Engineering Stability, Viscosity, and Immunogenicity of Antibodies by Computational Design.

abstract：:Controlling residual solvent levels is a major concern in pharmaceutical freeze-drying from co-solvent systems. This review provides an overview of the factors influencing this process and estimates their potential to reduce residual solvents in freeze-dried products. Decreased solvent contents are potentially correla...

journal_title：Journal of pharmaceutical sciences

authors： Kunz C,Gieseler H

更新日期：2018-08-01 00:00:00

abstract：:Corneal penetration studies were conducted in unanesthetized albino rabbits using various organic compounds representing both polar and nonpolar species. Very low molecular weight compounds demonstrate rapid uptake into the aqueous humor despite the lipid-like barrier imposed by the corneal epithelium. Evidence that t...

journal_title：Journal of pharmaceutical sciences

authors： Grass GM,Robinson JR

更新日期：1988-01-01 00:00:00

abstract：:The binding of nine diazepines to human serum albumin (HSA) and to alpha 1-acid glycoprotein (AGP) was investigated by means of fluorescence and circular dichroism (CD) spectroscopies. The binding parameters of diazepam obtained from fluorescence agreed with those obtained from CD measurements. Diazepines have one tig...

journal_title：Journal of pharmaceutical sciences

authors： Maruyama T,Furuie MA,Hibino S,Otagiri M

更新日期：1992-01-01 00:00:00

abstract：:The stability of therapeutic proteins formulated in prefilled syringes (PFS) may be negatively impacted by the exposure of protein molecules to silicone oil-water interfaces and air-water interfaces. In addition, agitation, such as that experienced during transportation, may increase the detrimental effects (i.e., pro...

journal_title：Journal of pharmaceutical sciences

authors： Gerhardt A,Mcgraw NR,Schwartz DK,Bee JS,Carpenter JF,Randolph TW

更新日期：2014-06-01 00:00:00

abstract：:Apomorphine, a dopamine receptor agonist for treating Parkinson's disease, has very poor oral bioavailability (<2%) due to the first-pass effect. The aim of this work was to investigate whether the oral bioavailability and brain regional distribution of apomorphine could be improved by utilizing solid lipid nanopartic...

journal_title：Journal of pharmaceutical sciences

authors： Tsai MJ,Huang YB,Wu PC,Fu YS,Kao YR,Fang JY,Tsai YH

更新日期：2011-02-01 00:00:00

abstract：:Chitosan and egg phosphatidylcholine (ePC) were used as a unique combination to prepare composite films for localized drug delivery. In comparison to other phospholipids analyzed, ePC was found to produce chitosan-based films with minimal swelling and a high degree of stability. The properties of the chitosan-ePC film...

journal_title：Journal of pharmaceutical sciences

authors： Grant J,Blicker M,Piquette-Miller M,Allen C

更新日期：2005-07-01 00:00:00

abstract：:Both developing (Days --1-+12 relative to inoculation) and established (Days +18-+29) stages of Mycobacterium butyricum adjuvant-induced polyarthritis in rats were treated orally with cryogenine (100 mg/kg/day), a prototype anti-inflammatory (phenylbutazone, 100 mg/kg/day), or a prototype immunosuppressive (cyclophosp...

journal_title：Journal of pharmaceutical sciences

authors： Watson WC,Malone MH

更新日期：1977-09-01 00:00:00

abstract：:Pharmaceutical aerosols are used to treat many pulmonary diseases. The use of low-density powders has proven useful to support efficient drug delivery. Measurements must account for the low-density, spherical particle features contributing to aerodynamic behavior. Ideally, the aerodynamic particle size distribution (A...

journal_title：Journal of pharmaceutical sciences

authors： Hickey AJ,Edwards DA

更新日期：2018-03-01 00:00:00

abstract：:Quantitative prediction of unbound drug fraction (fu) is essential for scaling pharmacokinetics through physiologically based approaches. However, few attempts have been made to evaluate the projection of fu values under pathological conditions. The primary objective of this study was to predict fu values (n = 105) of...

