Design and Synthesis of Polymer Prodrugs for Improving Water-Solubility, Pharmacokinetic Behavior and Antitumor Efficacy of TXA9.

abstract：PURPOSE:The objective of this study was to evaluate the in vivo consequences of glycyl-glutamate coadministration on gabapentin oral absorption. METHODS:Rats were administered gabapentin (10 mg/kg plus radiotracer) by gastric gavage, in the absence and presence of dipeptides, and by intravenous administration. Serial ...

journal_title：Pharmaceutical research

authors： Nguyen TV,Fleisher D,Smith DE

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:To study the reaction of artelinic acid with chemical model systems of cytochrome P-450 as a means of obtaining authentic samples of the putative metabolites necessary for identification of the mammalian metabolites of artelinic acid. METHODS:Artelinic acid was reacted with different organic complexes of iron(...

journal_title：Pharmaceutical research

authors： Idowu OR,Lin AJ,Grace JM,Peggins JO

更新日期：1997-10-01 00:00:00

abstract：PURPOSE:To investigate the possible pathways for transport of wheat germ agglutinin conjugated PEG-PLA nanoparticles (WGA-NP) into the brain after nasal administration. METHODS:The nose-to-brain pathways were investigated using WGA-NP containing 6-coumarin (as a fluorescent marker) and (125)I-labeled WGA-NP. Ex vivo i...

journal_title：Pharmaceutical research

authors： Liu Q,Shen Y,Chen J,Gao X,Feng C,Wang L,Zhang Q,Jiang X

更新日期：2012-02-01 00:00:00

abstract：PURPOSE:To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA. METHODS:Caco-2 monolayers were used to estimate intestinal transport and metabolism of the bis(pivaloyloxymethyl)-ester [bis(POM)-] and a s...

journal_title：Pharmaceutical research

authors： Annaert P,Gosselin G,Pompon A,Benzaria S,Valette G,Imbach JL,Naesens L,Hatse S,de Clercq E,Van den Mooter G,Kinget R,Augustijns P

更新日期：1998-02-01 00:00:00

abstract：PURPOSE:The purpose of this study was to clarify the localization and function of the ATP-binding cassette transporter G2 (ABCG2; BCRP/MXR/ABCP) in retinal capillary endothelial cells, which form the inner blood-retinal barrier, as an efflux transport system. METHODS:The expression was determined by reverse transcript...

journal_title：Pharmaceutical research

authors： Asashima T,Hori S,Ohtsuki S,Tachikawa M,Watanabe M,Mukai C,Kitagaki S,Miyakoshi N,Terasaki T

更新日期：2006-06-01 00:00:00

abstract：:Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized by a number of microorganisms. Large-scale fermentation with Aspergillus niger (ATCC 10549) and Nocardia corallina (ATCC 19070) have resulted in the isolation of four microbial metabolites which have been chara...

journal_title：Pharmaceutical research

authors： Lee IS,ElSohly HN,Hufford CD

更新日期：1990-02-01 00:00:00

abstract：PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...

journal_title：Pharmaceutical research

authors： Craane-van Hinsberg WH,Verhoef JC,Bax LJ,Junginger HE,Boddé HE

更新日期：1995-10-01 00:00:00

abstract：:Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...

journal_title：Pharmaceutical research

authors： Hussain MA,DiLuccio RC,Shefter E,Hurwitz AR

更新日期：1989-12-01 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:Using monolayers of human pancreatic adenocarcinoma cells (Panc-1) that express multidrug resistance-associated protein (MRP), the present work investigates the effects of Pluronic block copolymers on the functional activity of MRP. METHODS:The studies examined the accumulation and efflux of the MRP selective ...

journal_title：Pharmaceutical research

authors： Miller DW,Batrakova EV,Kabanov AV

更新日期：1999-03-01 00:00:00

abstract：:The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...

journal_title：Pharmaceutical research

authors： Leone M,Mönkäre J,Bouwstra JA,Kersten G

更新日期：2017-11-01 00:00:00

abstract：PURPOSE:Penetration enhancers (PEs) enhancing efficacy depends on two processes: PEs release from patches and action on skin. Compared with their action on skin, PEs release process was poorly understood. Therefore, the purpose of this study was to make a mechanistic understanding of PEs release from acrylic pressure-s...

