Delivery of HSP90 Inhibitor Using Water Soluble Polymeric Conjugates with High Drug Payload.

abstract：PURPOSE:The aim was to investigate the influence of polymer content and molecular weight on the morphology and heat- and moisture-induced transformations, as indicators of stability, of spray-dried composite particles of amorphous lactose and poly(vinylpyrrolidone) (PVP). METHODS:Amorphous lactose and composite partic...

journal_title：Pharmaceutical research

authors： Berggren J,Alderborn G

更新日期：2003-07-01 00:00:00

abstract：PURPOSE:To develop an isolated perfused rat liver (IPRL) model with low baseline levels of tumor necrosis factor (TNF)-alpha in the outlet perfusate to study the effects of immunostimulants and immunosuppressants on the release of TNF-alpha from this organ. METHODS:Isolated rat livers were perfused with a buffer conta...

journal_title：Pharmaceutical research

authors： Mehvar R,Zhang X

更新日期：2002-01-01 00:00:00

abstract：PURPOSE:Study the radiolysis of solid-state metoclopramide hydrochloride at various absorbed doses. Elucidate the structure of the degradation products to gain information on the radiolysis mechanisms. METHODS:Solid-state metoclopramide samples were irradiated at several doses with gamma rays and high-energy electrons...

journal_title：Pharmaceutical research

authors： Maquille A,Slegers C,Habib JL,Tilquin B

更新日期：2006-06-01 00:00:00

abstract：PURPOSE:In vitro and in vivo permeation studies were conducted to evaluate the characteristic of percutaneous administration of high hydrophilic drug L-carnitine (LC) by Functional MicroArray (FMA) painless intradermal delivery system. METHODS:In vitro study was designed to assess the effects of various skins, donor c...

journal_title：Pharmaceutical research

authors： Zhang S,Qin G,Wu Y,Gao Y,Qiu Y,Li F,Xu B

更新日期：2011-01-01 00:00:00

abstract：:Indomethacin microspheres based on a combination of ethylcellulose and polyethyleneglycol were prepared using the solvent evaporation process. Release profiles of ensemble and individual microspheres were measured. Both were found to follow first-order kinetics, in contrast to what was expected. This was attributed to...

journal_title：Pharmaceutical research

authors： Benita S,Babay D,Hoffman A,Donbrow M

更新日期：1988-03-01 00:00:00

abstract：PURPOSE:To develop a semi-mechanistic population pharmacokinetic model based on gastric emptying function for acetaminophen plasma concentration in critically ill patients tolerant and intolerant to enteral nutrition before and after prokinetic therapy. METHODS:Acetaminophen plasma concentrations were available from a...

journal_title：Pharmaceutical research

authors： Ogungbenro K,Vasist L,Maclaren R,Dukes G,Young M,Aarons L

更新日期：2011-02-01 00:00:00

abstract：PURPOSE:To test the hypothesis that modification of release pattern of nonsteroidal anti-inflammatory drugs (NSAIDs) formulations shifts gastrointestinal (GI) toxicity of the drugs from the upper GI region to the distal intestine. METHODS:We assessed tiaprofenic acid (TA)-induced upper and lower increased GI permeabil...

journal_title：Pharmaceutical research

authors： Vakily M,Khorasheh F,Jamali F

更新日期：1999-01-01 00:00:00

abstract：PURPOSE:We examined the ability of a protein transduction domain (PTD), YARA, to penetrate in the skin and carry a conjugated peptide, P20. The results with YARA were compared to those of a well-known PTD (TAT) and a control, nontransducing peptide (YKAc). The combined action of PTDs and lipid penetration enhancers was...

journal_title：Pharmaceutical research

authors： Lopes LB,Brophy CM,Furnish E,Flynn CR,Sparks O,Komalavilas P,Joshi L,Panitch A,Bentley MV

更新日期：2005-05-01 00:00:00

abstract：PURPOSE:To create poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), where a drug-encapsulating NP core is covered with polyethylene glycol (PEG) in a normal condition but exposes a cell-interactive TAT-modified surface in an environment rich in matrix metalloproteinases (MMPs). METHODS:PLGA NPs were modified w...

