abstract：:At low protein concentrations (c2), non-native protein aggregation rates are known to be sensitive to changes in conformational stability and "weak" or "colloidal" protein-protein interactions. Protein-protein interactions are also known to be strong functions of c2. In the present work, protein-protein interactions a...

journal_title：Journal of pharmaceutical sciences

authors： Ghosh R,Calero-Rubio C,Saluja A,Roberts CJ

更新日期：2016-03-01 00:00:00

abstract：:Ketoconazole (KTZ) has 2 chiral centers with the therapeutically active form being a racemic mixture of 2 cis-enantiomers, namely, (2R,4S)-(+)-KTZ and (2S,4R)-(-)-KTZ. The aims of the present study were to examine the effects of (+)-KTZ, (-)-KTZ, and (±)-KTZ on aryl hydrocarbon receptor activation and subsequently CYP...

journal_title：Journal of pharmaceutical sciences

authors： Anwar-Mohamed A,El-Sherbeni AA,Hamdy DA,Korashy HM,Brocks DR,El-Kadi AO

更新日期：2016-03-01 00:00:00

abstract：:This study aimed to investigate the surface energy factors behind improved aerosolization performance of spray-dried colistin powder formulations compared with those produced by jet milling. Inhalable colistin powder formulations were produced by jet milling or spray drying (with or without l-leucine). Scanning electr...

journal_title：Journal of pharmaceutical sciences

authors： Jong T,Li J,Morton DA,Zhou QT,Larson I

更新日期：2016-03-01 00:00:00

abstract：:We present a systematic evaluation of the Wajima superpositioning method to estimate the human intravenous (i.v.) pharmacokinetic (PK) profile based on a set of 54 marketed drugs with diverse structure and range of physicochemical properties. We illustrate the use of average of "best methods" for the prediction of cle...

journal_title：Journal of pharmaceutical sciences

authors： Lombardo F,Berellini G,Labonte LR,Liang G,Kim S

更新日期：2016-03-01 00:00:00

abstract：:We investigated the effect of cytochrome P450 (CYP) 2C9 polymorphism on the inhibition of methylhydroxylation activity of tolbutamide, a typical CYP2C9 substrate, by triazole antifungal agents, fluconazole and voriconazole. Although the Michaelis constants (Km), maximal velocities (Vmax), and Vmax/Km values for CYP2C9...

journal_title：Journal of pharmaceutical sciences

authors： Niwa T,Hata T

更新日期：2016-03-01 00:00:00

abstract：:Owing to proliferation of antibiotic-resistant bacteria, the use of antibiotics for livestock growth promotion is banned in many countries and alternatives to in-feed antibiotics are needed. Cinnamon essential oil exhibits strong in vitro antibacterial activity; however, direct addition of essential oils to animal fee...

journal_title：Journal of pharmaceutical sciences

authors： Ma YH,Wang Q,Gong J,Wu XY

更新日期：2016-03-01 00:00:00

abstract：:Central-nervous-system, physiologically based pharmacokinetic (PBPK) models predict exposure profiles in the brain, that is, the rate and extent of distribution. The current work develops one such model and presents improved methods for determining key input parameters. A simple linear regression statistical model est...

journal_title：Journal of pharmaceutical sciences

authors： Trapa PE,Belova E,Liras JL,Scott DO,Steyn SJ

更新日期：2016-02-01 00:00:00

abstract：:The aim of this study is to evaluate the effect of peptide cyclization on the blood-brain barrier (BBB) modulatory activity and plasma stability of His-Ala-Val peptides, which are derived from the extracellular 1 domain of human E-cadherin. The activities to modulate the intercellular junctions by linear HAV4 (Ac-SHAV...

journal_title：Journal of pharmaceutical sciences

authors： Alaofi A,On N,Kiptoo P,Williams TD,Miller DW,Siahaan TJ

更新日期：2016-02-01 00:00:00

abstract：:As part of a series of articles in this special issue evaluating model IgG1-Fc glycoforms for biosimilarity analysis, 3 well-defined IgG1-Fc glycoforms (high mannose-Fc, Man5-Fc, and N-acetylglucosamine-Fc) and a nonglycosylated Fc protein (N297Q-Fc) were examined in this work to elucidate chemical degradation pathway...

