Molecular modeling study of diltiazem mimics at L-type calcium channels.

abstract：PURPOSE:Lapatinib, a small molecule EGFR/HER2 inhibitor, partially inhibits the outgrowth of HER2+ brain metastases in preclinical models and in a subset of CNS lesions in clinical trials of HER2+ breast cancer. We investigated the ability of lapatinib to reach therapeutic concentrations in the CNS following (14)C-lapa...

journal_title：Pharmaceutical research

authors： Taskar KS,Rudraraju V,Mittapalli RK,Samala R,Thorsheim HR,Lockman J,Gril B,Hua E,Palmieri D,Polli JW,Castellino S,Rubin SD,Lockman PR,Steeg PS,Smith QR

更新日期：2012-03-01 00:00:00

abstract：PURPOSE:The aim of the study is to determine whether a biodegradable elastomeric device that uses an osmotic pressure delivery mechanism can release different therapeutic proteins at a nearly constant rate in nanomolar concentrations with high bioactivity, given the same formulation conditions. Vascular endothelial gro...

journal_title：Pharmaceutical research

authors： Gu F,Neufeld R,Amsden B

更新日期：2006-04-01 00:00:00

abstract：PURPOSE:Although flomoxef (FMOX) has attracted substantial attention as an antibiotic against extended-spectrum beta-lactamase-producing Escherichia coli (ESBL-producing E. coli), the pharmacokinetics/pharmacodynamics (PK/PD) characteristics of FMOX against ESBL-producing E. coli is unclear. The aim of this study was t...

journal_title：Pharmaceutical research

authors： Tashiro S,Hayashi M,Takemura W,Igarashi Y,Liu X,Mizukami Y,Kojima N,Enoki Y,Taguchi K,Yokoyama Y,Nakamura T,Matsumoto K

更新日期：2021-01-06 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：PURPOSE:To apply physiologically-based pharmacokinetic (PBPK) modeling to investigate the consequences of reduction in activity of hepatic and intestinal uptake and efflux transporters by cyclosporine and its metabolite AM1. METHODS:Inhibitory potencies of cyclosporine and AM1 against OATP1B1, OATP1B3 and OATP2B1 were...

journal_title：Pharmaceutical research

authors： Gertz M,Cartwright CM,Hobbs MJ,Kenworthy KE,Rowland M,Houston JB,Galetin A

更新日期：2013-03-01 00:00:00

abstract：PURPOSE:The heats of reaction between the enantiomers and racemates of ibuprofen and naproxen and human serum albumin (HSA) are to be measured with and without the addition of octanoic acid. The effects of octanoic acid on the free energies of interaction between the drugs and HSA is to be determined and compared to th...

journal_title：Pharmaceutical research

authors： Cheruvallath VK,Riley CM,Narayanan SR,Lindenbaum S,Perrin JH

更新日期：1996-01-01 00:00:00

abstract：PURPOSE:Cationic host defence peptides constitute a promising class of therapeutic drug leads with a wide range of therapeutic applications, including anticancer therapy, immunomodulation, and antimicrobial activity. Although potent and efficacious, systemic toxicity and low chemical stability have hampered their comme...

journal_title：Pharmaceutical research

authors： Water JJ,Kim Y,Maltesen MJ,Franzyk H,Foged C,Nielsen HM

更新日期：2015-08-01 00:00:00

abstract：:The effects of tertiary amine-containing basic drugs on the enzymes located in the mitochondria and the effect of monoamine oxidase inhibitors (MAOIs) on drug accumulation in lung mitochondria have been studied. Various basic drugs inhibited MAO activity but not other mitochondrial marker enzymes. The potency of MAO i...

journal_title：Pharmaceutical research

authors： Yoshida H,Kamiya A,Okumura K,Hori R

更新日期：1989-10-01 00:00:00

abstract：PURPOSE:To determine whether LHRH-receptor is expressed in Calu-3, a human bronchial epithelial cell line, and to further determine whether this receptor plays a role in the transport of deslorelin, an LHRH agonist. METHODS:Using cultured monolayers of Calu-3 grown at air-interface, the presence and localization of LH...

