Emerging topics in structure-based virtual screening.

abstract：PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...

journal_title：Pharmaceutical research

authors： Liang R,Li X,Zhang R,Shi Y,Wang A,Chen D,Sun K,Liu W,Li Y

更新日期：2014-08-01 00:00:00

abstract：PURPOSE:Development of a human mitochondrial gene delivery vector is a critical step in the ability to treat diseases arising from mutations in mitochondrial DNA. Although we have previously cloned the mouse mitochondrial genome in its entirety and developed it as a mitochondrial gene therapy vector, the human mitochon...

journal_title：Pharmaceutical research

authors： Bigger BW,Liao AY,Sergijenko A,Coutelle C

更新日期：2011-11-01 00:00:00

abstract：:Celiac disease (CD) is an immune-mediated enteropathy triggered by the ingestion of gluten-containing grains that affects ~1% of the white ethnic population. In the last decades, a rise in prevalence of CD has been observed that cannot be fully explained by improved diagnostics. Genetic predisposition greatly influenc...

journal_title：Pharmaceutical research

authors： Matoori S,Fuhrmann G,Leroux JC

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...

journal_title：Pharmaceutical research

authors： Schmidt ST,Neustrup MA,Harloff-Helleberg S,Korsholm KS,Rades T,Andersen P,Christensen D,Foged C

更新日期：2017-08-01 00:00:00

abstract：PURPOSE:Basal insulins with improved kinetic properties can potentially be produced using acylation by fatty acids that enable soluble, high-molecular weight complexes to form post-injection. A series of insulins, acylated at B29 with fatty acids via glutamic acid spacers, were examined to deduce the structural require...

journal_title：Pharmaceutical research

authors： Jonassen I,Havelund S,Hoeg-Jensen T,Steensgaard DB,Wahlund PO,Ribel U

更新日期：2012-08-01 00:00:00

abstract：:A method for determination of absorption rate and bioavailability was developed to reduce the influence of intraindividual variability and applied to the absolute intraperitoneal availability of lithium in the rat. In this method the test and the reference doses are given with a few hours' interval, and the resulting ...

journal_title：Pharmaceutical research

authors： Karlsson MO,Bredberg U

更新日期：1989-09-01 00:00:00

abstract：PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...

journal_title：Pharmaceutical research

authors： Louey MD,Van Oort M,Hickey AJ

更新日期：2004-07-01 00:00:00

abstract：PURPOSE:To design, synthesize, and test synthetic glycopeptide-based delivery systems for gene targeting to hepatocytes by systemic administration. METHODS:All peptides were synthesized by the solid phase method developed using Fmoc chemistry on a peptide synthesizer. The binding of galactosylated peptides to HepG2 ce...

journal_title：Pharmaceutical research

authors： Anwer K,Logan M,Tagliaferri F,Wadhwa M,Monera O,Tung CH,Chen W,Leonard P,French M,Proctor B,Wilson E,Singhal A,Rolland A

更新日期：2000-04-01 00:00:00

abstract：:Assessment of bioavailability/bioequivalence generally relies on the comparison of rate and extent of drug absorption between products. Rate of absorption is commonly expressed by peak concentration (C(max)) and time to peak concentration (T(max)), although these parameters are indirect measures of absorption rate. Re...

journal_title：Pharmaceutical research

authors： Chen ML,Davit B,Lionberger R,Wahba Z,Ahn HY,Yu LX

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:The gastric mucoadhesive property of tetracycline-sucralfate acidic complex (CO) was evaluated by using a novel method in vitro to compare with the in vivo test. The mucoadhesive mechanism of the acidic complex was also studied. METHODS:The gastric mucosa removed from a rat was placed covering the end of a plu...

journal_title：Pharmaceutical research

authors： Higo S,Ori K,Takeuchi H,Yamamoto H,Hino T,Kawashima Y

更新日期：2004-03-01 00:00:00

abstract：:Sulfasalazine, 60 mg/kg, was administered orally to groups of rats (n = 4) along with 1, 5, or 10 mg/kg of riboflavin. Plasma and urine were assayed for 5-aminosalicylic acid, acetyl-5-aminosalicylic acid, sulfapyridine, and acetyl-sulfapyridine using an HPLC method. The mean percent of dose recovered as total metabol...