journal_title：Journal of pharmaceutical sciences

authors： Mozziconacci O,Okbazghi S,More AS,Volkin DB,Tolbert T,Schöneich C

更新日期：2016-02-01 00:00:00

abstract：:Conventionally, it is believed that the fraction of orally administered drugs absorbed from the intestine (Fa) and intestinal availability (Fg) are independently determined by the apical membrane permeation and intestinal metabolism, respectively. However, the validity of this belief has not been well discussed, and F...

journal_title：Journal of pharmaceutical sciences

authors： Tanaka Y,Kitamura Y,Maeda K,Sugiyama Y

更新日期：2016-02-01 00:00:00

abstract：:The expression of carboxylesterase (CES) and the transdermal movement of an ester prodrug were studied in rat skin. Ethyl-fexofenadine (ethyl-FXD) was used as a model lipophilic prodrug that is slowly hydrolyzed to its parent drug, FXD (MW 502). Among the CES1 and CES2 isozymes, Hydrolase A is predominant in rat skin ...

journal_title：Journal of pharmaceutical sciences

authors： Imai T,Ariyoshi S,Ohura K,Sawada T,Nakada Y

更新日期：2016-02-01 00:00:00

abstract：:The challenge of defining the concentration of unbound drug at the lung target site after inhalation limits the possibility to optimize target exposure by compound design. In this study, a novel rat lung slice methodology has been developed and applied to study drug uptake in lung tissue, and the mechanisms by which t...

journal_title：Journal of pharmaceutical sciences

authors： Bäckström E,Lundqvist A,Boger E,Svanberg P,Ewing P,Hammarlund-Udenaes M,Fridén M

更新日期：2016-02-01 00:00:00

abstract：:Nicotine is absorbed from the lungs into the systemic circulation during cigarette smoking. However, there is little information concerning the transport mechanism of nicotine in alveolar epithelial cells. In this study, we characterized the uptake of nicotine in rat primary cultured type II (TII) and transdifferentia...

journal_title：Journal of pharmaceutical sciences

authors： Takano M,Nagahiro M,Yumoto R

更新日期：2016-02-01 00:00:00

abstract：:Nanocrystals have emerged as a potential formulation strategy to eliminate the bioavailability-related problems by enhancing the initial dissolution rate and moderately super-saturating the thermodynamic solubility. This review contains an in-depth knowledge of, the processing method for formulation, an accurate quant...

journal_title：Journal of pharmaceutical sciences

authors： Shah DA,Murdande SB,Dave RH

更新日期：2016-01-01 00:00:00

abstract：:This study explored the ability to conduct primary drying during lyophilization at product temperatures above the glass transition temperature of the maximally freeze-concentrated solution (Tg′) in amorphous formulations for four proteins from three different classes. Drying above Tg′ resulted in significant reduction...

journal_title：Journal of pharmaceutical sciences

authors： Depaz RA,Pansare S,Patel SM

更新日期：2016-01-01 00:00:00

abstract：:In this study, curcumin and/or docosahexaenoic acid (DHA) were encapsulated in Thai silk fibroin/gelatin (SF/G) sponges, prepared at different blending ratios, aimed to be applied as a controlled release system for localized cancer therapy. The SF/G sponges were fabricated by freeze-drying and glutaraldehyde cross-lin...

journal_title：Journal of pharmaceutical sciences

authors： Lerdchai K,Kitsongsermthon J,Ratanavaraporn J,Kanokpanont S,Damrongsakkul S

更新日期：2016-01-01 00:00:00

abstract：:To characterize and evaluate human serum albumin-encapsulated nanoparticles for drug delivery of a tyrosine kinase inhibitor combined with induction of photothermal ablation combination therapy of renal cell carcinoma (RCC), nanoparticles of varying preparations and concentrations were characterized via zeta potential...

journal_title：Journal of pharmaceutical sciences

authors： Callaghan C,Peralta D,Liu J,Mandava SH,Maddox M,Dash S,Tarr MA,Lee BR

更新日期：2016-01-01 00:00:00

abstract：:To evaluate the regional delivery of conventional aerosol medications, a new whole-lung computational fluid dynamics modeling approach was applied for metered dose inhaler (MDI) and dry powder inhaler (DPI) aerosols delivered to healthy and constricted airways. The computational fluid dynamics approach included comple...

