Constant-rate intravenous infusion methods for estimating steady-state volumes of distribution and mean residence times in the body for drugs undergoing reversible metabolism.

abstract：PURPOSE:The pharmacokinetics, analgesic efficacy, and irritancy potential of Buprederm, a new transdermal delivery system of buprenorphine, was evaluated. METHODS:Single and multiple dose pharmacokinetic studies were conducted in mice and rabbits. The analgesic efficacy and skin irritation potential were determined by...

journal_title：Pharmaceutical research

authors： Park I,Kim D,Song J,In CH,Jeong SW,Lee SH,Min B,Lee D,Kim SO

更新日期：2008-05-01 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:Highly lipophilic basic drugs, the antiestrogens AE 1 (log P = 5.82) and AE 2 (log P = 7.8) shall be delivered transdermally. METHODS:Transdermal permeation of drugs, enhancers, and solvents from various fluid formulations were characterized by in-vitro permeation studies through excised skin of hairless mice....

journal_title：Pharmaceutical research

authors： Funke AP,Schiller R,Motzkus HW,Günther C,Müller RH,Lipp R

更新日期：2002-05-01 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：:Solution calorimetry has been employed to evaluate the stability constants and enthalpy changes associated with complex formation between alpha-, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. Data from thermal titrations of the compounds were analyzed using no...

journal_title：Pharmaceutical research

authors： Tong WQ,Lach JL,Chin TF,Guillory JK

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:Pluronics are known as inhibitors of multidrug resistance thus making tumor cells sensitive to therapeutic doses of drugs. The purpose of our study consists in revealing molecular targets of the hydrophobic poly(propylene oxide) block of pluronics in living cells and the dependence of the polymers chemosensitiz...

journal_title：Pharmaceutical research

authors： Zhirnov A,Nam E,Badun G,Romanyuk A,Ezhov A,Melik-Nubarov N,Grozdova I

更新日期：2018-09-06 00:00:00

abstract：:The pharmacokinetics of trilostane and one of its metabolites ketotrilostane are described and characterized in the rat following the separate intravenous administration of trilostane and ketotrilostane. It was noted during these studies that the parent compound and its metabolite undergo metabolic interconversion-tri...

journal_title：Pharmaceutical research

authors： McGee JP,Shaw PN

更新日期：1992-04-01 00:00:00

abstract：PURPOSE:The purpose of the present study is to explore whether a poly-L-arginine (poly-L-Arg)-induced increase in tight junctions (TJ) permeability of fluorescein isothiocyanate-labeled dextran (MW 4.4 kDa, FD-4) is associated with the Ca2+-dependent signaling and occurs following the phosphorylation/dephosphorylation ...

journal_title：Pharmaceutical research

authors： Ohtake K,Maeno T,Ueda H,Ogihara M,Natsume H,Morimoto Y

更新日期：2003-11-01 00:00:00

abstract：PURPOSE:The trial-and-error approach is still predominantly used in pharmaceutical development of nanosuspensions. Physicochemical dispersion stability is a primary focus and therefore, various analytical bulk methods are commonly employed. Clearly less attention is directed to surface changes of nanoparticles even tho...

journal_title：Pharmaceutical research

authors： Aleandri S,Schönenberger M,Niederquell A,Kuentz M

更新日期：2018-02-21 00:00:00

abstract：PURPOSE:To describe a computational tool to calculate molecular descriptors of potential application in ADME virtual screening of antitumor Pt(II) drug candidates. METHODS:The multistep computational procedure consists in (a) building and optimization (PM3) of the 3D structures of the investigated complexes, (b) param...

journal_title：Pharmaceutical research

authors： Caron G,Ravera M,Ermondi G

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:The purpose of this study was to establish a useful methodology, possibly providing information on the stoichiometry of pharmaceutical drug salts obtained from salt screening by using a multiwell plate and a Raman microscope. METHODS:Tamoxifen salt screening was conducted with monobasic and polybasic acids on ...