journal_title：Pharmaceutical research

authors： Koushik K,Bandi N,Sundaram S,Kompella UB

更新日期：2004-06-01 00:00:00

abstract：:The crystal growth kinetics of theophylline monohydrate from aqueous buffered supersaturated solutions were investigated at 10, 20, 30, and 40 degrees C. Crystallization experiments were carried out isothermally at pH 6. During growth the crystal count and size distributions were monitored in situ. The growth rate was...

journal_title：Pharmaceutical research

authors： Rodríguez-Hornedo N,Wu HJ

更新日期：1991-05-01 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 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：PURPOSE:We have already demonstrated that the HMG-CoA reductase inhibitor, pravastatin is actively taken up by isolated rat hepatocytes via a multispecific anion transporter (Yamazaki et al., Am. J. Physiol. 264, G36-44, (1993)). We further attempted the quantitative evaluation of this uptake in different experimental ...

journal_title：Pharmaceutical research

authors： Ishigami M,Tokui T,Komai T,Tsukahara K,Yamazaki M,Sugiyama Y

更新日期：1995-11-01 00:00:00

abstract：:The interaction of dicumarol and phenothiazine neuroleptics binding to alpha 1-acid glycoprotein (AGP) was investigated by circular dichroism (CD) and equilibrium dialysis. The induced CD spectra of the dicumarol-AGP complex were affected differently by the different substituents of the phenothiazine molecule. The sig...

journal_title：Pharmaceutical research

authors： Miyoshi T,Yamamichi R,Maruyama T,Otagiri M

更新日期：1992-07-01 00:00:00

abstract：:Monte Carlo simulation technique used to evaluate the effect of the arrangement of concentrations on the efficiency of estimation of population pharmacokinetic parameters in the preclinical setting is described. Although the simulations were restricted to the one compartment model with intravenous bolus input, they pr...

journal_title：Pharmaceutical research

authors： Ette EI,Howie CA,Kelman AW,Whiting B

更新日期：1995-05-01 00:00:00

abstract：PURPOSE:The United States Pharmacopoeia (USP) imposes strict requirements on the geometry and operating conditions of the USP Dissolution Testing Apparatus II. A previously validated Computational Fluid Dynamics (CFD) approach was used here to study the hydrodynamics of USP Apparatus II when the impeller was placed at ...

journal_title：Pharmaceutical research

authors： Bai G,Armenante PM

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:The major goal of this study was to compare the relative utility of the Hanson Microette and the Van Kel apparatus, two fully automated devices, as in vitro release tests (IVRT) for semisolids. We attempted to develop methodology that can be used to discriminate formulation changes, and to evaluate the precisio...

journal_title：Pharmaceutical research

authors： Rapedius M,Blanchard J

更新日期：2001-10-01 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：:Interleukin-1 receptor antagonist (IL-1Ra) is a naturally occurring anti-inflammatory antagonist of interleukin-1 family of pro-inflammatory cytokines. The broad spectrum anti-inflammatory effects of IL-1Ra have been investigated against various auto-immune diseases such as diabetes mellitus, rheumatoid arthritis. Des...

journal_title：Pharmaceutical research

authors： Akash MS,Rehman K,Chen S

更新日期：2013-11-01 00:00:00

abstract：PURPOSE:Proteasome inhibition induces endoplasmic reticulum (ER) stress and compensatory autophagy to relieve ER stress. Disturbance of intracellular calcium homeostasis can lead to ER stress and alter the autophagy process. It has been suggested that inhibition of the proteasome disrupts intracellular calcium homeosta...

