16 alpha-hydroxy-(-)-kauranoic acid: a selectively cytotoxic diterpene from Annona bullata.

abstract：:A rapid quantitative, enantioselective HPLC method for the analysis of the four stereoisomers, (+) and (-) erythro and (+) and (-) threo forms, of mefloquine has been developed using a Chiralpak Ad analytical column containing amylose tris-3,5-dimethylphenyl carbonate coated on silica gel and hexane/ethanol/diethylami...

journal_title：Pharmaceutical research

authors： Qiu Y,Kitamura S,Guillory JK

更新日期：1992-12-01 00:00:00

abstract：PURPOSE:Previous studies by other investigators have shown an enhancement of mitomycin C (MMC) activity at acidic extracellular pH (pHe) in monolayer cultures of human cells. The goal of the present study was to determine if the efficacy of intravesical MMC therapy in patients treated for superficial bladder cancer can...

journal_title：Pharmaceutical research

authors： Yen WC,Schmittgen T,Au JL

更新日期：1996-12-01 00:00:00

abstract：PURPOSE:The growing amount of heterogeneous bioactivity data requires effective strategies to assess the promiscuity/selectivity of small-molecules and aid drug discovery. In the current study, we aim to evaluate the potential of assay profiles (APs, i.e., unique combinations of assay-related features describing how ac...

journal_title：Pharmaceutical research

authors： Avram S,Curpan R,Bora A,Neanu C,Halip L

更新日期：2018-10-18 00:00:00

abstract：PURPOSE:To determine the correlation among progesterone dose, rate of import of progesterone-occupied progesterone receptor (PR) complexes into the nucleus of cells, and transcriptional activity of progesterone-PR complexes. METHODS:Live cell imaging and time-lapse microscopy of green fluorescent protein-tagged PR wer...

journal_title：Pharmaceutical research

authors： Li H,Yan G,Kern SE,Lim CS

更新日期：2003-10-01 00:00:00

abstract：PURPOSE:To identify High Molecular Weight Products (HMWP) formed in human insulin formulation during storage. METHODS:Commercial formulation of human insulin was stored at 37°C for 1 year and HMWP was isolated using preparative size exclusion chromatography (SEC) and reverse phase (RP) chromatography. The primary stru...

journal_title：Pharmaceutical research

authors： Hjorth CF,Hubálek F,Andersson J,Poulsen C,Otzen D,Naver H

更新日期：2015-06-01 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:Topoisomerase II (Topo II) preferentially cuts DNA at alternating purine-pyrimidine repeats. Different Topo II poisons may affect Topo II to produce distinct drug-specific DNA cleavage patterns. GL331 is a new podophyllotoxin derivative exhibiting potent Topo II-poisoning activity. Therefore, the sequence selec...

journal_title：Pharmaceutical research

authors： Lee CC,Huang TS

更新日期：2001-06-01 00:00:00

abstract：PURPOSE:The present study evaluates immobilized artificial membrane (IAM) chromatography for predicting drug permeability across the blood-brain barrier (BBB) and outlines the potential and limitations of IAMs as a predictive tool by comparison with conventional methods based on octanol/water partitioning and octadecyl...

journal_title：Pharmaceutical research

authors： Reichel A,Begley DJ

更新日期：1998-08-01 00:00:00

abstract：PURPOSE:The effects of liposomes on nitric oxide (NO) production from mouse peritoneal macrophages following intraperitoneal injection of liposomes were investigated. METHODS:Mouse peritoneal macrophages were collected following intraperitoneal injection of liposomes and cultured with and without lipopolysaccharide (L...

journal_title：Pharmaceutical research

authors： Aramaki Y,Arima H,Hara T,Tsuchiya S

更新日期：1996-09-01 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

abstract：:We report the chemical and enzymatic hydrolysis of two hydrophobic prodrugs of ganciclovir (3 = dipropionate ester; 4 = diadamantoate ester). Both prodrugs undergo hydrolysis showing a pH dependence of kobs = kH+aH+ + ko + kHO-aHO- and a pH of maximum stability near pH 5. Only 4 exhibited a shelf life (t90) greater th...

