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：:Gender and immune status can considerably impact on the pharmacokinetics (PK) of macromolecular and small molecule drugs. However, these effects are often not considered in drug development. We aimed to quantitatively evaluate effects of gender and immune status on the PK of PEGylated interferon in frequently used mur...

journal_title：Journal of pharmaceutical sciences

authors： Landersdorfer CB,Caliph SM,Shackleford DM,Ascher DB,Kaminskas LM

更新日期：2015-05-01 00:00:00

abstract：:Intravenously administered (i.v.) drug-cyclodextrin (CD) inclusion complexes are generally expected to dissociate rapidly and completely, such that the i.v. pharmacokinetic profile of a drug is unchanged in the presence of CD. The altered pharmacokinetics of a synthetic ozonide in rats has been attributed to an unusua...

journal_title：Journal of pharmaceutical sciences

authors： Leong NJ,Prankerd RJ,Shackleford DM,Mcintosh MP

更新日期：2015-04-01 00:00:00

abstract：:The utility of inhaled protein therapeutics to treat lung-resident diseases is limited by protein degradation in the lungs and rapid clearance. This study therefore aimed to evaluate the impact of PEGylation on the lung and systemic exposure of interferon (IFN) α2 after intratracheal administration to rats. An inverse...

journal_title：Journal of pharmaceutical sciences

authors： Mcleod VM,Chan LJ,Ryan GM,Porter CJ,Kaminskas LM

更新日期：2015-04-01 00:00:00

abstract：:Robust higher order structure (HOS) characterization capability and strategy are critical throughout biopharmaceutical development from initial candidate selection and formulation screening to process optimization and manufacturing. This case study describes the utility of several orthogonal HOS methods as investigati...

journal_title：Journal of pharmaceutical sciences

authors： Budyak IL,Doyle BL,Weiss WF 4th

更新日期：2015-04-01 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：:This whitepaper highlights current challenges and opportunities associated with continuous synthesis, workup, and crystallization of active pharmaceutical ingredients (drug substances). We describe the technologies and requirements at each stage and emphasize the different considerations for developing continuous proc...

journal_title：Journal of pharmaceutical sciences

authors： Baxendale IR,Braatz RD,Hodnett BK,Jensen KF,Johnson MD,Sharratt P,Sherlock JP,Florence AJ

更新日期：2015-03-01 00:00:00

abstract：:We describe the key issues and possibilities for continuous final dosage formation, otherwise known as downstream processing or drug product manufacturing. A distinction is made between heterogeneous processing and homogeneous processing, the latter of which is expected to add more value to continuous manufacturing. W...

journal_title：Journal of pharmaceutical sciences

authors： Byrn S,Futran M,Thomas H,Jayjock E,Maron N,Meyer RF,Myerson AS,Thien MP,Trout BL

更新日期：2015-03-01 00:00:00

abstract：:This white paper provides a perspective of the challenges, research needs, and future directions for control systems engineering in continuous pharmaceutical processing. The main motivation for writing this paper is to facilitate the development and deployment of control systems technologies so as to ensure quality of...

journal_title：Journal of pharmaceutical sciences

authors： Myerson AS,Krumme M,Nasr M,Thomas H,Braatz RD

更新日期：2015-03-01 00:00:00

abstract：:The association efficiency of oxytetracycline (OTC) to pharmaceutical available, ionic oil-in-water nanoemulsions is studied. Theoretical mathematical developments allowed us to differentiate by diafiltration (DF) between thermodynamically and kinetically controlled binding of the drug to the nanoemulsions, and relate...

journal_title：Journal of pharmaceutical sciences

authors： Orellana SL,Torres-Gallegos C,Araya-Hermosilla R,Oyarzun-Ampuero F,Moreno-Villoslada I

更新日期：2015-03-01 00:00:00

abstract：:Ethylene oxide (EtO) is widely used in sterilization of drug product primary containers and medical devices. The impact of residual EtO on protein therapeutics is of significant interest in the biopharmaceutical industry. The potential for EtO to modify individual amino acids in proteins has been previously reported. ...

journal_title：Journal of pharmaceutical sciences

authors： Chen L,Sloey C,Zhang Z,Bondarenko PV,Kim H,Ren D,Kanapuram S

更新日期：2015-02-01 00:00:00

abstract：:Upon exposure to shaking stress, an IgG1 mAb formulation in both the liquid and lyophilized state formed subvisible particles. Because freeze-drying was expected to minimize protein physical instability under these conditions, the extent and nature of aggregate formation in the lyophilized preparation were examined us...

