Correlation of partitioning of nitroimidazoles in the n-octanol/saline and liposome systems with pharmacokinetic parameters and quantitative structure-activity relationships (QSAR).

abstract：:HPLC analyses of GM-CSF in solution mixtures containing both GM-CSF and HSA showed losses of GM-CSF which could not be accounted for using conventional electrophoretic and/or RP-HPLC techniques. Further investigation of these mixtures by immunoblotting and by immunoaffinity chromatography demonstrated the presence of ...

journal_title：Pharmaceutical research

authors： Kumarasamy R,Bausch J,Kopcha D,Patel S,McGonigle E

更新日期：1994-03-01 00:00:00

abstract：:Sodium taurodihydrofusidate (STDHF) is one of the most promising absorption enhancers for nasal delivery of peptide drugs. Drugs and additives in nasal formulations should not interfere with the self-cleaning capacity of the nose by the ciliary epithelium. Measured in vitro on human adenoid tissue with a photoelectric...

journal_title：Pharmaceutical research

authors： Hermens WA,Hooymans PM,Verhoef JC,Merkus FW

更新日期：1990-02-01 00:00:00

abstract：:At an ever increasing pace, synthetic biomaterials are being developed with specific functionalities for tissue engineering applications. These biomaterials possess properties including biocompatibility, mechanical strength, and degradation as well as functionalities such as specific cell adhesion and directed cell mi...

journal_title：Pharmaceutical research

authors： Falco EE,Patel M,Fisher JP

更新日期：2008-10-01 00:00:00

abstract：PURPOSE:The purpose of this study was to assess the effect of several chemical permeation enhancers on the buccal permeability of nicotine and to image the spatial distribution of nicotine in buccal mucosa with and without buccal permeation enhancers. METHODS:The impact of sodium taurodeoxycholate (STDC), sodium dodec...

journal_title：Pharmaceutical research

authors： Marxen E,Jin L,Jacobsen J,Janfelt C,Hyrup B,Nicolazzo JA

更新日期：2018-02-21 00:00:00

abstract：PURPOSE:It is reported that the cerebrospinal fluid (CSF) to plasma unbound concentration ratio of fleroxacin at steady-state is approximately 0.5 in experimental animals. These results can be accounted for by assuming the presence of an active transport system for the efflux of this compound across the choroid plexus....

journal_title：Pharmaceutical research

authors： Ooie T,Suzuki H,Terasaki T,Sugiyama Y

更新日期：1996-04-01 00:00:00

abstract：PURPOSE:In vitro in vivo correlation (IVIVC) is a biopharmaceutical tool recommended for use in formulation development. When validated, IVIVC can be used to set dissolution limits and, based on the dissolution limits, as a surrogate for an in vivo study. The purpose of this paper is to study the various methods used t...

journal_title：Pharmaceutical research

authors： Roudier B,Davit BM,Beyssac E,Cardot JM

更新日期：2014-09-01 00:00:00

abstract：PURPOSE:Manufacturing processes for polypeptide/protein drugs are designed to ensure robust quality, efficacy and safety. Process differences introduced by follow-on manufacturers may result in changes in quality and clinical outcomes. This study investigated the impact of production methods on the stability and impuri...

journal_title：Pharmaceutical research

authors： Staby A,Steensgaard DB,Haselmann KF,Marino JS,Bartholdy C,Videbæk N,Schelde O,Bosch-Traberg H,Spang LT,Asgreen DJ

更新日期：2020-06-08 00:00:00

abstract：:Published permeability coefficient (Kp) data for the transport of a large group of compounds through mammalian epidermis were analyzed by a simple model based upon permeant size [molecular volume (MV) or molecular weight (MW)] and octanol/water partition coefficient (Koct). The analysis presented is a facile means to ...

journal_title：Pharmaceutical research

authors： Potts RO,Guy RH

更新日期：1992-05-01 00:00:00

abstract：PURPOSE:Percutaneous absorption assays of molecules for pharmaceutical and cosmetology purposes are important to determine the bioavailability of new compounds, once topically applied. The current method of choice is to measure the rate of diffusion through excised human skin using a diffusion cell. This method however...

journal_title：Pharmaceutical research

authors： Provin C,Nicolas A,Grégoire S,Fujii T

更新日期：2015-08-01 00:00:00

abstract：:Since many chiral pharmaceutical excipients, such as cellulose polymers and cyclodextrins, are used as stationary phases for the separation of enantiomers by high performance liquid chromatography (HPLC), it is hypothesized that one enantiomer of a chiral drug will be released faster than the other from a pharmaceutic...

journal_title：Pharmaceutical research

authors： Duddu SP,Vakilynejad M,Jamali F,Grant DJ

更新日期：1993-11-01 00:00:00

abstract：PURPOSE:The objective of this investigation is to develop a rational design of Osteotropic Drug Delivery System (ODDS), which we have proposed as a novel method for drug delivery to the skeleton via bisphosphonic prodrug, based on the relationship between physicochemical and pharmacokinetic properties of bisphosphonate...

journal_title：Pharmaceutical research

authors： Hirabayashi H,Sawamoto T,Fujisaki J,Tokunaga Y,Kimura S,Hata T

更新日期：2001-05-01 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：:A biopharmaceutics drug classification scheme for correlating in vitro drug product dissolution and in vivo bioavailability is proposed based on recognizing that drug dissolution and gastrointestinal permeability are the fundamental parameters controlling rate and extent of drug absorption. This analysis uses a transp...