journal_title：Pharmaceutical research

authors： Chungi VS,Dittert LW,Shargel L

更新日期：1989-12-01 00:00:00

abstract：PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...

journal_title：Pharmaceutical research

authors： Chen H,Zhang Z,Almarsson O,Marier JF,Berkovitz D,Gardner CR

更新日期：2005-03-01 00:00:00

abstract：:A procedure is described that is suitable for the radioimmunoassay (RIA) of 9-[(l,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) in plasma or serum at concentrations as low as 0.7 ng/ml (2.75 × 10(-9) M). Antiserum was prepared by coupling DHPG monohemisuccinate to bovine serum albumin and immunizing rabbits with the re...

journal_title：Pharmaceutical research

authors： Nerenberg C,McClung S,Martin J,Fass M,La Fargue J,Kushinsky S

更新日期：1986-04-01 00:00:00

abstract：:In order to study the influence of hydrogen bonding in the amide backbone of a peptide on permeability across a cell membrane, a series of tetrapeptide analogues was prepared from D-phenylalanine. The amide nitrogens in the parent oligomer were sequentially methylated to give a series containing from one to four methy...

journal_title：Pharmaceutical research

authors： Conradi RA,Hilgers AR,Ho NF,Burton PS

更新日期：1992-03-01 00:00:00

abstract：:The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...

journal_title：Pharmaceutical research

authors： Colthorpe P,Farr SJ,Smith IJ,Wyatt D,Taylor G

更新日期：1995-03-01 00:00:00

abstract：PURPOSE:The purpose of this study was to investigate the delivery of itraconazole (ITZ) particles to a murine lung model by nebulization. METHODS:Three ITZ formulations were prepared and characterized in the dry state using contact angle, dissolution, X-ray powder diffraction, scanning electron microscopy, and Brunaue...

journal_title：Pharmaceutical research

authors： McConville JT,Overhoff KA,Sinswat P,Vaughn JM,Frei BL,Burgess DS,Talbert RL,Peters JI,Johnston KP,Williams RO 3rd

更新日期：2006-05-01 00:00:00

abstract：PURPOSE:The blood-brain barrier (BBB) essentially restricts therapeutic drugs from entering into the brain. This study tests the hypothesis that brain endothelial cell derived exosomes can deliver anticancer drug across the BBB for the treatment of brain cancer in a zebrafish (Danio rerio) model. MATERIALS AND METHODS...

journal_title：Pharmaceutical research

authors： Yang T,Martin P,Fogarty B,Brown A,Schurman K,Phipps R,Yin VP,Lockman P,Bai S

更新日期：2015-06-01 00:00:00

abstract：:Losartan, an antihypertensive agent in clinical development, was found to exist in two enantiotropic polymorphic forms, a low-temperature stable form (Form I) and a high-temperature stable form (Form II), the temperatures at which they are stable being related to the transition temperature. X-ray powder diffraction pa...

journal_title：Pharmaceutical research

authors： Raghavan K,Dwivedi A,Campbell GC Jr,Johnston E,Levorse D,McCauley J,Hussain M

更新日期：1993-06-01 00:00:00

abstract：PURPOSE:The aim was to evaluate fluorescent molecular rotors (DCVJ and CCVJ), which are mainly sensitive to viscosity, for the characterization of polysorbate-containing IgG formulations and compare them to the polarity-sensitive dyes ANS, Bis-ANS and Nile Red. METHODS:IgG formulations with polysorbate 20 or 80 were s...

journal_title：Pharmaceutical research

authors： Hawe A,Filipe V,Jiskoot W

更新日期：2010-02-01 00:00:00

abstract：PURPOSE:To characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of a new polyethylene glycol (PEG) conjugate formulation of interferon (IFN)-beta la following subcutaneous (SC) administration in monkeys. METHODS:Single SC injections of 0.3, 1, and 3 million international units (MIU)/kg of PEG-IFN-beta 1...

journal_title：Pharmaceutical research

authors： Mager DE,Neuteboom B,Jusko WJ

更新日期：2005-01-01 00:00:00

abstract：PURPOSE:To investigate the effect of atomization conditions on particle size and stability of spray-freeze dried protein. METHODS:Atomization variables were explored for excipient-free (no zinc added) and zinc-complexed bovine serum albumin (BSA). Particle size was measured by laser diffraction light scattering follow...