journal_title：Pharmaceutical research

authors： Zeng L,Song W,He W,Zhang J,Wang Y,Bian J,Mao Z,Quan D,Liu J

更新日期：2020-08-13 00:00:00

abstract：PURPOSE:To study the influence of solid form on the behavior of the salt siramesine hydrochloride in aqueous environments. METHODS:The solubilities and dissolution rates of siramesine hydrochloride anhydrate and monohydrate were determined at pH 3.4 and 6.4, and precipitates were examined by X-ray powder diffraction. ...

journal_title：Pharmaceutical research

authors： Zimmermann A,Tian F,Lopez de Diego H,Ringkjøbing Elema M,Rantanen J,Müllertz A,Hovgaard L

更新日期：2009-04-01 00:00:00

abstract：PURPOSE:To characterize factor(s) contained in apical medium of primary cultured rat alveolar epithelial type II cell-like monolayers (RAECM-II) that enhance insulin absorption across alveolar epithelial cells. MATERIALS AND METHODS:Primary rat alveolar epithelial cell monolayers cultured on Transwells in the presence...

journal_title：Pharmaceutical research

authors： Bahhady R,Kim KJ,Borok Z,Crandall ED,Shen WC

更新日期：2007-09-01 00:00:00

abstract：PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...

journal_title：Pharmaceutical research

authors： Monteiro-Riviere NA,Inman AO,Mak V,Wertz P,Riviere JE

更新日期：2001-07-01 00:00:00

abstract：:Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

journal_title：Pharmaceutical research

authors： Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

更新日期：2020-06-03 00:00:00

abstract：PURPOSE:Because interleukin-10 (IL-10) seems a promising new antifibrotic drug, we investigated the pharmacokinetic and biodistribution profile of this potent therapeutic cytokine in rats with extensive liver fibrosis (BDL-3). IL-10 receptor expression was also determined in relation to these aspects. METHODS:To study...

journal_title：Pharmaceutical research

authors： Rachmawati H,Beljaars L,Reker-Smit C,Van Loenen-Weemaes AM,Hagens WI,Meijer DK,Poelstra K

更新日期：2004-11-01 00:00:00

abstract：PURPOSE:In this study, modulation of the immune response against diphtheria toxoid (DT) by various adjuvants in transcutaneous immunization (TCI) with microneedle array pretreatment was investigated. METHODS:TCI was performed on BALB/c mice with or without microneedle array pretreatment using DT as a model antigen co-...

journal_title：Pharmaceutical research

authors： Ding Z,Van Riet E,Romeijn S,Kersten GF,Jiskoot W,Bouwstra JA

更新日期：2009-07-01 00:00:00

abstract：PURPOSE:This study was conducted to assess the pharmacokinetics and pharmacodynamics of 7-nitroindazole (7-NI), a selective inhibitor of neuronal nitric oxide synthase (NOS). METHODS:Male Sprague-Dawley rats were equipped with peritoneal/ venous cannulae and a microdialysis probe in the hippocampal cortex. Rats receiv...

journal_title：Pharmaceutical research

authors： Bush MA,Pollack GM

更新日期：2001-11-01 00:00:00

abstract：:A method of immobilizing urokinase on albumin microspheres has been developed. Laser scattering, which was used to follow particle size from the initial emulsification stage to the final aqueous resuspension of the microsphere stage, showed that particle coalescence and crosslinking were critical parameters in manufac...

journal_title：Pharmaceutical research

authors： Bhargava K,Ando HY

更新日期：1992-06-01 00:00:00

abstract：:An oral formulation of controlled-release isosorbide-5-nitrate pellets has been used to investigate the location of pellets in the gastrointestinal (GI) tract and, in parallel, to measure the drug absorption from these locations. Using the method of gamma scintigraphy the transit times and spreading of pellets in the ...

journal_title：Pharmaceutical research

authors： Fischer W,Boertz A,Davis SS,Khosla R,Cawello W,Sandrock K,Cordes G

更新日期：1987-12-01 00:00:00

abstract：PURPOSE:The objective of this work was to assess, in vitro, the passage of P-glycoprotein dependent drugs across brain capillary endothelial cells, when these drugs are associated with a reversing agent. METHODS:An in vitro model of the blood-brain barrier consisting of a coculture of brain capillary endothelial cells...