journal_title：Journal of pharmaceutical sciences

authors： Walenga RL,Longest PW

更新日期：2016-01-01 00:00:00

abstract：:Two polymorphs of the 1:1 fumarate salt of 1,4-diazabicyclo[3.2.2]nonane-4-carboxylic acid 4-bromophenyl ester, developed for the treatment of cognitive symptoms of schizophrenia and Alzheimer disease, have been characterized. The 2 crystal structures have been solved, and their phase relationships have been establish...

journal_title：Journal of pharmaceutical sciences

authors： Robert B,Perrin MA,Barrio M,Tamarit JL,Coquerel G,Ceolin R,Rietveld IB

更新日期：2016-01-01 00:00:00

abstract：:Drugs possessing the ability to bind to melanin-rich tissue, such as the eye, are linked with higher ocular exposure, and therefore have the potential to affect the efficacy and safety profiles of therapeutics. A high-throughput melanin chromatographic affinity assay has been developed and validated, which has allowed...

journal_title：Journal of pharmaceutical sciences

authors： Reilly J,Williams SL,Forster CJ,Kansara V,End P,Serrano-Wu MH

更新日期：2015-12-01 00:00:00

abstract：:This study was designed to assess the effects of cooling rate, storage temperature, and formulation composition on trehalose phase distribution and protein stability in frozen solutions. The data demonstrate that faster cooling rates (>100°C/min) result in trehalose crystallization and protein aggregation as determine...

journal_title：Journal of pharmaceutical sciences

authors： Connolly BD,Le L,Patapoff TW,Cromwell MEM,Moore JMR,Lam P

更新日期：2015-12-01 00:00:00

abstract：:Crystallization of polymorphs still has a touch of art, as even prior observations of polymorphs do not guarantee their crystallization. However, once crystals of various polymorphs have been obtained, their relative stabilities can be established with a straightforward thermodynamic approach even if the conclusion wi...

journal_title：Journal of pharmaceutical sciences

authors： Rietveld IB,Céolin R

更新日期：2015-12-01 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：:Scale up of pan coating process is of high importance to the pharmaceutical and food industry. The number of process variables and their interdependence in a pan coating process can make it a rather complex scale-up problem. This review discusses breaking down the coating process variables into three main categories: ...

journal_title：Journal of pharmaceutical sciences

authors： Agrawal AM,Pandey P

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：:A combination of coformer screening and modeling, followed by characterization using calorimetry, structure elucidation, and solubility led to the identification of novel crystalline forms of the hepatitis C protease inhibitor, telaprevir. The lead crystalline form, a cocrystalline solid of telaprevir with 4-aminosaly...

journal_title：Journal of pharmaceutical sciences

authors： Stavropoulos K,Johnston SC,Zhang Y,Rao BG,Hurrey M,Hurter P,Topp EM,Kadiyala I

更新日期：2015-10-01 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

abstract：:The present study was carried out to investigate the blood-to-retina transport of nicotine across the inner blood-retinal barrier (BRB). Using the in vivo vascular injection method, the blood-to-retina influx clearance of nicotine across the BRB was determined as 131 μL/(min?g retina), which is much higher than that o...

journal_title：Journal of pharmaceutical sciences

authors： Tega Y,Kubo Y,Yuzurihara C,Akanuma S,Hosoya K

更新日期：2015-09-01 00:00:00

abstract：:Since its inception in the 1930s, disintegration testing has become an important quality control (QC) test in pharmaceutical industry, and disintegration test procedures for various dosage forms have been described by the different pharmacopoeias, with harmonization among them still not quite complete. However, becaus...

journal_title：Journal of pharmaceutical sciences

authors： Al-Gousous J,Langguth P

更新日期：2015-09-01 00:00:00

abstract：:Literature and experimental data relevant for the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing levetiracetam are reviewed. Data on solubility and permeability suggest that levetiracetam belongs to class I of the biopharm...

journal_title：Journal of pharmaceutical sciences

authors： Petruševska M,Berglez S,Krisch I,Legen I,Megušar K,Peternel L,Abrahamsson B,Cristofoletti R,Groot DW,Kopp S,Langguth P,Mehta M,Polli JE,Shah VP,Dressman J