journal_title：Pharmaceutical research

authors： Costantino HR,Firouzabadian L,Hogeland K,Wu C,Beganski C,Carrasquillo KG,Córdova M,Griebenow K,Zale SE,Tracy MA

更新日期：2000-11-01 00:00:00

abstract：PURPOSE:To identify the mechanism behind the unexpected bio-performance of two amorphous solid dispersions: BMS-A/PVP-VA and BMS-A/HPMC-AS. METHODS:Solubility of crystalline BMS-A in PVP-VA and HPMC-AS was measured by DSC. Drug-polymer interaction parameters were obtained by Flory-Huggins model fitting. Drug dissoluti...

journal_title：Pharmaceutical research

authors： Qian F,Wang J,Hartley R,Tao J,Haddadin R,Mathias N,Hussain M

更新日期：2012-10-01 00:00:00

abstract：PURPOSE:The possibility of direct delivery of steroids through the skin to the trachea and the effect of iontophoresis on delivery efficacy were evaluated after the application of an ionic steroidal prodrug, prednisolone sodium succinate (PS-Na), to the throat skin. METHODS:Fluorescein sodium salt (FL-Na) and PS-Na we...

journal_title：Pharmaceutical research

authors： Ishii H,Suzuki T,Todo H,Kamimura M,Sugibayashi K

更新日期：2011-04-01 00:00:00

abstract：PURPOSE:To evaluate 26 marketed oncology drugs for time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes. Evaluate TDI-positive drugs for potential to generate reactive intermediates. Assess clinical drug-drug interaction (DDI) risk using static mechanistic models. METHODS:Human liver microsomes and CYP-spe...

journal_title：Pharmaceutical research

authors： Kenny JR,Mukadam S,Zhang C,Tay S,Collins C,Galetin A,Khojasteh SC

更新日期：2012-07-01 00:00:00

abstract：PURPOSE:To evaluate the mechanism of renal transport of quinolone antibacterial drugs, we examined the interaction of levofloxacin with p-aminohippurate (PAH) transport systems and the transport of levofloxacin in renal epithelial cells. METHODS:Transport of [14C]PAH or [14C]levofloxacin was measured using OK cell mon...

journal_title：Pharmaceutical research

authors： Matsuo Y,Yano I,Habu Y,Katsura T,Hashimoto Y,Inui K

更新日期：2001-05-01 00:00:00

abstract：PURPOSE:To develop a new technique, spray freeze drying, for preparing protein aerosol powders. Also, to compare the spray freeze-dried powders with spray-dried powders in terms of physical properties and aerosol performance. METHODS:Protein powders were characterized using particle size analysis, thermogravimetric an...

journal_title：Pharmaceutical research

authors： Maa YF,Nguyen PA,Sweeney T,Shire SJ,Hsu CC

更新日期：1999-02-01 00:00:00

abstract：PURPOSE:A novel bioequivalence limit is proposed taking into account the therapeutic window. METHODS:The therapeutic range is introduced as the ratios maximum tolerated dose/therapeutic dose (MTD/D) and the therapeutic dose/lowest effective dose. The performance of the new acceptance range was compared with the method...

journal_title：Pharmaceutical research

authors： Jacobs T,De Ridder F,Rusch S,Van Peer A,Molenberghs G,Bijnens L

更新日期：2008-11-01 00:00:00

abstract：:Polymeric biomaterials have extensively been used in medicinal applications. However, factors that determine their biocompatibility are still not very clear. This article reviews various effects of the chemical structure and the surface properties of polymeric biomaterials on their biocompatibility, including protein ...

journal_title：Pharmaceutical research

authors： Wang YX,Robertson JL,Spillman WB Jr,Claus RO

更新日期：2004-08-01 00:00:00

abstract：:The transient dynamic swelling and dissolution behavior during the release of a growth hormone releasing peptide, [D-Trp2-D-Phe5]GHRP, from erodible, non-cross-linked poly(methyl methacrylate-co-methacrylic acid) (PMMA/MAA) beads has been investigated at pH 7.4 as a function of buffer concentration. Although the swell...

journal_title：Pharmaceutical research

authors： Lee PI

更新日期：1993-07-01 00:00:00

abstract：PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...

journal_title：Pharmaceutical research

authors： Tomar DS,Singh SK,Li L,Broulidakis MP,Kumar S

更新日期：2018-08-20 00:00:00