journal_title：Pharmaceutical research

authors： Powell MF,Magill A,Chu N,Hama K,Mau CI,Foster L,Bergstrom R

更新日期：1991-11-01 00:00:00

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:Studies were conducted to evaluate whether the use of an in vitro model of the blood-brain barrier (BBB) resulted in more accurate predictions of the in vivo transport of compounds compared to the use of a human intestinal cell line (Caco-2). METHODS:The in vitro BBB model employs bovine brain capillary endoth...

journal_title：Pharmaceutical research

authors： Lundquist S,Renftel M,Brillault J,Fenart L,Cecchelli R,Dehouck MP

更新日期：2002-07-01 00:00:00

abstract：:The absorption of insulin across the vaginal mucosa into the systemic circulation was studied in ovariectomized rats given subsequent estrogen treatment. Blood glucose levels were determined as an indirect measure of insulin absorption, and the effect of various enhancers on the hypoglycemic response was investigated....

journal_title：Pharmaceutical research

authors： Richardson JL,Illum L,Thomas NW

更新日期：1992-07-01 00:00:00

abstract：:Over the last few decades, intraperitoneal (IP) local drug delivery, providing high drug concentrations with prolonged retention in the peritoneal cavity, has opened a new horizon for the management of life-threatening peritoneal disorders, such as peritoneal carcinomatosis (PC). However, clinical translation of this ...

journal_title：Pharmaceutical research

authors： Alavi S,Haeri A,Mahlooji I,Dadashzadeh S

更新日期：2020-06-03 00:00:00

abstract：PURPOSE:To study the use of poly (lactide-co-glycolide) (PLGA) microparticles in respirable sizes as carriers for recombinant tuberculosis (TB) antigen, TB10.4-Ag85B, with the ultimate goal of pulmonary delivery as vaccine for the prevention of TB. MATERIALS AND METHODS:Recombinant TB antigens were purified from E. co...

journal_title：Pharmaceutical research

authors： Shi S,Hickey AJ

更新日期：2010-02-01 00:00:00

abstract：:The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...

journal_title：Pharmaceutical research

authors： Stebler T,Guentert TW

更新日期：1992-10-01 00:00:00

abstract：PURPOSE:The purpose of this research was to evaluate the effect of ultrasound on mass transport across fetal membrane for direct fetal drug delivery and sensing of the amniotic fluid in a noninvasive manner. METHODS:Post-delivery human fetal membranes (chorioamnion) were used for in vitro experiments, in which the eff...

journal_title：Pharmaceutical research

authors： Wolloch L,Azagury A,Goldbart R,Traitel T,Groisman G,Hallak M,Kost J

更新日期：2015-02-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate transepithelial ionic permeation via the paracellular pathway of human Caco-2 epithelial monolayers and its contribution to absorption of the base guanidine. METHODS:Confluent monolayers of Caco-2 epithelial cells were mounted in Ussing chambers and the transepithelial ...

journal_title：Pharmaceutical research

authors： Carr G,Haslam IS,Simmons NL

更新日期：2006-03-01 00:00:00

abstract：PURPOSE:To evaluate 26 marketed oncology drugs for time-dependent inhibition (TDI) of cytochrome P450 (CYP) enzymes. Evaluate TDI-positive drugs for potential to generate reactive intermediates. Assess clinical drug-drug interaction (DDI) risk using static mechanistic models. METHODS:Human liver microsomes and CYP-spe...

journal_title：Pharmaceutical research

authors： Kenny JR,Mukadam S,Zhang C,Tay S,Collins C,Galetin A,Khojasteh SC

更新日期：2012-07-01 00:00:00

abstract：PURPOSE:Radial basis function artificial neural networks and theoretical descriptors were used to develop a quantitative structure-pharmacokinetic relationship for structurally diverse drug compounds. METHODS:Human bioavailability values were taken from the literature and descriptors were generated from the drug struc...