journal_title：Pharmaceutical research

authors： Gullotti E,Park J,Yeo Y

更新日期：2013-08-01 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：: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:Levofloxacin, a quinolone antibacterial drug, is a zwitterion at physiological pH. We examined the effect of cationic and anionic drugs on renal excretion of levofloxacin by means of in vivo clearance to characterize the mechanisms of renal excretion of this drug. METHODS:In vivo clearance was studied in male ...

journal_title：Pharmaceutical research

authors： Yano I,Ito T,Takano M,Inui K

更新日期：1997-04-01 00:00:00

abstract：PURPOSE:The purpose of this work was to study the influence of cell differentiation on the mRNA expression of transporters and channels in Caco-2 cells and to assess Caco-2 cells as a model for carrier-mediated drug transport in the intestines. METHOD:Gene mRNA expression was measured using a custom-designed microarra...

journal_title：Pharmaceutical research

authors： Anderle P,Rakhmanova V,Woodford K,Zerangue N,Sadée W

更新日期：2003-01-01 00:00:00

abstract：:The mechanism of release from sustained-release adinazolam mesylate tablets was assessed by the Higuchi equation and by analysis of drug release profiles through 60% released using the Peppas equation. Computed values of the diffusional exponent, n, ranged from 0.59 to 0.66. Values of n in this range are consistent wi...

journal_title：Pharmaceutical research

authors： Skoug JW,Borin MT,Fleishaker JC,Cooper AM

更新日期：1991-12-01 00:00:00

abstract：PURPOSE:To investigate whether conjunctival epithelial cells express transport processes for opioid peptides. METHODS:We monitored the uptake of [(3)H]deltorphin II and [(3)H]DADLE, two hydrolysis-resistant synthetic opioid peptides, in the rabbit conjunctival epithelial cell line CJVE and elucidated the characteristi...

journal_title：Pharmaceutical research

authors： Ananth S,Karunakaran S,Martin PM,Nagineni CN,Hooks JJ,Smith SB,Prasad PD,Ganapathy V

更新日期：2009-05-01 00:00:00

abstract：PURPOSE:Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS:Several bile acid derivatives were screened b...

journal_title：Pharmaceutical research

authors： Jeon OC,Hwang SR,Al-Hilal TA,Park JW,Moon HT,Lee S,Park JH,Byun Y

更新日期：2013-04-01 00:00:00

abstract：:We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...

journal_title：Pharmaceutical research

authors： Powell MF,Magill A,Chu N,Hama K,Mau CI,Foster L,Bergstrom R

更新日期：1991-11-01 00:00:00

abstract：PURPOSE:To develop a semi-distributed liver model for the evaluation of saturable sinusoidal uptake and binding kinetics of the Oatp1a4 substrate digoxin. METHODS:In the perfused rat liver, two successive digoxin doses of 42 and 125 microg were administered, and the outflow concentration was determined by LC/MS/MS. [1...

journal_title：Pharmaceutical research

authors： Weiss M,Li P,Roberts MS

更新日期：2010-09-01 00:00:00

abstract：:A colorless, parallelepiped crystal of methyl (2R,3S)-N-benzoyl-3-phenylisoserinate belonging to the space group P2(1) with a = 5.414(4), b = 7.813(1), c = 17.802(7) A, beta = 90.87(4) degrees, Z = 2, V = 752.9 A3, Dcalc = 1.32 g cm-3, and mu calc = 1.02 cm-1 was selected and the structure solved using direct methods....

journal_title：Pharmaceutical research

authors： Peterson JR,Do HD,Rogers RD

更新日期：1991-07-01 00:00:00

abstract：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...

journal_title：Pharmaceutical research

authors： Kipp JE,Hlavaty JJ

更新日期：1991-05-01 00:00:00

abstract：:Intranasal route continues to be one of the main focuses of drug delivery research. Although it is generally perceived that the nasal route could avoid the first-pass metabolism in liver and gastrointestinal tract, the role of metabolic conversions in systemic and brain-targeted deliveries of the parent compounds and ...