journal_title：Pharmaceutical research

authors： Fenart L,Buée-Scherrer V,Descamps L,Duhem C,Poullain MG,Cecchelli R,Dehouck MP

更新日期：1998-07-01 00:00:00

abstract：PURPOSE:This study was aimed to investigate the effects of a phenolic antioxidant, butylated hydroxyanisole (BHA) and its metabolite, tert-butylhydroquinone (tBHQ) on the induction of HO-1, NQO1 and Nrf2 proteins and their regulatory mechanisms in primary-cultured hepatocytes. METHODS:After exposure of BHA and tBHQ to...

journal_title：Pharmaceutical research

authors： Keum YS,Han YH,Liew C,Kim JH,Xu C,Yuan X,Shakarjian MP,Chong S,Kong AN

更新日期：2006-11-01 00:00:00

abstract：PURPOSE:To identify High Molecular Weight Products (HMWP) formed in human insulin formulation during storage. METHODS:Commercial formulation of human insulin was stored at 37°C for 1 year and HMWP was isolated using preparative size exclusion chromatography (SEC) and reverse phase (RP) chromatography. The primary stru...

journal_title：Pharmaceutical research

authors： Hjorth CF,Hubálek F,Andersson J,Poulsen C,Otzen D,Naver H

更新日期：2015-06-01 00:00:00

abstract：PURPOSE:The development of a new two-dimensional (2D) model to predict follicular permeation, with integration into a recently reported multi-scale model of transdermal permeation is presented. METHODS:The follicular pathway is modelled by diffusion in sebum. The mass transfer and partition properties of solutes in li...

journal_title：Pharmaceutical research

authors： Kattou P,Lian G,Glavin S,Sorrell I,Chen T

更新日期：2017-10-01 00:00:00

abstract：:Nucleoside transporters play a critical role in the absorption, disposition, and targeting of therapeutically used nucleosides and nucleoside analogs. This review is focused on the Na(+)-dependent, concentrative nucleoside transporters which are found in a variety of cells including renal, intestinal and hepatic epith...

journal_title：Pharmaceutical research

authors： Wang J,Schaner ME,Thomassen S,Su SF,Piquette-Miller M,Giacomini KM

更新日期：1997-11-01 00:00:00

abstract：PURPOSE:We investigated optimum formulation characteristics in the nasal absorption of salmon calcitonin (sCT) by incorporation of acylcarnitines. METHODS:Nasal sCT formulations were administered to anesthetized rats. Plasma calcium level was measured and pharmacological bioavailability (P.bioav) was calculated. RESU...

journal_title：Pharmaceutical research

authors： Kagatani S,Shinoda T,Fukui M,Ohmura T,Hasumi S,Sonobe T

更新日期：1996-05-01 00:00:00

abstract：PURPOSE:The present investigation describes a formulative study for the development of innovative drug delivery systems for bromocriptine. METHODS:Solid lipid nanoparticles (SLN) based on different lipidic components have been produced and characterized. Morphology and dimensional distribution have been investigated b...

journal_title：Pharmaceutical research

authors： Esposito E,Fantin M,Marti M,Drechsler M,Paccamiccio L,Mariani P,Sivieri E,Lain F,Menegatti E,Morari M,Cortesi R

更新日期：2008-07-01 00:00:00

abstract：PURPOSE:The aim of this work was to investigate the influence of the oily nucleus composition on physico-chemical properties and anesthetic activity of poly (lactide-co-glycolide) nanocapsules with benzocaine. METHODS:Nanocapsules containing benzocaine were prepared with three different oily nucleus composition and ch...

journal_title：Pharmaceutical research

authors： de Melo NF,Grillo R,Guilherme VA,de Araujo DR,de Paula E,Rosa AH,Fraceto LF

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:Following extracellular drug clearance, we analyzed the rate of doxorubicin efflux from the nucleus of three human leukemic cells (K562, Molt4 and CCRF-CEM) and related it to their differential sensitivity to this drug, after a short drug pulse. RESULTS:For many pulse-chase regimes, K562 cell viability was lea...

journal_title：Pharmaceutical research

authors： Chen VY,Posada MM,Zhao L,Rosania GR

更新日期：2007-11-01 00:00:00