The relationship of pKa and acute skin irritation in man.

abstract：PURPOSE:In this study, a new modified nanoprecipitation approach that more efficient and simpler than conventional approach was developed to synthesize D-alpha-Tocopheryl polyethylene glycol 1000 succinate stabilized liposome-PLGA hybrid nanoparticle, loaded with simvastatin (ST-TLPN). METHODS:The optimum formulation ...

journal_title：Pharmaceutical research

authors： Zhang M,He J,Zhang W,Liu J

更新日期：2018-08-30 00:00:00

abstract：:A method is described for the assay of phenobarbital N-glucosylation using UDP-D-[6-3H]glucose. The radioactive phenobarbital N-glucoside conjugates [(5R)-PBG, (5S)-PBG] formed during the incubations were resolved from each other and from uncharacterized radioactive products by semipreparative HPLC. The product ratio ...

journal_title：Pharmaceutical research

authors： Soine WH,Safi H,Westkaemper RB

更新日期：1992-05-01 00:00:00

abstract：PURPOSE:Since the molecular mechanism of the cell cycle was established, various theoretical models of this process have been developed. A recent study revealed significant variability in cell cycle duration between mother and daughter cells, but this observation has not been incorporated into the theoretical models. ...

journal_title：Pharmaceutical research

authors： Bae H,Go YH,Kwon T,Sung BJ,Cha HJ

更新日期：2019-02-22 00:00:00

abstract：PURPOSE:For passive dry powder inhalers (DPIs) entrainment and emission of the aerosolized drug dose depends strongly on device geometry and the patient's inhalation manoeuvre. We propose a computational method for optimizing the entrainment part of a DPI. The approach assumes that the pulmonary delivery location of ae...

journal_title：Pharmaceutical research

authors： Kopsch T,Murnane D,Symons D

更新日期：2016-11-01 00:00:00

abstract：PURPOSE:Novel itraconazole (ITZ)-based dry powders for inhalation (DPI) were optimized for aerodynamic and dissolution properties and contained excipients that are acceptable for inhalation. METHODS:The DPI were produced by spray drying solutions. The drug content, crystallinity state, and morphological evaluation of ...

journal_title：Pharmaceutical research

authors： Duret C,Wauthoz N,Sebti T,Vanderbist F,Amighi K

更新日期：2012-10-01 00:00:00

abstract：PURPOSE:To investigate cellular uptake pathways of novel anionic siRNA-lipoplexes as a function of formulation composition. METHODS:Anionic formulations with anionic lipid/Ca(2+)/siRNA ratio of 1.3/2.5/1 (AF1) and 1.3/0.3/1 (AF2) were utilized. Uptake mechanisms were investigated using uptake inhibition and co-localiz...

journal_title：Pharmaceutical research

authors： Kapoor M,Burgess DJ

更新日期：2013-04-01 00:00:00

abstract：PURPOSE:To provide a systematic biophysical approach towards a better understanding of impact of conjugation chemistry on higher order structure and physical stability of an antibody drug conjugate (ADC). METHODS:ADC was prepared using thiol-maleimide chemistry. Physical stabilities of ADC and its parent IgG1 mAb were...

journal_title：Pharmaceutical research

authors： Guo J,Kumar S,Prashad A,Starkey J,Singh SK

更新日期：2014-07-01 00:00:00

abstract：PURPOSE:The cause of antibody positive pure red cell aplasia associated with the subcutaneous administration of EPREX to patients with chronic kidney failure has been determined to be due to the leaching of weakly adjuvant compounds from the uncoated rubber stoppers that were formerly used in prefilled syringes. Other ...

journal_title：Pharmaceutical research

authors： Villalobos AP,Gunturi SR,Heavner GA

更新日期：2005-07-01 00:00:00

abstract：PURPOSE:The aim of this work was to evaluate whether improved topical delivery of finasteride, focussed to the hair follicles of human scalp skin could be achieved with application of short durations of heat and use of specific chemical penetration enhancers. METHODS:Franz cell experiments with human scalp skin were p...

journal_title：Pharmaceutical research

authors： Farah HA,Brown MB,McAuley WJ

更新日期：2020-05-31 00:00:00

abstract：:The pharmacokinetics of 2',3'-dideoxyinosine (ddI) were examined in rats given intravenous doses of 8, 40, or 200 mg/kg. The concentrations of ddI in whole blood and plasma were identical. The concentration decline was multiexponential, with mean half-lives of 2 and 20 min for the first and second phases, respectively...

journal_title：Pharmaceutical research

authors： Wientjes MG,Mukherji E,Au JL

更新日期：1992-08-01 00:00:00

abstract：:The synthesis of an homologous series of new water-soluble derivatives of pilocarpine is described. The new compounds, referred to as soft quaternary salts, are water soluble by virtue of a cationic ammonium head and their lipophilicity can be modulated by manipulating the size and the nature of the substituent in the...

journal_title：Pharmaceutical research

authors： Druzgala P,Winwood D,Drewniak-Deyrup M,Smith S,Bodor N,Kaminski JJ

更新日期：1992-03-01 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: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: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:This work describes a method for functionalisation of nanoparticle surfaces with hydrophilic "nano-shields" and the application of advanced surface characterisation to determine PEG amount and accumulation at the outmost 10 nm surface that is the predominant factor in determining protein and cellular interactio...

