Uptake of colchicine, a microtubular system disrupting agent, by isolated rat hepatocytes.

abstract：PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...

journal_title：Pharmaceutical research

authors： Manaspon C,Nasongkla N,Chaimongkolnukul K,Nittayacharn P,Vejjasilpa K,Kengkoom K,Boongird A,Hongeng S

更新日期：2016-12-01 00:00:00

abstract：PURPOSE:(i) To use trehalose as a model compound to evaluate the concept of crystallinity in pharmaceuticals. (ii) To understand the structural nature of dehydrated trehalose dihydrate. MATERIALS AND METHODS:Trehalose dihydrate was dehydrated isothermally at several temperatures below 100 degrees C and the anhydrous p...

journal_title：Pharmaceutical research

authors： Rani M,Govindarajan R,Surana R,Suryanarayanan R

更新日期：2006-10-01 00:00:00

abstract：OBJECTIVE:The objective of this work was to determine plasma protein adsorption and macrophage phagocytosis of biodegradable polyanhydride, polylactic acid and polylactic-co-glycolic acid microspheres prepared by both spray-drying and solvent evaporation techniques. METHODS:Microspheres were characterized by scanning ...

journal_title：Pharmaceutical research

authors： Lacasse FX,Filion MC,Phillips NC,Escher E,McMullen JN,Hildgen P

更新日期：1998-02-01 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：PURPOSE:To identify the molecules responsible for amyloid beta-peptide (1-40) (Abeta(1-40)) uptake by the liver, which play a major role in the systemic clearance of Abeta(1-40). METHODS:The liver uptake index method was used to examine the mechanisms of Abeta(1-40) uptake by the liver in vivo. RESULTS:[125I]Abeta(1-...

journal_title：Pharmaceutical research

authors： Tamaki C,Ohtsuki S,Iwatsubo T,Hashimoto T,Yamada K,Yabuki C,Terasaki T

更新日期：2006-07-01 00:00:00

abstract：PURPOSE:Evidence suggests that uremic toxins such as hippurate (HA), indoleacetate (IA), indoxyl sulfate (IS), and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF) promote the progression of renal failure by damaging tubular cells via rat organic anion transporter 1 (rOat1) and rOat3 on the basolateral membrane of ...

journal_title：Pharmaceutical research

authors： Deguchi T,Kouno Y,Terasaki T,Takadate A,Otagiri M

更新日期：2005-04-01 00:00:00

abstract：PURPOSE:The main goal of this research was to assess the mechanical properties of APIs' polymorphic forms at the single-crystal level (piroxicam, famotidine, nifedipine, olanzapine) in order to predict their bulk deformational attributes, which are critical for some pharmaceutical technology processes. METHODS:The mec...

journal_title：Pharmaceutical research

authors： Egart M,Janković B,Lah N,Ilić I,Srčič S

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:To investigate the effect of benzofusion on NO donor properties and related biological activities of the furoxan system. The biological properties considered were the ability to increase the cytosolic levels of cGMP in C6 cells and vasodilation. METHODS:NO donor properties were investigated either in the prese...

journal_title：Pharmaceutical research

authors： Medana C,Di Stilo A,Visentin S,Fruttero R,Gasco A,Ghigo D,Bosia A

更新日期：1999-06-01 00:00:00

abstract：PURPOSE:The objective of this study was to determine the influence of the peptide bond with emphasis on the carbonyl group on the interaction with and transport by the intestinal small-peptide carrier. Therefore enalapril, a known substrate for the small-peptide carrier, has been modified to an analogue with a reduced ...

journal_title：Pharmaceutical research

authors： Schoenmakers RG,Stehouwer MC,Tukker JJ

更新日期：1999-01-01 00:00:00

abstract：:Lecithin-stabilized triglyceride emulsions are subject to hydrolysis by pancreatic lipase. The time profiles of these reactions are characterized by a lag-phase and a zero-order phase. Lag phases are more pronounced with long-chain triglycerides. Ca2+ is effective in reducing the lag-phase and activating lipase. Kinet...

journal_title：Pharmaceutical research

authors： Alvarez FJ,Stella VJ

更新日期：1989-06-01 00:00:00

abstract：PURPOSE:To compare the systemic delivery of deslorelin following intratracheal administration of different deslorelin formulations. The formulations included dry powders of deslorelin, large-porous deslorelin-poly(lactide-co-glycolide) (PLGA) particles, and small conventional deslorelin-PLGA particles. Also, solution f...

journal_title：Pharmaceutical research

authors： Koushik K,Dhanda DS,Cheruvu NP,Kompella UB

更新日期：2004-07-01 00:00:00

abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

journal_title：Pharmaceutical research

authors： Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

更新日期：1994-10-01 00:00:00

abstract：PURPOSE:The purpose of this study was to determine the existence of insulin-degrading enzyme (EC 3.4.22.11) (IDE) in rat intestinal enterocytes. METHODS:Subcellular fractionation, biochemical characterization, immunoprecipitation, and western blots were employed. RESULTS:Insulin-degrading activity was localized in th...

journal_title：Pharmaceutical research

authors： Bai JP,Chang LL

更新日期：1995-08-01 00:00:00

abstract：PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...

