abstract：:Phenylpropanolamine was determined by measuring its fluorescent fluorescamine derivative. The method is rapid, sensitive, and easily automated. Statistics are presented for an effervescent cold product, and recovery data are presented for other commercially available products. ...

journal_title：Journal of pharmaceutical sciences

authors： Shankle LL

更新日期：1978-11-01 00:00:00

abstract：:The interaction between four different microparticulate drug carriers and macrophages was investigated in vitro. The microparticles, consisting of crosslinked starch (1,4-alpha-D-glucan with 1,6-alpha-branches), dextran (1,6-alpha-D-glucan with 1,3-alpha-branches), lichenan (1,3-beta-D-glucan), or mannan (1,6-alpha-D-...

journal_title：Journal of pharmaceutical sciences

authors： Artursson P,Arro E,Edman P,Ericsson JL,Sjöholm I

更新日期：1987-02-01 00:00:00

abstract：:To prepare (+)-tubocurine and O,O-dimethyl-(+)-tubocurine, the commonly used dequaternization procedures with sodium theophenoxide and ethanolamine were investigated. The quaternary compounds were (+)-tubocurarine chloride and the chloride and iodide salts of O,O-dimethyl-(+)-chondocurarine. The results obtained with ...

journal_title：Journal of pharmaceutical sciences

authors： Naghaway JA,Soine TO

更新日期：1978-09-01 00:00:00

abstract：:The concept of cosolvent exclusion was developed by a group of Timasheff's laboratory in 1970-1990 and is currently used widely to explain the effects of a variety of cosolvents on the stability and solubility of macromolecules. Not surprisingly, these concepts have had substantial influence in the fields of formulati...

journal_title：Journal of pharmaceutical sciences

authors： Arakawa T,Gagnon P

更新日期：2018-09-01 00:00:00

abstract：:In the present study, the interaction between phenobarbital and activated carbons which is driven by hydrophobic bonding was evaluated. The Two-Mechanism Langmuir-Like Equation was proposed to describe the isotherms for phenobarbital adsorbing to activated carbons. The parameters in the Two-Mechanism Langmuir-Like Equ...

journal_title：Journal of pharmaceutical sciences

authors： Yu P,Wurster DE

更新日期：2019-01-01 00:00:00

abstract：:In drug release systems using hydrogels as carriers, the presence of the polymer network will reduce the drug release rate, which can extend the release period. For a controlled-release process of drug, usually the ideal situation is to get a zero-order drug release rate. In this paper, the mathematical model of hydro...

journal_title：Journal of pharmaceutical sciences

authors： Xu Y,Jia Y,Wang Z,Wang Z

更新日期：2013-05-01 00:00:00

abstract：:The pneumococcal histidine triad protein D (PhtD) is believed to play a central role in pneumococcal metal ion homeostasis and has been proposed as a promising vaccine candidate against pneumococcal disease. To investigate for potential stabilizers, a panel of physiologically relevant metals was screened using the the...

journal_title：Journal of pharmaceutical sciences

authors： Ausar SF,Jayasundara K,Akawi L,Roque C,Sheung A,Hu J,Kirkitadze M,Rahman N

更新日期：2017-10-01 00:00:00

abstract：:This article describes a procedure to facilitate scale-up for the primary drying phase of lyophilization using a combination of empirical testing and numerical modeling. Freeze dry microscopy is used to determine the temperature at which lyophile collapse occurs. A laboratory scale freeze-dryer equipped with manometri...

journal_title：Journal of pharmaceutical sciences

authors： Kramer T,Kremer DM,Pikal MJ,Petre WJ,Shalaev EY,Gatlin LA

更新日期：2009-01-01 00:00:00

abstract：:In many manufacturing and research areas, the ability to accurately monitor and characterize nanoparticles is becoming increasingly important. Nanoparticle tracking analysis is rapidly becoming a standard method for this characterization, yet several key factors in data acquisition and analysis may affect results. Nan...

