Drug delivery studies in Caco-2 monolayers. IV. Absorption enhancer effects of cyclodextrins.

abstract：PURPOSE:To show, using a model study, how electronic structure theory can be applied in combination with LC/UV/MS/MS for the prediction and identification of oxidative degradants. METHODS:The benzyloxazole 1, was used to represent an active pharmaceutical ingredient for oxidative forced degradation studies. Bond disso...

journal_title：Pharmaceutical research

authors： Reid DL,Calvitt CJ,Zell MT,Miller KG,Kingsmill CA

更新日期：2004-09-01 00:00:00

abstract：PURPOSE:Herein we report the discovery of a group of derivatized alpha-amino acids that increase the oral bioavailability of sodium cromolyn. METHODS:We prepared three N-acylated alpha-amino acids and used these compounds to demonstrate the oral delivery of cromolyn in an in vivo rat model. In vitro experiments, inclu...

journal_title：Pharmaceutical research

authors： Leone-Bay A,Leipold H,Sarubbi D,Variano B,Rivera T,Baughman RA

更新日期：1996-02-01 00:00:00

abstract：PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...

journal_title：Pharmaceutical research

authors： Suárez Del Pino JA,Kolhatkar R

更新日期：2017-12-01 00:00:00

abstract：:A quantitative analysis of the dependence of dissolution rate on the relative surface area occupied by two non-interacting drug mixtures from co-compressed slabs is described. The results from the experimental dissolution rates of each component from naproxen/phenytoin co-compressed slabs under laminar flow conditions...

journal_title：Pharmaceutical research

authors： Neervannan S,Southard MZ,Stella VJ

更新日期：1994-10-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the specific changes in body distribution of camptothecin (CA) through incorporation into solid lipid nanoparticles (SLN) by peroral route. METHODS:Camptothecin loaded solid lipid nanoparticles (CA-SLN) coated with poloxamer 188 were produced by high pressure homogeniza...

journal_title：Pharmaceutical research

authors： Yang S,Zhu J,Lu Y,Liang B,Yang C

更新日期：1999-05-01 00:00:00

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:The cell surface adhesion molecule CD44 plays important roles in the initiation and development of atherosclerotic plaques. We aim to develop nanoparticles that can selectively target CD44 for the non-invasive detection of atherosclerotic plaques by magnetic resonance imaging. METHODS:Magnetic glyconanoparticl...

journal_title：Pharmaceutical research

authors： El-Dakdouki MH,El-Boubbou K,Kamat M,Huang R,Abela GS,Kiupel M,Zhu DC,Huang X

更新日期：2014-06-01 00:00:00

abstract：PURPOSE:A series of studies was conducted to evaluate the preclinical pharmacokinetics of SB-239063 (trans-1-(4-hydroxycyclohexyl)-4-(4-fluorophenyl)-5-[(2-methoxy)pyrimidin-4-yl] imidazole), a potent and selective p38 MAP kinase inhibitor. METHODS:SB-239063 was administered both i.v. and p.o. in the rat, dog, cynomol...

journal_title：Pharmaceutical research

authors： Ward KW,Proksch JW,Azzarano LM,Salyers KL,McSurdy-Freed JE,Molnar TM,Levy MA,Smith BR

更新日期：2001-09-01 00:00:00

abstract：:The permeation enhancing property of 5% oleic acid in ethanol on beta-estradiol was investigated in vitro and in vivo using symmetrical and asymmetrical side-by-side diffusion cells and the human skin sandwich flap, respectively. beta-Estradiol permeability in vitro and in vivo was similar in 75% ethanol (ETOH). Oleic...

journal_title：Pharmaceutical research

authors： Pershing LK,Parry GE,Lambert LD

更新日期：1993-12-01 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: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

abstract：:We describe a simplified and rapid liquid chromatographic determination of antipyrine clearance (CLAP) calculated from peak height ratios of drug/internal standard. Saliva or plasma was collected 24 hr after the oral administration of 1 g of antipyrine to the subject. A 25-microliter aliquot of the sample is deprotein...

journal_title：Pharmaceutical research

authors： el-Yazigi A,Raines DA,Ali H,Sieck J,Ernst P,Dossing M

更新日期：1991-02-01 00:00:00

abstract：PURPOSE:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...

journal_title：Pharmaceutical research

authors： Massarella JW,Nazareno LA,Passe S,Min B

更新日期：1996-03-01 00:00:00

abstract：PURPOSE:Information on genetic variants that affect the pharmacokinetics and pharmacodynamics (PK/PD) of drugs in different populations from Mexico is still an ongoing endeavor. Here, we investigate allele frequencies on pharmacogenetic targets in Mexican Mestizos and Natives from three different States and its associa...

journal_title：Pharmaceutical research

authors： Gonzalez-Covarrubias V,Martínez-Magaña JJ,Coronado-Sosa R,Villegas-Torres B,Genis-Mendoza AD,Canales-Herrerias P,Nicolini H,Soberón X

更新日期：2016-11-01 00:00:00

abstract：PURPOSE:A rapid immune response is required to prevent death from Anthrax, caused by Bacillus anthracis. METHOD:We formulated a vaccine carrier comprised of acetalated dextran microparticles encapsulating recombinant protective antigen (rPA) and resiquimod (a toll-like receptor 7/8 agonist). RESULTS:We were able to p...