journal_title：Pharmaceutical research

authors： Wong YC,Zuo Z

更新日期：2010-07-01 00:00:00

abstract：PURPOSE:To study the impact of different process conditions and formulation compositions on metastable mannitol forms in protein formulations during lyophilization. METHODS:Mannitol was studied with and without other formulation components. A cryostage was used to mimic the different processing steps during lyophiliza...

journal_title：Pharmaceutical research

authors： Cao W,Xie Y,Krishnan S,Lin H,Ricci M

更新日期：2013-01-01 00:00:00

abstract：PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...

journal_title：Pharmaceutical research

authors： Han S,Hu L,Quach T,Simpson JS,Trevaskis NL,Porter CJ

更新日期：2015-05-01 00:00:00

abstract：PURPOSE:Since the adoption of highly active antiretroviral therapy, HIV disease progression has slowed across the world; however, patients are often required to take multiple medications daily of poorly bioavailable drugs via the oral route, leading to gastrointestinal irritation. Recently, long acting antiretroviral i...

journal_title：Pharmaceutical research

authors： Collier MA,Gallovic MD,Bachelder EM,Sykes CD,Kashuba A,Ainslie KM

更新日期：2016-08-01 00:00:00

abstract：:Human monocytes/macrophages (MO/MAC) were isolated from peripheral blood and cultivated on hydrophobic Teflon membranes. This culture system is suitable for HIV infection of MO/MAC in vitro. After transfer into 24-well plates the mature macrophages (infected or uninfected) were used for measurements of phagocytosis. T...

journal_title：Pharmaceutical research

authors： Schäfer V,von Briesen H,Andreesen R,Steffan AM,Royer C,Tröster S,Kreuter J,Rübsamen-Waigmann H

更新日期：1992-04-01 00:00:00

abstract：PURPOSE:Generation of valuable information about the biphasic geometrical configuration of porcine stratum corneum from Very Small Angle Neutron Scattering (VSANS) data and investigation of its effect on the corresponding effective diffusivity. METHODS:Spectra of porcine stratum corneum are mathematically transformed ...

journal_title：Pharmaceutical research

authors： Charalambopoulou GC,Karamertzanis P,Kikkinides ES,Stubos AK,Kanellopoulos NK,Papaioannou AT

更新日期：2000-09-01 00:00:00

abstract：PURPOSE:To develop an efficient tumor vasculature-targeted polymeric micelle delivery system for combretastatin A4 (CA4), a novel antivascular agent. METHODS:CA4-loaded micelles were prepared from poly (ethylene glycol)-b-poly (d, l-lactide) copolymers. RGD peptides that target integrins alphavbeta3 and alphavbeta5, m...

journal_title：Pharmaceutical research

authors： Wang Y,Yang T,Wang X,Wang J,Zhang X,Zhang Q

更新日期：2010-09-01 00:00:00

abstract：PURPOSE:We describe the AERX aerosol delivery system, a new, bolus inhalation device that is actuated at preprogrammed values of inspiratory flow rate and inhaled volume. We report on its in vitro characterization using a particular set of conditions used in pharmacokinetic and scintigraphic studies. METHODS:Multiple ...

journal_title：Pharmaceutical research

authors： Schuster J,Rubsamen R,Lloyd P,Lloyd J

更新日期：1997-03-01 00:00:00

abstract：PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...

journal_title：Pharmaceutical research

authors： Lederhofer J,van Lent J,Bhoelan F,Karneva Z,de Haan A,Wilschut JC,Stegmann T

更新日期：2018-07-03 00:00:00

abstract：PURPOSE:Several phenomena in tablets indicate that an inhomogeneous pore distribution is formed during the compaction process. Examples are lamination and the capping of corners. In order to gain an understanding of the relation between structure and compact properties, analyzing the structure in a location dependent m...

journal_title：Pharmaceutical research

authors： Wu YS,Frijlink HW,van Vliet LJ,Stokroos I,van der Voort Maarschalk K

更新日期：2005-08-01 00:00:00