journal_title：Journal of pharmaceutical sciences

authors： Krueger AB,Carnell P,Carpenter JF

更新日期：2016-04-01 00:00:00

abstract：:Nasal mucosa excised from dogs or rabbits was mounted as a flat sheet in an in vitro chamber. The permeability was assessed by measuring the unidirectional flux of the radiolabeled tracer compounds, water, sucrose, polyethylene glycol, and cholecystokinin octapeptide. The permeability coefficients calculated from the ...

journal_title：Journal of pharmaceutical sciences

authors： Hersey SJ,Jackson RT

更新日期：1987-12-01 00:00:00

abstract：:A sensitive (10 ng/mL) and specific high-performance liquid chromatographic (HPLC) assay, with electrochemical (EC) detection, for the geometric isomers of 3-hydroxy-N-(2-phenyl-2-(2-thienyl)ethenyl-5-(trifluoromethyl)benzo(b) thiophene-2-carboxamide in dog and human plasma has been developed. Both isomers strongly ab...

journal_title：Journal of pharmaceutical sciences

authors： Matuszewski BK,Kanovsky SM,Constanzer ML,Yeh KC,Bayne WF

更新日期：1988-10-01 00:00:00

abstract：:Vaults, at 13 MDa, are the largest ribonucleoprotein particles known. In vitro, expression of the major vault protein (MVP) alone in Sf9 insect cells results in the production of recombinant particles with characteristic vault structure. With the ultimate goal of using recombinant vaults as nanocapsules for the delive...

journal_title：Journal of pharmaceutical sciences

authors： Esfandiary R,Kickhoefer VA,Rome LH,Joshi SB,Middaugh CR

更新日期：2009-04-01 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：:Continuing work on the interaction of inorganic additives with nonionic surfactants in aqueous solution dealt with their effect on the CMC and surface tension. The surfactants were octoxynol and polyoxyethylated oleyl alcohol, containing an average of 9.5 and 10 ethylene oxide units, respectively. Their CMC values wer...

journal_title：Journal of pharmaceutical sciences

authors： Schott H,Han SK

更新日期：1976-07-01 00:00:00

abstract：:Isomazole matrix tablet formulations, with various concentrations of hydroxypropyl methylcellulose (HPMC) hydrogel, were prepared and tested for sustained-release activity. Sustained-release activity was determined by administering isomazole test formulations orally to conscious dogs, instrumented with an indwelling l...

journal_title：Journal of pharmaceutical sciences

authors： Wilson HC,Cuff GW

更新日期：1989-07-01 00:00:00

abstract：:Melphalan (30 microgram/ml) is completely hydrolyzed in water at 37 degrees after 8 hr. At lower temperatures, hydrolysis proceeds at slower rates. The presence of bovine serum albumin retards hydrolysis of melphalan (30 microgram/ml) in water. The melphalan hydrolysis rate is directely releated to the bovine serum al...

journal_title：Journal of pharmaceutical sciences

authors： Chang SY,Alberts DS,Farquhar D,Melnick LR,Walson PD,Salmon SE

更新日期：1978-05-01 00:00:00

abstract：:Metronidazole (MTZ) is a drug of choice for protozoal infections such as luminal amoebiasis. We designed and synthesized N-nicotinoyl-2-{2-(2-methyl-5-nitroimidazol-1-yl)ethyloxy}-D,L-glycine (NMG) as a colon-specific prodrug of MTZ. The synthetic yield of NMG was about 34%. The apparent partition coefficient of MTZ w...

journal_title：Journal of pharmaceutical sciences

authors： Kim D,Hong S,Jung S,Jung Y,Kim YM

更新日期：2009-11-01 00:00:00

abstract：:A GLC-mass spectrometric assay for methylphenidate in biological fluids was developed using the ethyl ester homolog of the drug as the internal standard. The procedure has a lower level of sensitivity of 1.2 ng/ml and is based on GLC-mass spectrometic monitoring of the m/e 180 ion common to the mass spectra of the N-t...

journal_title：Journal of pharmaceutical sciences

authors： Gal J,Hodshon BJ,Pintauro C,Flamm BL,Cho AK

更新日期：1977-06-01 00:00:00