journal_title：Journal of pharmaceutical sciences

authors： Telikepalli S,Kumru OS,Kim JH,Joshi SB,O'Berry KB,Blake-Haskins AW,Perkins MD,Middaugh CR,Volkin DB

更新日期：2015-02-01 00:00:00

abstract：:The assessment of provenance of heparin is becoming a major concern for the pharmaceutical industry and its regulatory bodies. Batch-specific [carbon (δ(13) C), nitrogen (δ(15) N), oxygen (δ(18) O), sulfur (δ(34) S), and hydrogen (δD)] stable isotopic compositions of five different animal-derived heparins were perform...

journal_title：Journal of pharmaceutical sciences

authors： Jasper JP,Zhang F,Poe RB,Linhardt RJ

更新日期：2015-02-01 00:00:00

abstract：:Benzyl alcohol (BA) is the most widely used antimicrobial preservative in multidose protein formulations, and has been shown to cause protein aggregation. Our previous work on a model protein cytochrome c demonstrated that this phenomenon occurs via partial unfolding. Here, we examine the validity of these results by ...

journal_title：Journal of pharmaceutical sciences

authors： Bis RL,Singh SM,Cabello-Villegas J,Mallela KM

更新日期：2015-02-01 00:00:00

abstract：:Industry experience suggests that g-forces sustained when vials containing protein formulations are accidentally dropped can cause aggregation and particle formation. To study this phenomenon, a shock tower was used to apply controlled g-forces to glass vials containing formulations of two monoclonal antibodies and re...

journal_title：Journal of pharmaceutical sciences

authors： Randolph TW,Schiltz E,Sederstrom D,Steinmann D,Mozziconacci O,Schöneich C,Freund E,Ricci MS,Carpenter JF,Lengsfeld CS

更新日期：2015-02-01 00:00:00

abstract：:Although PEGylation of biologics is currently the gold standard for half-life extension, the technology has a number of limitations, most importantly the non-biodegradability of PEG and the extremely high viscosity at high concentrations. HESylation is a promising alternative based on coupling to the biodegradable pol...

journal_title：Journal of pharmaceutical sciences

authors： Liebner R,Meyer M,Hey T,Winter G,Besheer A

更新日期：2015-02-01 00:00:00

abstract：:The long serum half-lives of mAbs are conferred by pH-dependent binding of IgG-Fc to the neonatal Fc receptor (FcRn). The Fc region of human IgG1 has three conserved methionine residues, Met252, Met358, and Met428. Recent studies showed oxidation of these Met residues impairs FcRn binding and consequently affects phar...

journal_title：Journal of pharmaceutical sciences

authors： Gao X,Ji JA,Veeravalli K,Wang YJ,Zhang T,Mcgreevy W,Zheng K,Kelley RF,Laird MW,Liu J,Cromwell M

更新日期：2015-02-01 00:00:00

abstract：:Peptide-based therapies have the potential to induce antibody formation if the molecules differ from a native human peptide. Several reports have disclosed the occurrence of antibody generation in a patient treated with exenatide. The immune response can be problematic from a clinical stand point, particularly if the ...

journal_title：Journal of pharmaceutical sciences

authors： Lim SM,Eom HN,Jiang HH,Sohn M,Lee KC

更新日期：2015-01-01 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：:In this study, the adsorption of an IgG1 antibody to siliconized vials was investigated with focus on the formulation parameters pH, ionic strength, and nonionic surfactants. Electrophoretic mobility measurements were performed to investigate the charge characteristics of protein and siliconized glass particles at dif...

journal_title：Journal of pharmaceutical sciences

authors： Höger K,Mathes J,Frieß W

更新日期：2015-01-01 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：:Although significant progress had been made in developing general scale-up rules for an aqueous pan-coating process, there are often scenarios where small-scale experiments are not found to be truly reflective of what may be observed at the large scale. This article reviews some of the methods traditionally used for s...

journal_title：Journal of pharmaceutical sciences

authors： Pandey P,Bindra DS

更新日期：2014-11-01 00:00:00

abstract：:Patients with burn wounds are susceptible to wound infection and sepsis. This research introduces a novel burn wound dressing that contains silver nanoparticles (SNPs) to treat infection in a 2-acrylamido-2-methylpropane sulfonic acid sodium salt (AMPS-Na(+) ) hydrogel. Silver nitrate was dissolved in AMPS-Na(+) solut...