journal_title：Pharmaceutical research

authors： Ebbesen MF,Whitehead B,Ballarin-Gonzalez B,Kingshott P,Howard KA

更新日期：2013-07-01 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:Development of a human mitochondrial gene delivery vector is a critical step in the ability to treat diseases arising from mutations in mitochondrial DNA. Although we have previously cloned the mouse mitochondrial genome in its entirety and developed it as a mitochondrial gene therapy vector, the human mitochon...

journal_title：Pharmaceutical research

authors： Bigger BW,Liao AY,Sergijenko A,Coutelle C

更新日期：2011-11-01 00:00:00

abstract：PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...

journal_title：Pharmaceutical research

authors： Chen D,Song SH,Wientjes MG,Yeh TK,Zhao L,Villalona-Calero M,Otterson GA,Jensen R,Grever M,Murgo AJ,Au JL

更新日期：2006-06-01 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：PURPOSE:The purpose of this study is to show how disaccharides differ in their ability to protect lyophilized β-galactosidase from enzymatic activity loss and secondary structure changes during storage. METHODS:β-galactosidase was lyophilized with trehalose, sucrose, cellobiose or melibiose at 2:1, 20:1 and 40:1 excip...

journal_title：Pharmaceutical research

authors： Heljo VP,Jouppila K,Hatanpää T,Juppo AM

更新日期：2011-03-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the depth-dependent intradermal immunogenicity of inactivated polio vaccine (IPV) delivered by depth-controlled microinjections via hollow microneedles (HMN) and to investigate antibody response enhancing effects of IPV immunization adjuvanted with CpG oligodeoxynucleoti...

journal_title：Pharmaceutical research

authors： Schipper P,van der Maaden K,Romeijn S,Oomens C,Kersten G,Jiskoot W,Bouwstra J

更新日期：2016-09-01 00:00:00

abstract：:Chimeric L6 is a mouse-human monoclonal antibody specific for tumor cell-associated antigens. The factors affecting the physical and chemical stability of chimeric L6 were assessed at elevated temperatures (30-60 degrees C) and by multiple freezing and thawing. Three routes of degradation were observed: chemical degra...

journal_title：Pharmaceutical research

authors： Paborji M,Pochopin NL,Coppola WP,Bogardus JB

更新日期：1994-05-01 00:00:00

abstract：PURPOSE:Characterization of virosomes, in late stage preclinical development as vaccines for Respiratory Syncytial Virus (RSV), with a membrane-incorporated synthetic monophosphoryl lipid A, 3D-PHAD® adjuvant. METHODS:Virosomes were initially formed by contacting a lipid film containing 3D-PHAD® with viral membranes s...

journal_title：Pharmaceutical research

authors： Lederhofer J,van Lent J,Bhoelan F,Karneva Z,de Haan A,Wilschut JC,Stegmann T

更新日期：2018-07-03 00:00:00

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:Adenoviruses are being developed for diseases of the gastrointestinal tract. Several in vitro assays were used to predict stability of PEGylated adenovirus along the GI tract and determine in vivo gene transfer after oral administration. METHODS:Recombinant adenovirus was modified with monomethoxypoly(ethylene...

journal_title：Pharmaceutical research

authors： Cheng X,Ming X,Croyle MA

更新日期：2003-09-01 00:00:00

abstract：PURPOSE:The purpose of the study was to examine the suitability of using laser diffraction to measure the fine particle fraction (FPF) of drugs emitted from carrier-free dry powder aerosol formulations. MATERIALS AND METHODS:Particle size distribution of terbutaline sulphate from Bricanyl Turbohaler, which contained l...

journal_title：Pharmaceutical research

authors： Martin GP,MacRitchie HB,Marriott C,Zeng XM

更新日期：2006-09-01 00:00:00

abstract：PURPOSE:Paclitaxel is active and widely used to treat multiple types of solid tumors. The commercially available paclitaxel formulation uses Cremophor/ethanol (C/E) as the solubilizers. Other formulations including nanoparticles have been introduced. This study evaluated the effects of nanoparticle formulation of pacli...

journal_title：Pharmaceutical research

authors： Yeh TK,Lu Z,Wientjes MG,Au JL

更新日期：2005-06-01 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：PURPOSE:[corrected] The purpose of this study was to design novel gastroretentive dosage forms (GRDFs) based on unfolding multilayer polymeric films, to investigate the mechanism of their gastroretentivity in dogs, and to assess the effect of compounding a narrow absorption window drug in a GRDF on the drug's absorptio...

journal_title：Pharmaceutical research

authors： Klausner EA,Lavy E,Stepensky D,Friedman M,Hoffman A

更新日期：2002-10-01 00:00:00

abstract：PURPOSE:Polyesters with hydrophilic domains, i.e., poly(D,L-lactic-co-glycolic-co-hydroxymethyl glycolic acid) (PLGHMGA) and a multiblock copolymer of poly(ε-caprolactone)-PEG-poly(ε-caprolactone) and poly(L-lactide) ((PC-PEG-PC)-(PL)) are expected to cause less acylation of encapsulated peptides than fully hydrophobic...

journal_title：Pharmaceutical research

authors： Shirangi M,Hennink WE,Somsen GW,van Nostrum CF

更新日期：2015-09-01 00:00:00