journal_title：Journal of pharmaceutical sciences

authors： Li GF,Yu G,Li Y,Zheng Y,Zheng QS,Derendorf H

更新日期：2018-07-01 00:00:00

abstract：:The development of order during the aging of aluminum hydroxide gel prepared by the reaction of aluminum chloride and ammonium hydroxide to a final pH of 7.0 can be monitored by differential thermal analysis. The loss fo acid reactivity upon aging is accompanied by an increase in the temperature and intensity of the d...

journal_title：Journal of pharmaceutical sciences

authors： Aboul-Enein N,Sam J

更新日期：1976-09-01 00:00:00

abstract：:The blood-brain barrier permeation has been investigated by using a topological substructural molecular design approach (TOPS-MODE). A linear regression model was developed to predict the in vivo blood-brain partitioning coefficient on a data set of 119 compounds, treated as the logarithm of the blood-brain concentrat...

journal_title：Journal of pharmaceutical sciences

authors： Cabrera MA,Bermejo M,Pérez M,Ramos R

更新日期：2004-07-01 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：:Baclofen immediate release mode of administration exhibit sharp plasma peaking that results in the emergence of side effects like hypotension. This research employs preformulation studies to design an optimum dosage form for baclofen to enhance therapeutic outcomes. These studies include partition coefficient and ex-v...

journal_title：Journal of pharmaceutical sciences

authors： Ibrahim M,Naguib YW,Sarhan HA,Abdelkader H

更新日期：2020-10-15 00:00:00

abstract：:Twelve 6,8-disubstituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acid derivatives were prepared and evaluated for their antibacterial activity. Among these, only the 6,8-difluoroquinolinone-3-carboxylic acid showed moderate activity. ...

journal_title：Journal of pharmaceutical sciences

authors： Krishnan R,Lang SA Jr

更新日期：1986-12-01 00:00:00

abstract：:Determination of the kinetics of water-soluble degradation products inside poly(lactide-co-glycolide) (PLGA) delivery systems during polymer degradation is important to evaluate the polymer microclimate conditions, particularly microclimate pH changes for optimization of encapsulated drug stability. A pre-derivatizati...

journal_title：Journal of pharmaceutical sciences

authors： Ding AG,Schwendeman SP

更新日期：2004-02-01 00:00:00

abstract：:This work investigated the impact of primary drying conditions on the microstructure and protein stability of bovine serum albumin (BSA) containing lyophilized cakes. Two primary drying conditions were employed (termed 'conservative', slower drying rate and 'aggressive', higher drying rate) at two protein loadings (5 ...

journal_title：Journal of pharmaceutical sciences

authors： Parker A,Rigby-Singleton S,Perkins M,Bates D,Le Roux D,Roberts CJ,Madden-Smith C,Lewis L,Teagarden DL,Johnson RE,Ahmed SS

更新日期：2010-11-01 00:00:00

abstract：:The development of multiple drug modalities over the past 20 years has dramatically expanded the therapeutic space for intervention in disease processes. Rather than being alternative therapeutic approaches, these modalities tend to be complimentary both in the scope of target space and the biological mechanisms harne...

journal_title：Journal of pharmaceutical sciences

authors： Hochman JH

更新日期：2021-01-01 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：:Aqueous solubilities for some guanine derivatives were estimated by semiempirical equations developed by Yalkowsky and Valvani1 using the data for partition coefficient and melting temperature. It was shown that in the case of guanine derivatives examined in this study, the solubility values could not be estimated ade...

journal_title：Journal of pharmaceutical sciences

authors： Kristl A

更新日期：1999-01-01 00:00:00

abstract：:The human immunodeficiency virus has infected millions of people and the epidemic continues to grow rapidly in some parts of the world. Antiretroviral (ARV) therapy has provided improved treatment and prolonged the life expectancy of patients. Moreover, there is growing interest in using ARVs to protect against new in...