journal_title：Journal of pharmaceutical sciences

authors： Boonkaew B,Barber PM,Rengpipat S,Supaphol P,Kempf M,He J,John VT,Cuttle L

更新日期：2014-10-01 00:00:00

abstract：:Sucrose fatty acid esters are increasingly used as excipients in pharmaceutical products, but few data are available on their toxicity profile, mode of action, and efficacy on intestinal epithelial models. Three water-soluble sucrose esters, palmitate (P-1695), myristate (M-1695), laurate (D-1216), and two reference a...

journal_title：Journal of pharmaceutical sciences

authors： Kiss L,Hellinger É,Pilbat AM,Kittel Á,Török Z,Füredi A,Szakács G,Veszelka S,Sipos P,Ózsvári B,Puskás LG,Vastag M,Szabó-Révész P,Deli MA

更新日期：2014-10-01 00:00:00

abstract：:To explore the possibility of cyclodextrin click clusters (CCCs) as a new cyclodextrin-based excipient, we prepared three different CCCs; heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}-β-cyclodextrin (HT-β-CD), heptakis{6-(4-hydroxymethyl-1H-[1,2,3]triazol-1-yl)-6-deoxy}{2,3-di-O-methyl}-β-cyclodextrin (...

journal_title：Journal of pharmaceutical sciences

authors： Le HT,Jeon HM,Lim CW,Kim TW

更新日期：2014-10-01 00:00:00

abstract：:Solution pH and ionic strength (I) have complex effects on protein stability. We developed an experimental approach based on exploitation of the zwitterionic characteristic of amino acid molecules to probe the relative contribution from each. A variety of types of amino acid solutions were adopted to investigate the e...

journal_title：Journal of pharmaceutical sciences

authors： Zhou R,Nashine V,Palm T,Gandhi R,Adams M

更新日期：2014-10-01 00:00:00

abstract：:Pharmaceutical materials, crystalline and amorphous, sorb water from the atmosphere, which affects critical factors in the development of drugs, such as the selection of drug substance crystal form, compatibility with excipients, dosage form selection, packaging, and product shelf-life. It is common practice to quanti...

journal_title：Journal of pharmaceutical sciences

authors： Sacchetti M

更新日期：2014-09-01 00:00:00

abstract：:(14)N nuclear quadrupole resonance (NQR) in two known polymorphs of famotidine was measured. At room temperature, seven quadrupolar sets of transition frequencies (ν(+), ν(-), and ν(0)) corresponding to seven different nitrogen sites in the crystal structure of each of the two polymorphs were found. This confirms the ...

journal_title：Journal of pharmaceutical sciences

authors： Luźnik J,Pirnat J,Jazbinšek V,Lavrič Z,Žagar V,Srčič S,Seliger J,Trontelj Z

更新日期：2014-09-01 00:00:00

abstract：:The knowledge of physicochemical properties of organic compounds becomes increasingly important in pharmaceutical sciences, chemical engineering, and other fields. In this study, we developed UPPER (Unified Physicochemical Property Estimation Relationships), a comprehensive model for the estimation of 20 physicochemic...

journal_title：Journal of pharmaceutical sciences

authors： Lian B,Yalkowsky SH

更新日期：2014-09-01 00:00:00

abstract：:Blends of polymers with complementary properties hold promise for addressing the diverse, demanding polymer performance requirements in amorphous solid dispersions (ASDs), but we lack comprehensive property understanding for blends of important ASD polymers. Herein, we prepare pairwise blends of commercially available...

journal_title：Journal of pharmaceutical sciences

authors： Marks JA,Wegiel LA,Taylor LS,Edgar KJ

更新日期：2014-09-01 00:00:00

abstract：:The mechanism of how poly(vinyl alcohol-co-acrylic acid-co-methyl methacrylate) (PVA copolymer) stabilizes an amorphous drug was investigated. Solid dispersions of PVA copolymer, poly(vinyl pyrrolidone) (PVP), and poly(vinyl pyrrolidone-co-vinyl acetate) (PVPVA) with indomethacin (IMC) were prepared. The glass transit...

