Leukotriene biosynthesis inhibitors.

abstract：PURPOSE:Anticancer chemotherapy usually involves the administration of several anticancer drugs that differ in their action mechanisms. Here, we aimed to test whether the combination of omacetaxine mepesuccinate (OMT) and doxorubicin (DOX) could show synergism, and whether the liposomal co-delivery of these two drugs c...

journal_title：Pharmaceutical research

authors： Shim G,Lee S,Choi J,Lee S,Kim CW,Oh YK

更新日期：2014-08-01 00:00:00

abstract：BACKGROUND:With the recent approval of the first small interfering RNA (siRNA) therapeutic formulated as nanoparticles, there is increased incentive for establishing the factors of importance for the design of stable solid dosage forms of such complex nanomedicines. METHODS:The aims of this study were: (i) to identify...

journal_title：Pharmaceutical research

authors： Dormenval C,Lokras A,Cano-Garcia G,Wadhwa A,Thanki K,Rose F,Thakur A,Franzyk H,Foged C

更新日期：2019-08-02 00:00:00

abstract：PURPOSE:The work aims at investigating the correlation of water sorption potential with different measures of molecular mobility in an annealed amorphous model compound (trehalose). METHODS:Amorphous trehalose, prepared by freeze-drying, was annealed at 100°C (17°C < T (g)) for up to 120 h. Global mo...

journal_title：Pharmaceutical research

authors： Bhardwaj SP,Suryanarayanan R

更新日期：2013-03-01 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:To determine the pharmacokinetics of GS-522, an oligodeoxynucleotide (GGTTGGTGTGGTTGG) inhibitor of thrombin, after constant infusion and bolus administration in the cynomolgus monkey. METHODS:Using a stability indicating HPLC method, the GS-522 plasma concentration versus time data were obtained after constan...

journal_title：Pharmaceutical research

authors： Lee WA,Fishback JA,Shaw JP,Bock LC,Griffin LC,Cundy KC

更新日期：1995-12-01 00:00:00

abstract：PURPOSE:To determine by pharmacokinetic (PK) means the role of erythropoietin-receptor (EPO-R) upregulation in fetuses on the elimination of erythropoietin (EPO). MATERIALS AND METHODS:Six fetal sheep were catheterized at a gestational age of 125-127 days and phlebotomized daily for 6 days. Paired tracer PK studies us...

journal_title：Pharmaceutical research

authors： Freise KJ,Widness JA,Segar JL,Schmidt RL,Veng-Pedersen P

更新日期：2007-09-01 00:00:00

abstract：PURPOSE:The aim of this study was to examine if sparging with CO2(g) could be used to establish stable biorelevant bicarbonate buffers, in aqueous medium, for use in dissolution characterization of low-solubility ionizable drugs. METHODS:Preparation of the bicarbonate-containing dissolution medium was monitored by use...

journal_title：Pharmaceutical research

authors： McNamara DP,Whitney KM,Goss SL

更新日期：2003-10-01 00:00:00

abstract：PURPOSE:Simvastatin (SIM), a HMG-CoA reductase inhibitor widely prescribed for hypercholesterolemia, has been reported to ameliorate inflammation and promote osteogenesis. Its clinical applications on these potential secondary indications, however, have been hampered by its lack of osteotropicity and poor water solubil...

journal_title：Pharmaceutical research

authors： Wang X,Jia Z,Almoshari Y,Lele SM,Reinhardt RA,Wang D

更新日期：2018-06-25 00:00:00

abstract：:Inhibition of efflux pumps is an emerging approach in cancer therapy and drug delivery. Since it has been discovered that polymeric pharmaceutical excipients such as Tweens or Pluronics can inhibit efflux pumps, various other polymers have been investigated regarding their potential efflux pump inhibitory activity. Am...

journal_title：Pharmaceutical research

authors： Werle M

更新日期：2008-03-01 00:00:00

abstract：PURPOSE:To evaluate the influence of the main biopharmaceutical factors on the viability of a new probiotic yeast strain, using dynamic in vitro systems simulating human gastric/small intestinal (TIM) and large intestinal (ARCOL) environments. METHODS:The viability of Saccharomyces cerevisiae CNCM I-3856 throughout th...

journal_title：Pharmaceutical research

authors： Blanquet-Diot S,Denis S,Chalancon S,Chaira F,Cardot JM,Alric M

更新日期：2012-06-01 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：PURPOSE:Induction of cell-mediated immune (CMI) responses is crucial for vaccine-mediated protection against difficult vaccine targets, e.g., Chlamydia trachomatis (Ct). Adjuvants are included in subunit vaccines to potentiate immune responses, but many marketed adjuvants stimulate predominantly humoral immune response...

journal_title：Pharmaceutical research

authors： Schmidt ST,Neustrup MA,Harloff-Helleberg S,Korsholm KS,Rades T,Andersen P,Christensen D,Foged C

更新日期：2017-08-01 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:To evaluate the use of an in vitro intestinal permeability model to predict rat and human absorption as well as to evaluate the use of an internal standard to control for intra- and inter-rat variability. METHODS:In vivo peroral absorption and in vitro steady-state intestinal permeability coefficients were det...