journal_title：Journal of pharmaceutical sciences

authors： Kirtane AR,Langer R,Traverso G

更新日期：2016-12-01 00:00:00

abstract：:Although inaccurate true density affects analysis of powder compaction data, such effects have not been systematically evaluated in the literature. This work is aimed at quantitatively evaluating effects of inaccurate true density on tableting data analysis using the Ryshkewitch equation, sigma = sigma0 e - bepsilon, ...

journal_title：Journal of pharmaceutical sciences

authors： Sun CC

更新日期：2005-09-01 00:00:00

abstract：:Pharmaceutical scientists are often asked to assess the impact of modifications to the illumination in the manufacturing and product packaging environment on product quality. To assess the impact of switching light sources, four model compounds were exposed to standard fluorescent light, LED, and "yellow light" and th...

journal_title：Journal of pharmaceutical sciences

authors： Wasylaschuk W,Pierce B,Geng X,Socia A,Kim D,Wuelfing WP,Abend A

更新日期：2020-11-01 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：:With the introduction of Quality by Design (QbD) to the pharmaceutical industry, there has been an increased focus on understanding the nature of particles and composites, with the aim of understanding and modeling how they interact in complex systems, leading to robust dosage forms. Particle characterization tools ha...

journal_title：Journal of pharmaceutical sciences

authors： Gamble JF,Tobyn M,Hamey R

更新日期：2015-05-01 00:00:00

abstract：:Role of water in chemical (in)stability is revisited, with focus on deamidation in freeze-dried amorphous proteins and peptides. Two distinct patterns for deamidation versus water have been reported, that is, a consistent increase in rate constant with water, and a "hockey stick"-type behavior. For the latter, deamida...

journal_title：Journal of pharmaceutical sciences

authors： Ohtake S,Feng S,Shalaev E

更新日期：2018-01-01 00:00:00

abstract：:Pinacidil [(+/-)-2-cyano-1-(4-pyridyl)-3-(1,2,2-trimethylpropyl)guanidine monohydrate] is a novel, direct-acting vasodilator antihypertensive agent. The cyano 14C-labeled drug is rapidly and completely absorbed after an oral 12.5-mg dose in solution. The blood:plasma concentration ratios (0.8-0.9) indicate transient p...

journal_title：Journal of pharmaceutical sciences

authors： DeLong AF,Oldham SW,DeSante KA,Nell G,Henry DP

更新日期：1988-02-01 00:00:00

abstract：:Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibi...

journal_title：Journal of pharmaceutical sciences

authors： Greenslade FC,Scott CK,Newquist KL,Krider KM,Chasin M

更新日期：1982-01-01 00:00:00

abstract：:The aim of this study was to evaluate a strategy based on static and dynamic physiologically based pharmacokinetic (PBPK) modeling for the prediction of metabolite and parent drug area under the time-concentration curve ratio (AUCm/AUCp) and their PK profiles in humans using in vitro data when active transport process...

journal_title：Journal of pharmaceutical sciences

authors： Nguyen HQ,Lin J,Kimoto E,Callegari E,Tse S,Obach RS

更新日期：2017-09-01 00:00:00

abstract：:The aim of this study was to prepare and characterize thiolated chitosan (TC) nanoparticles (NPs) of tizanidine HCl (TZ) and to evaluate its transport across monolayer of RPMI 2650 cells (Human nasal septum carcinoma cell line) followed by assessment of their pharmacokinetic and pharmacodynamic attributes, after intra...

journal_title：Journal of pharmaceutical sciences

authors： Patel D,Naik S,Misra A

更新日期：2012-02-01 00:00:00

abstract：:The period of time after administration over which blood level measurements are required to obtain a reliable bioavailability comparison of two or more formulations of the same drug was considered by the analysis of bioavailability data taken from the literature. The drugs examined, selected to represent a range of ab...

journal_title：Journal of pharmaceutical sciences

authors： Lovering EG,McGilveray IJ,McMillan I,Tostowaryk W

更新日期：1975-09-01 00:00:00