journal_title：Pharmaceutical research

authors： Turner JV,Maddalena DJ,Agatonovic-Kustrin S

更新日期：2004-01-01 00:00:00

abstract：PURPOSE:A Selegiline Transdermal System (STS) is under development for indications which may not be optimally or safely treated with oral selegiline. Studies were conducted to evaluate the in vitro penetration and skin metabolism of selegiline in order to better understand the toxicological findings and the observed pl...

journal_title：Pharmaceutical research

authors： Rohatagi S,Barrett JS,McDonald LJ,Morris EM,Darnow J,DiSanto AR

更新日期：1997-01-01 00:00:00

abstract：:The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate (DDAIP) on epithelial membrane lipids was examined using human buccal cell membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC) were la...

journal_title：Pharmaceutical research

authors： Turunen TM,Urtti A,Paronen P,Audus KL,Rytting JH

更新日期：1994-02-01 00:00:00

abstract：PURPOSE:For the assessment of bioequivalence it is assumed that drug clearance in each subject on each of the study days is the same and any observed differences in AUC and/or Cmax between a brand and generic formulation are due to differences in bioavailability. We hypothesized that this assumption was invalid for hig...

journal_title：Pharmaceutical research

authors： Tsang YC,Pop R,Gordon P,Hems J,Spino M

更新日期：1996-06-01 00:00:00

abstract：PURPOSE:Carboxylesterases are important in the detoxification of drugs, pesticides and other xenobiotics. This study was to evaluate a series of substrates and inhibitors for characterizing these enzymes. METHODS:A series of novel aliphatic esters and thioesters were used in spectral assays to monitor human, murine an...

journal_title：Pharmaceutical research

authors： Huang TL,Shiotsuki T,Uematsu T,Borhan B,Li QX,Hammock BD

更新日期：1996-10-01 00:00:00

abstract：PURPOSE:Previously, we have shown that complexes of plasmid DNA with the biodegradable polymer poly(2-dimethylamino ethylamino)phosphazene (p(DMAEA)-ppz) mediated tumor selective gene expression after intravenous administration in mice. In this study, we investigated the effect of p(DMAEA)-ppz molecular weight on both ...

journal_title：Pharmaceutical research

authors： de Wolf HK,de Raad M,Snel C,van Steenbergen MJ,Fens MH,Storm G,Hennink WE

更新日期：2007-08-01 00:00:00

abstract：:Human serum albumin (HSA) was encapsulated in a 50:50 copolymer of DL-lactide/glycolide in the form of microspheres. These microspheres were used as a model formulation to study the feasibility of controlling the release of large proteins over a 20- to 30-day period. We show that HSA can be successfully incorporated i...

journal_title：Pharmaceutical research

authors： Hora MS,Rana RK,Nunberg JH,Tice TR,Gilley RM,Hudson ME

更新日期：1990-11-01 00:00:00

abstract：PURPOSE:This study aimed to characterize the transepithelial transport of miltefosine (HePC), the first orally effective drug against visceral leishmaniasis, across the intestinal barrier to further understand its oral absorption mechanism. MATERIALS AND METHODS:Caco-2 cell monolayers were used as an in vitro model of...

journal_title：Pharmaceutical research

authors： Ménez C,Buyse M,Dugave C,Farinotti R,Barratt G

更新日期：2007-03-01 00:00:00

abstract：PURPOSE:A pattern fitting procedure using X-ray powder diffraction patterns was applied to study the crystallization kinetics of amorphous griseofulvin. From the optimized parameters obtained by pattern fitting, a change in the quantity and quality of griseofulvin crystals with crystallization was also investigated. M...

journal_title：Pharmaceutical research

authors： Yamamura S,Takahira R,Momose Y

更新日期：2007-05-01 00:00:00

abstract：:We describe an assay for acrolein in urine, employing derivatization with m-aminophenol in the presence of ferrous sulfate solution in sulfuric acid. The derivative (7-OH quinoline; DER) and the internal standard (quinine-bisulfate; IS) were separated on a 10-micron particle, 8 mm x 10-cm C18 cartridge in conjunction ...

journal_title：Pharmaceutical research

authors： al-Rawithi S,el-Yazigi A,Nicholls PJ

更新日期：1993-11-01 00:00:00