Interaction mechanism between indoxyl sulfate, a typical uremic toxin bound to site II, and ligands bound to site I of human serum albumin.

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：PURPOSE:Low temperature sensitive liposome (LTSL) encapsulated docetaxel were combined with mild hyperthermia (40-42°C) to investigate in vivo biodistribution and efficacy against a castrate resistant prostate cancer. METHOD:Female athymic nude mice with human prostate PC-3 M-luciferase cells grown subcutaneously into...

journal_title：Pharmaceutical research

authors： Ranjan A,Benjamin CJ,Negussie AH,Chokshi S,Chung PH,Volkin D,Yeram N,Linehan WM,Dreher MR,Pinto PA,Wood BJ

更新日期：2016-10-01 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 transepithelial transport of arginine vasopressin (AVP) across cultured rat alveolar epithelial cell monolayers was studied. At 0.1 nM donor [125I]AVP, the radiolabel flux measured in the apical-to-basolateral (AB) direction was about 10 times greater than that in the reverse (BA) direction. HPLC analyses of the b...

journal_title：Pharmaceutical research

authors： Yamahara H,Morimoto K,Lee VH,Kim KJ

更新日期：1994-11-01 00:00:00

abstract：PURPOSE:To advance fundamental biological and translational research with the bacterium Neisseria gonorrhoeae through the prediction of novel small molecule growth inhibitors via naïve Bayesian modeling methodology. METHODS:Inspection and curation of data from the publicly available ChEMBL web site for small molecule ...

journal_title：Pharmaceutical research

authors： Pereira JC,Daher SS,Zorn KM,Sherwood M,Russo R,Perryman AL,Wang X,Freundlich MJ,Ekins S,Freundlich JS

更新日期：2020-07-13 00:00:00

abstract：:Diltiazem (DTZ) is a calcium channel blocker widely used in the treatment of angina and hypertension. DTZ undergoes extensive metabolism yielding several metabolites, some of which are active like N-desmethyldiltiazem (MA), desacetyldiltiazem (M1) and N-desmethyl,desacetyldiltiazem (M2). Due to the nature of its biotr...

journal_title：Pharmaceutical research

authors： Homsy W,Lefebvre M,Caillé G,du Souich P

更新日期：1995-04-01 00:00:00

abstract：PURPOSE:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...

journal_title：Pharmaceutical research

authors： Fabiilli ML,Lee JA,Kripfgans OD,Carson PL,Fowlkes JB

更新日期：2010-12-01 00:00:00

abstract：PURPOSE:To examine the theoretical/practical utility of the liver-to-blood partition coefficient (Kpuu) for predicting drug-drug interactions (DDIs), and compare the Kpuu-approach to the extended clearance concept AUCR-approach. METHODS:The Kpuu relationship was derived from first principles. Theoretical simulations i...

journal_title：Pharmaceutical research

authors： Sodhi JK,Liu S,Benet LZ

更新日期：2020-03-25 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：BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...

journal_title：Pharmaceutical research

authors： Kobayashi M,Tsujiuchi T,Okui Y,Mizutani A,Nishi K,Nakanishi T,Nishii R,Fukuchi K,Tamai I,Kawai K

更新日期：2018-11-29 00:00:00

abstract：:The role of phosphatidylserine in the cellular and subcellular lung distribution of quinidine was investigated in rats, since quinidine was found to bind preferentially to phosphatidylserine. The concentration of phosphatidylserine in the cellular and subcellular fractions was determined after separation by two-dimens...

journal_title：Pharmaceutical research

authors： Nishiura A,Murakami T,Higashi Y,Yata N

更新日期：1988-04-01 00:00:00

abstract：:The role of a bile salt (sodium taurocholate) and lipolysis products (monoglyceride and fatty acid) in the intestinal absorption of a poorly water-soluble drug, diazepam, was investigated. Absorption rates and bioavailabilities were determined with the in situ rat gut technique of Doluisio et al. and analyzing the dia...

journal_title：Pharmaceutical research

authors： Serajuddin AT,Rosoff M,Goldberg AH

更新日期：1985-09-01 00:00:00

abstract：:Five aliphatic 5'-esters of 5-iodo-2'deoxyuridine (IDU) were synthesized via an acid chloride alcoholysis reaction. The solubility in pH 7.4 phosphate buffer, lipophilicity as determined by partition experiments in octanol/pH 7.4 buffer, and cytotoxicity of these potential prodrugs were evaluated. The esters showed a ...

journal_title：Pharmaceutical research

authors： Narurkar MM,Mitra AK

更新日期：1988-11-01 00:00:00

abstract：PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...

journal_title：Pharmaceutical research

authors： Baba H,Takahara J,Mamitsuka H

更新日期：2015-07-01 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:Interleukin-10 (IL-10) is an anti-inflammatory molecule that has achieved interest as a therapeutic for neuropathic pain. In this work, the potential of plasmid DNA-encoding IL-10 (pDNA-IL-10) slowly released from biodegradable microparticles to provide long-term pain relief in an animal model of neuropathic pa...