journal_title：Pharmaceutical research

authors： Kojima T,Onoue S,Murase N,Katoh F,Mano T,Matsuda Y

更新日期：2006-04-01 00:00:00

abstract：PURPOSE:The use of "Trojan Horse" nanocarriers for antibiotics to enhance the activity of antibiotics against susceptible and resistant bacteria is investigated. METHODS:Antibiotic carriers (CD-MAN and CD-GLU) are prepared from β-cyclodextrin grafted with sugar molecules (D-mannose and D-glucose, respectively) via azi...

journal_title：Pharmaceutical research

authors： Li M,Neoh KG,Xu L,Yuan L,Leong DT,Kang ET,Chua KL,Hsu LY

更新日期：2016-05-01 00:00:00

abstract：PURPOSE:Modulation of 5-HT3 receptor in the central nervous system (CNS) is a promising approach for treatment of neuropathic pain. The goal was to evaluate the role of P-glycoprotein (Pgp) in limiting exposure of different parts of the CNS to ondansetron (5-HT3 receptor antagonist) using wild-type and genetic knockout...

journal_title：Pharmaceutical research

authors： Chiang M,Back HM,Lee JB,Oh S,Guo T,Girgis S,Park C,Haroutounian S,Kagan L

更新日期：2020-09-28 00:00:00

abstract：PURPOSE:To study the biorelevant drug release from novel starch-based polyvinyl alcohol capsules (S-PVA-C). The effect of the shell material is studied by considering microstructural formulation changes during hydration. METHODS:Two different self-emulsifying systems containing either fenofibrate or probucol were fill...

journal_title：Pharmaceutical research

authors： Misic Z,Urbani R,Pfohl T,Muffler K,Sydow G,Kuentz M

更新日期：2014-01-01 00:00:00

abstract：PURPOSE:The possibility of preparing nanoparticles in the supercooled thermotropic liquid crystalline state from cholesterol esters with saturated acyl chains as well as the incorporation of model drugs into the dispersions was investigated using cholesteryl myristate (CM) as a model cholesterol ester. METHODS:Nanopar...

journal_title：Pharmaceutical research

authors： Kuntsche J,Westesen K,Drechsler M,Koch MH,Bunjes H

更新日期：2004-10-01 00:00:00

abstract：:The conditions under which the absorption enhancer palmitoyl L-carnitine chloride (PCC) improved the bioavailability of the poorly absorbed antibiotic cefoxitin throughout the rat intestine has been studied. Cefoxitin alone was appreciably absorbed only in the duodenum (31% vs less than 7% elsewhere). PCC solutions (3...

journal_title：Pharmaceutical research

authors： Sutton SC,LeCluyse EL,Cammack L,Fix JA

更新日期：1992-02-01 00:00:00

abstract：PURPOSE:This work explores the distribution of water and its effects on molecular mobilities in poly(vinylpyrrolidone) (PVP) glasses using molecular dynamics (MD) simulation technology. METHODS:PVP glasses containing 0.5% and 10% w/w water and a small amount of ammonia and Phe-Asn-Gly were generated. Physical aging pr...

journal_title：Pharmaceutical research

authors： Xiang TX,Anderson BD

更新日期：2005-08-01 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:The objective of the current study was to investigate whether blood-brain barrier (BBB) permeability studies in vitro could be accelerated by running several compounds together in the same experiment. METHODS:To address this question, we compared the transport of six compounds run separately with the results o...

journal_title：Pharmaceutical research

authors： Berezowski V,Landry C,Lundquist S,Dehouck L,Cecchelli R,Dehouck MP,Fenart L

更新日期：2004-05-01 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：:The bioavailability of dipyridamole, a poorly soluble weak base, was evaluated in 11 healthy, older subjects (> or = 65 years), 6 with a low fasting gastric pH (control) and 5 with a fasting gastric pH > 5 (achlorhydric), in a randomized, crossover design. Subjects received 50 mg dipyridamole as a single oral dose bot...

journal_title：Pharmaceutical research

authors： Russell TL,Berardi RR,Barnett JL,O'Sullivan TL,Wagner JG,Dressman JB

更新日期：1994-01-01 00:00:00

abstract：:Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...