journal_title：Pharmaceutical research

authors： Williams JA,Hou Y,Ni HM,Ding WX

更新日期：2013-09-01 00:00:00

abstract：:Aucubin, a promising hepatoprotecting iridoid glucoside, was given intravenously (iv), orally (po), intraperitoneally (ip), and hepatoportally (pv) to rats. A linear pharmacokinetic behavior was obtained after iv administation of 400-400 mg/kg of aucubin. The half-life of aucubin in the postdistributive phase (t1/2, b...

journal_title：Pharmaceutical research

authors： Suh NJ,Shim CK,Lee MH,Kim SK,Chang IM

更新日期：1991-08-01 00:00:00

abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...

journal_title：Pharmaceutical research

authors： Sasaki I,Tamura T,Shibakawa T,Fujita T,Murakami M,Yamamoto A,Muranishi S

更新日期：1997-08-01 00:00:00

abstract：PURPOSE:To investigate differences in the cellular uptake and intracellular distribution of protein-bound doxorubicin in comparison to free doxorubicin and a liposomal formulation (CAELYX) METHODS: LXFL 529 lung carcinoma cells were incubated with an acid-sensitive transferrin and albumin conjugate of doxorubicin, a st...

journal_title：Pharmaceutical research

authors： Beyer U,Rothern-Rutishauser B,Unger C,Wunderli-Allenspach H,Kratz F

更新日期：2001-01-01 00:00:00

abstract：PURPOSE:To determine the mechanism(s) by which effervescence induces penetration enhancement of a broad range of compounds ranging in size, structure, and other physiocochemical properties across rat and rabbit small intestinal epithelium. METHODS:Effervescent induced penetration enhancement was investigated in vitro ...

journal_title：Pharmaceutical research

authors： Eichman JD,Robinson JR

更新日期：1998-06-01 00:00:00

abstract：PURPOSE:A novel infusion system (PatchPump®) has been developed using an electrochemical actuator and a semi-flexible container to deliver liquid formulations through an infusion set. In vitro studies characterized pump performance, and clinical studies evaluated functionality and pharmacokinetic (PK) performance in hu...

journal_title：Pharmaceutical research

authors： Shaked A,Tenenbaum-Koren E,Atsmon J,Noymer P

更新日期：2016-01-01 00:00:00

abstract：PURPOSE:Delivery of apoptosis-inducing compounds to hepatic stellate cells (HSC) may be an effective strategy to reverse liver fibrosis. The aim of this study was therefore to examine the selective targeting of the apoptosis-inducing drug 15-deoxy-delta12,14-prostaglandin J2 (15dPGJ2) with two different HSC-carriers: h...

journal_title：Pharmaceutical research

authors： Hagens WI,Mattos A,Greupink R,de Jager-Krikken A,Reker-Smit C,van Loenen-Weemaes A,Gouw IA,Poelstra K,Beljaars L

更新日期：2007-03-01 00:00:00

abstract：PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...

journal_title：Pharmaceutical research

authors： Nihal M,Roelke CT,Wood GS

更新日期：2010-06-01 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:Three types of acyl tetragastrin (TG), acetyl-TG (C2-TG), butyryl-TG (C4-TG) and caproyl-TG (C6-TG) were synthesized and their in vitro intestinal permeability characteristics were examined using Caco-2 monolayers. METHODS:The disappearance of acyl-TGs from the apical side of Caco-2 monolayers was estimated by...

journal_title：Pharmaceutical research

authors： Fujita T,Kawahara I,Quan Y,Hattori K,Takenaka K,Muranishi S,Yamamoto A

更新日期：1998-09-01 00:00:00

abstract：PURPOSE:Studies were conducted to investigate dilute solutions of the monoclonal antibody (mAb) bevacizumab, mAb fragment ranibizumab and fusion protein aflibercept, develop common procedures for formulation of low concentration mAbs and identify a stabilizing formulation for anti-VEGF mAbs for use in in vitro permeati...

journal_title：Pharmaceutical research

authors： Giannos SA,Kraft ER,Zhao ZY,Merkley KH,Cai J

更新日期：2018-02-28 00:00:00