journal_title：Pharmaceutical research

authors： Soderquist RG,Sloane EM,Loram LC,Harrison JA,Dengler EC,Johnson SM,Amer LD,Young CS,Lewis MT,Poole S,Frank MG,Watkins LR,Milligan ED,Mahoney MJ

更新日期：2010-05-01 00:00:00

abstract：PURPOSE:To investigate, for the first time, the performance of a dry powder inhaler (DPI, Aerolizer(®)) in the case of a model drug (i.e. albuterol sulphate) formulated with spray dried mannitol carrier particles with homogeneous shape and solid-state form but different sizes. METHODS:Spray dried mannitol (SDM) partic...

journal_title：Pharmaceutical research

authors： Kaialy W,Hussain T,Alhalaweh A,Nokhodchi A

更新日期：2014-01-01 00:00:00

abstract：:Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...

journal_title：Pharmaceutical research

authors： Kamei S,Kopecek J

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...

journal_title：Pharmaceutical research

authors： van Dijkhuizen-Radersma R,Wright SJ,Taylor LM,John BA,de Groot K,Bezemer JM

更新日期：2004-03-01 00:00:00

abstract：PURPOSE:To investigate the suitability of three antimicrobial peptides (AMPs) as cell-penetrating antimicrobial peptides. METHODS:Cellular uptake of three AMPs (PK-12-KKP, SA-3 and TPk) and a cell-penetrating peptide (penetratin), all 5(6)-carboxytetramethylrhodamine-labeled, were tested in HeLa WT cells and analyzed ...

journal_title：Pharmaceutical research

authors： Bahnsen JS,Franzyk H,Sayers EJ,Jones AT,Nielsen HM

更新日期：2015-05-01 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:Vancomycin (VCM) concentration is often out of therapeutic range (10-20 μg/ml) in patients receiving continuous renal replacement therapy (CRRT). The purposes of this study were to develop a practical VCM population pharmacokinetic (PPK) model and to evaluate the potential of Bayesian prediction-based therapeut...

journal_title：Pharmaceutical research

authors： Oda K,Jono H,Kamohara H,Nishi K,Tanoue N,Saito H

更新日期：2020-05-28 00:00:00

abstract：PURPOSE:For selective inhibition of endothelial cell activation in chronic inflammation, we have developed a dexamethasone-anti-E-selectin immunoconjugate. The present study was performed to evaluate the cellular handling of this immunoconjugate by activated primary endothelial cells and to compare its drug delivery ca...

journal_title：Pharmaceutical research

authors： Kok RJ,Everts M,Asgeirsdóttir SA,Meijer DK,Molema G

更新日期：2002-11-01 00:00:00

abstract：PURPOSE:To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium. METHODS:PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel st...

journal_title：Pharmaceutical research

authors： Carlisle R,Seymour LW,Coussios CC

更新日期：2013-02-01 00:00:00

abstract：:High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...

journal_title：Pharmaceutical research

authors： Golomb G,Avramoff A,Hoffman A

更新日期：1993-06-01 00:00:00

abstract：:We investigated the effects of increased concentrations of the solutes, salicylic acid, benzoic acid, and o-, m-, and p-methoxy benzoic acids, on the anisotropic properties of a liquid crystal solvent. The lamellar liquid crystal was composed of 37% polyoxyethylene (20) isohexadecyl ether in aqueous buffer of pH 1. Ph...

journal_title：Pharmaceutical research

authors： Ibrahim HG,Sallam ES,Takieddin M,Habboub M

更新日期：1993-05-01 00:00:00

abstract：:Nanoparticles, including lipopolyamines leading to lipoplexes, liposomes, and polyplexes are targeted drug carrier systems in the current search for a successful delivery system for polynucleic acids. This review is focused on the impact of gene and siRNA delivery for studies of efficacy, pharmacodynamics, and pharmac...

journal_title：Pharmaceutical research

authors： Blagbrough IS,Zara C

更新日期：2009-01-01 00:00:00

abstract：PURPOSE:To develop novel biomineral-binding liposomes (BBL) for the prevention of orthopedic implant associated osteomyelitis. METHODS:A biomineral-binding lipid, alendronate-tri(ethyleneglycol)-cholesterol conjugate (ALN-TEG-Chol), was synthesized through Cu(I)-catalyzed Huisgen 1,3-dipolar cycloaddition (a versatile...

journal_title：Pharmaceutical research

authors： Liu XM,Zhang Y,Chen F,Khutsishvili I,Fehringer EV,Marky LA,Bayles KW,Wang D

更新日期：2012-11-01 00:00:00

abstract：PURPOSE:Myricetin (MYR) flavonoid is well-recognized for its antioxidant, anti-inflammatory and anti-tumor potential. Introducing nanomedicine was the ultimate resort to solve the imperfections of this nutraceutical, namely solubility, stability and delivery issues. The study, thus, aims at developing inhalable micropa...

journal_title：Pharmaceutical research

authors： Nafee N,Gaber DM,Elzoghby AO,Helmy MW,Abdallah OY

更新日期：2020-04-14 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