journal_title：Pharmaceutical research

authors： Amidon GL,Lennernäs H,Shah VP,Crison JR

更新日期：1995-03-01 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：: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 characterize the electrochemical behavior of the photodegradation product of nifedipine, i.e., 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridine-carboxylic acid dimethyl ester (NPD) in different electrolytic media. We also evaluated the interaction between free radicals generated from NPD and xeno/endobiotics. ...

journal_title：Pharmaceutical research

authors： Núñez-Vergara LJ,Bollo S,Fuentealba J,Sturm JC,Squella JA

更新日期：2002-04-01 00:00:00

abstract：:Magnetic nanoparticles are useful as contrast agents for magnetic resonance imaging (MRI). Paramagnetic contrast agents have been used for a long time, but more recently superparamagnetic iron oxide nanoparticles (SPIOs) have been discovered to influence MRI contrast as well. In contrast to paramagnetic contrast agent...

journal_title：Pharmaceutical research

authors： Rümenapp C,Gleich B,Haase A

更新日期：2012-05-01 00:00:00

abstract：PURPOSE:The aim of the present study was to design a new mucosal drug delivery system composed of liposomes dispersed within a bioadhesive hydrogel containing methyl-beta-cyclodextrin (Me(beta)CD) for controlled drug release. METHODS:A hydrophilic model molecule, inulin, was encapsulated within positively charged and ...

journal_title：Pharmaceutical research

authors： Boulmedarat L,Piel G,Bochot A,Lesieur S,Delattre L,Fattal E

更新日期：2005-06-01 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：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：PURPOSE:To characterize the uptake mechanism of zidovudine (AZT), a nucleoside reverse transcriptase inhibitor, in syncytiotrophoblast cells using the TR-TBT 18d-1 cell line previously established by our group. MATERIALS AND METHODS:The effects of several transporter inhibitors on the initial and steady-state apical u...

journal_title：Pharmaceutical research

authors： Sai Y,Nishimura T,Shimpo S,Chishu T,Sato K,Kose N,Terasaki T,Mukai C,Kitagaki S,Miyakoshi N,Kang YS,Nakashima E

更新日期：2008-07-01 00:00:00

abstract：PURPOSE:To examine the presence of multiplicity for the biliary excretion of xenobiotic conjugates, we studied the disposition of glycyrrhizin (GR), which has glucuronide within its molecular structure and has the ability to inhibit the biliary excretion of liquiritigenin (LG) glucuronides. METHODS:GR was administered...

journal_title：Pharmaceutical research

authors： Shimamura H,Suzuki H,Tagaya O,Horie T,Sugiyama Y

更新日期：1996-12-01 00:00:00

abstract：PURPOSE:We compared cationic, polyamine-coated microparticles (MPs) and anionic, protein-coated MPs with respect to their phagocytosis and phagosomal fate in dendritic cells (DCs) and macrophages (Mphi). METHODS:Polystyrene MPs were surface modified by covalent coupling with fluorescein isothiocyanate-labeled polyamin...

journal_title：Pharmaceutical research

authors： Thiele L,Merkle HP,Walter E

更新日期：2003-02-01 00:00:00

abstract：PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...

journal_title：Pharmaceutical research

authors： Kafedjiiski K,Föger F,Werle M,Bernkop-Schnürch A

更新日期：2005-09-01 00:00:00

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：: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 investigate in vitro if P-glycoprotein (P-gp) transport can differentiate between antibiotic drugs exhibiting increased active renal clearance (CL(r)) in cystic fibrosis (CF) patients (i.e., dicloxacillin, trimethoprim) and drugs that do not exhibit this phenomenon (i.e.. cefsulodin, sulfamethoxazole). METH...

journal_title：Pharmaceutical research

authors： Susanto M,Benet LZ

更新日期：2002-04-01 00:00:00

abstract：PURPOSE:Excipients are added to lyophilized protein drug formulations to protect the protein during processing and storage, but the mechanisms are poorly understood. Here, hydrogen/deuterium (H/D) exchange with mass spectrometry was used to assess protein conformation and excipient interactions in lyophilized solids. ...

journal_title：Pharmaceutical research

authors： Li Y,Williams TD,Topp EM

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:In this work, the alacepril thiolesterase, which catalyzes the hydrolyzing reaction of the thiolester linkage in alacepril and the conversion from alacepril to deacetylalacepril, was purified from rat liver cytosol and characterized. METHODS:A purification procedure for the thiolesterase consisted of ammonium ...

journal_title：Pharmaceutical research

authors： Usui S,Kubota M,Iguchi K,Kiho T,Sugiyama T,Katagiri Y,Hirano K

更新日期：2003-08-01 00:00:00

abstract：:The influence of the jejunal bloodflow on the absorption of theophylline was investigated. The bloodflow through a segment under investigation was varied by changing the systemic blood pressure by means of a donor blood infusion into the jugular vein or by an infusion of isoprenaline or levarterenol into a femoral vei...

journal_title：Pharmaceutical research

authors： Schurgers N,de Blaey CJ

更新日期：1984-01-01 00:00:00