journal_title：Pharmaceutical research

authors： Dowty ME,Dietsch CR

更新日期：1997-12-01 00:00:00

abstract：PURPOSE:Formulate phospho-sulindac (P-S, OXT-328) in a Pluronic hydrogel to be used as a topical anti-inflammatory agent and study its efficacy, safety and pharmacokinetics in an arthritis model. METHODS:LEW/crlBR rats with Freund's adjuvant-induced arthritis were treated with P-S formulated in Pluronic hydrogel (PSH)...

journal_title：Pharmaceutical research

authors： Mattheolabakis G,Mackenzie GG,Huang L,Ouyang N,Cheng KW,Rigas B

更新日期：2013-06-01 00:00:00

abstract：PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...

journal_title：Pharmaceutical research

authors： Baginski L,Tewes F,Buckley ST,Healy AM,Bakowsky U,Ehrhardt C

更新日期：2012-01-01 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：: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:An in vitro dynamic pharmacokinetic (PK) cell culture system was developed to more precisely simulate physiologic nanoparticle/drug exposure. METHODS:A dynamic PK cell culture system was developed to more closely reflect physiologic nanoparticle/drug concentrations that are changing with time. Macrophages were...

journal_title：Pharmaceutical research

authors： Kutscher HL,Morse GD,Prasad PN,Reynolds JL

更新日期：2019-02-01 00:00:00

abstract：:Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...

journal_title：Pharmaceutical research

authors： Akula MR,Matowe WC,Wolowyk MW,Knaus EE

更新日期：1990-09-01 00:00:00

abstract：PURPOSE:In pharmacokinetic (PK)/pharmacodynamic (PD) modelling and simulations (M&S), omitting dropouts can cause inaccuracies in parameter estimation and clinical trial simulations (CTS). This study examines the impact of different imputation methods for missing data on the interpretation of model results, as well as ...

journal_title：Pharmaceutical research

authors： Yuen E,Gueorguieva I,Aarons L

更新日期：2014-10-01 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:Indomethacin is well known to be metabolized via O-demethylation and N-deacylation. In this paper we found an enzyme involved in the hydrolysis of amide-linkage of indomethacin and partially characterized it as well as its substrate specificity. METHODS:An indomethacin hydrolyzing enzyme was purified to homoge...

journal_title：Pharmaceutical research

authors： Terashima K,Takai S,Usami Y,Adachi T,Sugiyama T,Katagiri Y,Hirano K

更新日期：1996-09-01 00:00:00

abstract：PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...

journal_title：Pharmaceutical research

authors： Mason-Smith N,Duke DJ,Kastengren AL,Stewart PJ,Traini D,Young PM,Chen Y,Lewis DA,Soria J,Edgington-Mitchell D,Honnery D

更新日期：2016-05-01 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:Overexpression of the serine protease urokinase (uPA) is recognised as an important biomarker of metastatic disease and a druggable anticancer target. Plasminogen activator inhibitor type-2 (PAI-2/SerpinB2) is a specific uPA inhibitor with proven potential for use in targeted therapy. However, PAI-2 is rapidly ...

journal_title：Pharmaceutical research

authors： Vine KL,Lobov S,Indira Chandran V,Harris NL,Ranson M

更新日期：2015-03-01 00:00:00

abstract：PURPOSE:This study compared gene expression profiles in mouse lungs after administration of the cationic polymers polyethyleneimine (PEI) or chitosan alone or formulated with a luciferase reporter plasmid (PEI-pLuc, chitosan-pLuc). METHODS:The polymers and formulations were administered intratracheally to Balb/c mice ...

journal_title：Pharmaceutical research

authors： Regnström K,Ragnarsson EG,Fryknäs M,Köping-Höggård M,Artursson P

更新日期：2006-03-01 00:00:00

abstract：PURPOSE:Levofloxacin, a quinolone antibacterial drug, is a zwitterion at physiological pH. We examined the effect of cationic and anionic drugs on renal excretion of levofloxacin by means of in vivo clearance to characterize the mechanisms of renal excretion of this drug. METHODS:In vivo clearance was studied in male ...

journal_title：Pharmaceutical research

authors： Yano I,Ito T,Takano M,Inui K

更新日期：1997-04-01 00:00:00

abstract：PURPOSE:To assess the effects of selective lipid extraction and tape stripping on transepidermal water loss (TEWL) at three body regions in the pig. METHODS:Lipids were extracted from the abdominal, inguinal. and back regions using three different solvent extraction procedures or cellophane tape stripping (15x) on Yor...

journal_title：Pharmaceutical research

authors： Monteiro-Riviere NA,Inman AO,Mak V,Wertz P,Riviere JE

更新日期：2001-07-01 00:00:00

abstract：PURPOSE:The Caco-2 association of lectin-grafted PLGA-nanospheres was investigated compared to plain and BSA-coated spheres. METHODS:Nanospheres made from fluorescent-labeled PLGA were coated with wheat germ agglutinin (WGA) or BSA and incubated with Caco-2 monolayers varying the concentration of nanospheres, the time...

journal_title：Pharmaceutical research

authors： Weissenboeck A,Bogner E,Wirth M,Gabor F

更新日期：2004-10-01 00:00:00