journal_title：Journal of pharmaceutical sciences

authors： Ueda H,Aikawa S,Kashima Y,Kikuchi J,Ida Y,Tanino T,Kadota K,Tozuka Y

更新日期：2014-09-01 00:00:00

abstract：:A confocal Raman microscopic technique was optimized to more efficiently detect amorphous-amorphous phase separation in freeze-dried protein formulations. A Renishaw Raman inVia confocal microscope was used to collect 100-200 μm line maps (2 μm step size) of freeze-dried protein-excipient formulations. At each point a...

journal_title：Journal of pharmaceutical sciences

authors： Forney-Stevens KM,Pelletier MJ,Shalaev EY,Pikal MJ,Bogner RH

更新日期：2014-09-01 00:00:00

abstract：:This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) ...

journal_title：Journal of pharmaceutical sciences

authors： Georgieva D,Kostova B,Ivanova S,Rachev D,Tzankova V,Kondeva-Burdina M,Christova D

更新日期：2014-08-01 00:00:00

abstract：:Photoprotective potential and biological consequences (mutagenic potential) of octyl-dimethyl-PABA (ODP), titanium dioxide (TiO2 ), and montmorillonite (MMT) upon ultraviolet B (UVB) irradiation, alone and in different associations [physical mixtures (PMs)], were evaluated using a Saccharomyces cerevisiae ogg1 mutant ...

journal_title：Journal of pharmaceutical sciences

authors： Paiva JP,Santos BA,Kibwila DM,Gonçalves TC,Pinto AV,Rodrigues CR,Leitão AC,Cabral LM,De Pádula M

更新日期：2014-08-01 00:00:00

abstract：:In this study, injectable microspheres were developed for the local treatment of joint degeneration in rheumatoid arthritis (RA). Microspheres loaded with triamcinolone (TA), a corticosteroid drug, and/or raloxifene (Ral), a cartilage regenerative drug, were prepared with a biodegradable and biocompatible polymer, pol...

journal_title：Journal of pharmaceutical sciences

authors： Ocal Y,Kurum B,Karahan S,Tezcaner A,Ozen S,Keskin D

更新日期：2014-08-01 00:00:00

abstract：:The delamination of glass contact surfaces because of hydrolytic instability has been well documented. However, the lack of glass surface integrity can also lead to other undesirable outcomes prior to visible glass delamination. This work shows how the early stages of delamination, namely, glass corrosion, can influen...

journal_title：Journal of pharmaceutical sciences

authors： Watkins MA,Iacocca RG,Shelbourn TL,Dong X,Stobba-Wiley C

更新日期：2014-08-01 00:00:00

abstract：:Angiogenesis, the sprouting of capillaries from preexisting ones, is essential for the sustained growth of solid tumors. In this study, we used SU5416, a hydrophobic molecule with potent tyrosine kinase inhibitor of type 2 receptor for vascular endothelial growth factor (VEGF), as PEGylated emulsion (SU5416-PE), and e...

journal_title：Journal of pharmaceutical sciences

authors： Ogawara K,Abe S,Un K,Yoshizawa Y,Kimura T,Higaki K

更新日期：2014-08-01 00:00:00

abstract：:Granules prepared by the high shear wet granulation (HSWG) process commonly exhibit the problem of overgranulation, a phenomenon characterized by a severe loss of the ability to form adequately strong tablet. We hypothesize that the incorporation of brittle excipients promotes brittle fracture of granules during compa...

journal_title：Journal of pharmaceutical sciences

authors： Osei-Yeboah F,Zhang M,Feng Y,Sun CC

更新日期：2014-08-01 00:00:00

abstract：:This study was aimed to investigate chemical preactivated thiomers for their potential use in mucosal drug delivery. Thiomers--thiolated polymers--are mucoadhesive polymers with sulfhydryl group-bearing side chains. Thiomers are synthesized by covalent attachment of low molecular mass compounds bearing sulfhydryl grou...

journal_title：Journal of pharmaceutical sciences

authors： Laffleur F,Röggla J,Idrees MA,Griessinger J

更新日期：2014-08-01 00:00:00

abstract：:A model is presented for transdermal drug delivery from single-layered silicone matrix systems. The work is based on our previous results that, in particular, extend the well-known Higuchi model. Recently, we have introduced a numerical transient model describing matrix systems where the drug dissolution can be non-in...

journal_title：Journal of pharmaceutical sciences

authors： Snorradóttir BS,Jónsdóttir F,Sigurdsson ST,Másson M

更新日期：2014-08-01 00:00:00