journal_title：Pharmaceutical research

authors： Ravichandran E,Janardhanan P,Patel K,Riding S,Cai S,Singh BR

更新日期：2016-03-01 00:00:00

abstract：PURPOSE:Mannosylation of vaccines is a promising strategy to selectively target vaccine antigens to the mannose receptor expressed on dendritic cells (DCs). The purpose of this study was to investigate the effect of mannan (MN) chemically conjugated to poly(D, L-lactide-co-glycolic acid) (PLGA) nanoparticles (NPs) on a...

journal_title：Pharmaceutical research

authors： Hamdy S,Haddadi A,Shayeganpour A,Samuel J,Lavasanifar A

更新日期：2011-09-01 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:We have evaluated a new process, involving solution-enhanced dispersion by supercritical fluids (SEDS), for the production of polymeric microparticles. METHODS:The biodegradable polymers, Poly (DL-lactide-co-glycolide): copolymer composition 50:50 (DL-PLG), Poly (L-lactide) (L-PLA), Poly (DL-lactide) (DL-PLA) ...

journal_title：Pharmaceutical research

authors： Ghaderi R,Artursson P,Carlfors J

更新日期：1999-05-01 00:00:00

abstract：:Transport studies using intestinal brush-border membrane vesicles isolated from rats and rabbits have failed to demonstrate proton- or Na(+)-dependent carrier-mediated transport of thyrotropin-releasing hormone (TRH), despite a pharmacologically relevant oral bioavailability. To examine the hypothesis that reported le...

journal_title：Pharmaceutical research

authors： Thwaites DT,Hirst BH,Simmons NL

更新日期：1993-05-01 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:Simple uncoated compressed tablets with a central hole (donut-shape) are proposed to provide a constant drug release over a long period of time (> 20 hrs). The effect of hole size and drug solubility on the release kinetics is investigated. METHODS:The donut-shaped polyethylene oxide (PEO, Mw = 4 x 10(6)) tabl...

journal_title：Pharmaceutical research

authors： Kim CJ

更新日期：1995-07-01 00:00:00

abstract：PURPOSE:The purpose was to develop a population pharmacokinetic model for montelukast after intravenous administration. Clinical trial simulations were conducted using the model developed to identify the lowest intravenous dose in 6- to 14-year-old children that would give montelukast systemic exposures that were compa...

journal_title：Pharmaceutical research

authors： Ramakrishnan R,Migoya E,Knorr B

更新日期：2005-04-01 00:00:00

abstract：PURPOSE:Type I collagen accumulates during liver fibrosis primarily because α-complex protein-2 (αCP(2)), encoded by the poly(rC) binding protein 2 (PCBP2) gene, binds to the 3' end of the collagen mRNA and increases its half-life. This study aimed to reverse the pro-fibrogenic effect of alcohol on hepatic stellate cel...

journal_title：Pharmaceutical research

authors： Shukla RS,Qin B,Wan YJ,Cheng K

更新日期：2011-12-01 00:00:00

abstract：:A novel method of dipeptide synthesis is described that can be carried out in aqueous solution and does not require complicated protecting and deprotecting procedures. An analgesic neuropeptide named kyotorphin, H-Tyr-Arg-OH, was synthesized from unprotected tyrosine and arginine in a new enzymatic reaction catalyzed ...

journal_title：Pharmaceutical research

authors： Kitabatake S,Tsurutani R,Nakajima H,Tomita K,Yoshihara Y,Ueda H,Takagi H,Imahori K

更新日期：1987-04-01 00:00:00

abstract：:The molecular environment of sucrose and mineral oil within sucrose and mineral oil solid state emulsions was investigated by NMR techniques. The 13C and 1H chemical shifts of sucrose and mineral oil to those observed in solid state emulsions (comprised of sucrose and mineral oil) were equivalent, indicating that the ...

journal_title：Pharmaceutical research

authors： Shively ML,Dec SF

更新日期：1994-09-01 00:00:00

abstract：:Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to th...

journal_title：Pharmaceutical research

authors： Quadros E,Landzert NM,LeRoy S,Gasparini F,Worosila G

更新日期：1994-02-01 00:00:00

abstract：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

journal_title：Pharmaceutical research

authors： Kaul G,Amiji M

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:The type and relative importance of saturated and unsaturated phospholipid components of surfactant within the epithelial lining fluid (ELF) of the inner and outer surfaces of the lung is not known. METHODS:Seven healthy dogs were anesthetized and a bronchoalveolar lavage (BAL) was performed, immediately follo...

journal_title：Pharmaceutical research

authors： Mills PC,Chen Y,Hills YC,Hills BA

更新日期：2005-11-01 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:A major challenge facing nanoparticle-based delivery of chemotherapy agents is the natural and unavoidable accumulation of these particles in healthy tissue resulting in local toxicity and dose-limiting side effects. To address this issue, we have designed and characterized a new prodrug nanoparticle with contr...

journal_title：Pharmaceutical research

authors： Schutt C,Ibsen S,Zahavy E,Aryal S,Kuo S,Esener S,Berns M,Esener S

更新日期：2017-10-01 00:00:00

abstract：:The use of microdialysis sampling to study the binding of drugs to plasma proteins was evaluated. Microdialysis sampling is accomplished by placing a short length of dialysis fiber in the sample and perfusing the fiber with a vehicle. Small molecules in the sample, such as drugs, diffuse into the fiber and are transpo...

journal_title：Pharmaceutical research

authors： Herrera AM,Scott DO,Lunte CE

更新日期：1990-10-01 00:00:00