journal_title：Pharmaceutical research

authors： Rathore AS,Garcia-Aponte OF,Golabgir A,Vallejo-Diaz BM,Herwig C

更新日期：2017-02-01 00:00:00

abstract：PURPOSE:The amphiphilic block copolymer Pluronic P85 (P85) increases the permeability of the blood-brain barrier (BBB) with respect to a broad spectrum of drugs by inhibiting the drug efflux transporter, P-glycoprotein (Pgp). In this regard, P85 serves as a promising component for CNS drug delivery systems. To assess t...

journal_title：Pharmaceutical research

authors： Batrakova EV,Zhang Y,Li Y,Li S,Vinogradov SV,Persidsky Y,Alakhov VY,Miller DW,Kabanov AV

更新日期：2004-11-01 00:00:00

abstract：:The new generation of nanotechnology-based drug formulations is challenging the accepted ways of cancer treatment. Multi-functional nanomaterial constructs have the capability to be delivered directly to the tumor site and eradicate cancer cells selectively, while sparing healthy cells. Tailoring of the nano-construct...

journal_title：Pharmaceutical research

authors： Farrell D,Ptak K,Panaro NJ,Grodzinski P

更新日期：2011-02-01 00:00:00

abstract：PURPOSE:This study aimed to assess impact of different vehicles for laser-assisted skin drug delivery. We also tried to uncover the mechanisms by which different vehicles affect laser-aided skin permeation. METHODS:Full-surface ablative (conventional) and fractional lasers were used to irradiate nude mouse skin. Imiqu...

journal_title：Pharmaceutical research

authors： Lee WR,Shen SC,Aljuffali IA,Li YC,Fang JY

更新日期：2014-02-01 00:00:00

abstract：PURPOSE:To better understand the nature of drug-excipient interactions we have studied the phase behavior of amorphous binary and ternary mixtures of citric acid, indomethacin and PVP, as model systems. METHODS:We have prepared amorphous mixtures by co-melting or coprecipitation from solvents, and have measured glass ...

journal_title：Pharmaceutical research

authors： Lu Q,Zografi G

更新日期：1998-08-01 00:00:00

abstract：PURPOSE:The low aqueous solubility of many drugs impedes detailed investigation as the detection limit of standard testing routines is limited. This is further complicated within application relevant thin films typical used in patches or stripes for buccal or topical routes. METHODS:In this work a model system is deve...

journal_title：Pharmaceutical research

authors： Ehmann HM,Winter S,Griesser T,Keimel R,Schrank S,Zimmer A,Werzer O

更新日期：2014-10-01 00:00:00

abstract：:A new magnetic microsphere carrier has been formulated that may localize drugs by both biochemical and physical means. The microspheres, prepared from the polysaccharide chitosan, are designed to bind to anionic glycosaminoglycan receptors on the surface of capillary endothelial cells. The microspheres were formulated...

journal_title：Pharmaceutical research

authors： Gallo JM,Hassan EE

更新日期：1988-05-01 00:00:00

abstract：PURPOSE:Basal insulins with improved kinetic properties can potentially be produced using acylation by fatty acids that enable soluble, high-molecular weight complexes to form post-injection. A series of insulins, acylated at B29 with fatty acids via glutamic acid spacers, were examined to deduce the structural require...

journal_title：Pharmaceutical research

authors： Jonassen I,Havelund S,Hoeg-Jensen T,Steensgaard DB,Wahlund PO,Ribel U

更新日期：2012-08-01 00:00:00

abstract：PURPOSE:To assess the efficacy of the novel clinical formulation of fenretinide (LAU-7b) for the treatment of allergic asthma. To study the association between LAU-7b treatment in allergic asthma and the modulation of very long chain ceramides (VLCC). METHODS:We used two allergens (OVA and HDM) to induce asthma in mou...

journal_title：Pharmaceutical research

authors： Youssef M,De Sanctis JB,Kanagaratham C,Tao S,Ahmed E,Radzioch D

更新日期：2020-01-08 00:00:00