更新日期：2015-09-01 00:00:00

abstract：:The oral absorption of drugs has been represented by various concepts such as the absorption potential, the maximum absorbable dose, the biopharmaceutics classification system, and in vitro-in vivo correlation. The aim of this article is to provide an overview of the theoretical relationships between these concepts. I...

journal_title：Journal of pharmaceutical sciences

authors： Sugano K,Terada K

更新日期：2015-09-01 00:00:00

abstract：:Sonication process is regularly adopted for dispersing single-walled carbon nanotubes (SWCNTs) in an aqueous medium. This can be achieved by either covalent functionalization of SWCNTs with strong acid or by noncovalent functionalization using dispersants that adsorb onto the surface of SWCNTs during dispersion. Becau...

journal_title：Journal of pharmaceutical sciences

authors： Koh B,Cheng W

更新日期：2015-08-01 00:00:00

abstract：:Nonionic surfactants (caprylocaproyl macrogol-8 glycerides, octoxynol-12, polysorbate-20, and polyethylene glycol-40 hydrogenated castor oil) (47.03%, w/w), costabilizer (poloxamer 407) (12%-20%, w/w), oil (isopropyl myristate) (5.22%, w/w), water (q.s. ad 100%, w/w), and ibuprofen (5%, w/w) were used to develop oil-i...

journal_title：Journal of pharmaceutical sciences

authors： Djekic L,Martinovic M,Stepanović-Petrović R,Tomić M,Micov A,Primorac M

更新日期：2015-08-01 00:00:00

abstract：:A novel in-line technique utilising pulsed terahertz radiation for direct measurement of the film coating thickness of individual tablets during the coating process was previously developed and demonstrated on a production-scale coater. Here, we use this technique to monitor the evolution of tablet film coating thickn...

journal_title：Journal of pharmaceutical sciences

authors： Lin H,May RK,Evans MJ,Zhong S,Gladden LF,Shen Y,Zeitler JA

更新日期：2015-08-01 00:00:00

abstract：:The objective of this study was to investigate product performance of freeze dried l-arginine/sucrose-based formulations under variation of excipient weight ratios, l-arginine counter ions and formulation pH as a matrix to stabilize a therapeutic monoclonal antibody (MAb) during freeze drying and shelf life. Protein a...

journal_title：Journal of pharmaceutical sciences

authors： Stärtzel P,Gieseler H,Gieseler M,Abdul-Fattah AM,Adler M,Mahler HC,Goldbach P

更新日期：2015-07-01 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：:The tissue:plasma partition coefficients (Kp ) are good indicators of the extent of tissue distribution. Therefore, advanced tissue composition-based models were used to predict the Kp values of drugs under in vivo conditions on the basis of in vitro and physiological input data. These models, however, focus on animal...

journal_title：Journal of pharmaceutical sciences

authors： Poulin P

更新日期：2015-06-01 00:00:00

abstract：:The aim of this study was to investigate the role of porosity on the compression behavior and tablet tensile strength for granules produced by a dry granulation procedure. Microcrystalline cellulose was used as a typical pharmaceutical excipient and a comparison was made with the effect of granule porosity on the comp...

journal_title：Journal of pharmaceutical sciences

authors： Nordström J,Alderborn G

更新日期：2015-06-01 00:00:00

abstract：:Therapeutic antibodies and antibody derivatives comprise the majority of today's biotherapeutics. Routine methods to generate novel antibodies, such as immunization and phage-display, often give rise to several candidates with desired functional properties. On the contrary, resource-intense steps such as the developme...

journal_title：Journal of pharmaceutical sciences

authors： Jarasch A,Koll H,Regula JT,Bader M,Papadimitriou A,Kettenberger H

更新日期：2015-06-01 00:00:00

abstract：:The recently developed hydrogen-bonding propensity tool in the Cambridge Structural Database software package (Mercury) was tested to predict polymorphs. The compounds for the study were chosen from a list of approximately 300 pharmaceutically important compounds, for which multiple crystal forms had not been previous...

journal_title：Journal of pharmaceutical sciences

authors： Nauha E,Bernstein J

更新日期：2015-06-01 00:00:00