journal_title：Pharmaceutical research

authors： Schully KL,Sharma S,Peine KJ,Pesce J,Elberson MA,Fonseca ME,Prouty AM,Bell MG,Borteh H,Gallovic M,Bachelder EM,Keane-Myers A,Ainslie KM

更新日期：2013-05-01 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：PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...

journal_title：Pharmaceutical research

authors： Tian R,Koyabu N,Takanaga H,Matsuo H,Ohtani H,Sawada Y

更新日期：2002-06-01 00:00:00

abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...

journal_title：Pharmaceutical research

authors： Ring A,Tothfalusi L,Endrenyi L,Weiss M

更新日期：2000-05-01 00:00:00

abstract：PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...

journal_title：Pharmaceutical research

authors： Houdaihed L,Evans JC,Allen C

更新日期：2020-01-21 00:00:00

abstract：:A new method of analysis for the antihypertensive drug, hydralazine, is introduced. The assay involves the addition of p-nitrobenzaldehyde to blood samples containing hydralazine, to form a stable Schiff's base, hydralazine p-nitrobenzaldehyde hydrazone. The derivative is extracted from the blood into hexane and the s...

journal_title：Pharmaceutical research

authors： Semple HA,Tam YK,Tin S,Coutts RT

更新日期：1988-06-01 00:00:00

abstract：PURPOSE:This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system. METHODS:Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrosp...

journal_title：Pharmaceutical research

authors： Teoh XY,Yeoh Y,Yoong LK,Chan SY

更新日期：2020-01-07 00:00:00

abstract：PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...

journal_title：Pharmaceutical research

authors： van der Aa MA,Huth US,Häfele SY,Schubert R,Oosting RS,Mastrobattista E,Hennink WE,Peschka-Süss R,Koning GA,Crommelin DJ

更新日期：2007-08-01 00:00:00

abstract：PURPOSE:Previous literature has suggested the absence of an effective barrier between the nasal mucosa and the brain for compounds administered via the nasal route. These experiments were conducted to elucidate the role of the blood-brain barrier efflux transporter P-glycoprotein (P-gp) in attenuating delivery of P-gp ...

journal_title：Pharmaceutical research

authors： Graff CL,Pollack GM

更新日期：2003-08-01 00:00:00

abstract：:Liver fibrosis is a pathological condition originating from liver damage that leads to excess accumulation of extracellular matrix (ECM) proteins in the liver. Viral infection, chronic injury, local inflammatory responses and oxidative stress are the major factors contributing to the onset and progression of liver fib...

journal_title：Pharmaceutical research

authors： Kumar V,Mahato RI

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:The present study evaluates immobilized artificial membrane (IAM) chromatography for predicting drug permeability across the blood-brain barrier (BBB) and outlines the potential and limitations of IAMs as a predictive tool by comparison with conventional methods based on octanol/water partitioning and octadecyl...

journal_title：Pharmaceutical research

authors： Reichel A,Begley DJ

更新日期：1998-08-01 00:00:00

abstract：:To clarify the mechanism by which basic drugs accumulate in the lung, the binding selectivity of drugs to different subcellular structures of the perfused rat lung was examined. Imipramine, quinine, and metoclopramide were used as examples of basic drugs. The accumulation of basic drugs was highest in the mitochondria...

journal_title：Pharmaceutical research

authors： Yoshida H,Okumura K,Hori R

更新日期：1987-02-01 00:00:00

abstract：PURPOSE:Effects of polyvinylpyrrolidone (PVP) molecular weight on the solid-state intermolecular interactions among probucol/PVP/sodium dodecyl sulfate (SDS) ternary ground mixtures (GM) and the formation of nanoparticles were investigated by solid-state NMR spectroscopy. MATERIALS AND METHODS:Ternary GMs of probucol ...

journal_title：Pharmaceutical research

authors： Pongpeerapat A,Higashi K,Tozuka Y,Moribe K,Yamamoto K

更新日期：2006-11-01 00:00:00

abstract：PURPOSE:Within-subject dependency of observations has a strong impact on the evaluation of population pharmacokinetic (PK) and/or pharmacodynamic (PD) models. To our knowledge, none of the current model evaluation tools correctly address this issue. We present a new method with a global test and easy diagnostic plot wh...

journal_title：Pharmaceutical research

authors： Laffont CM,Concordet D

更新日期：2011-08-01 00:00:00

abstract：:Nanobiosensors with high sensitivity and specificity have shown great potential in the detection of diseases. The incorporation of therapeutic agents with nanobiosensors allows the simultaneous diagnosis and therapy of diseases. The delivery of nanobiosensors and therapeutic agents using polymers is a common strategy ...

journal_title：Pharmaceutical research

authors： Li Y,Yang HY,Lee DS

更新日期：2016-10-01 00:00:00

abstract：:The partitioning of a series of nine nitroimidazole drugs in liposomes (log Km) of various compositions has been determined and compared to their partitioning in the n-octanol/saline system (log K) at 30 degrees C. The log Km ranged from 1.5 to 0.5 and was three- to fourfold greater than the log K; further, the linear...

journal_title：Pharmaceutical research

authors： Betageri GV,Rogers JA

更新日期：1989-05-01 00:00:00