Bioactive-Chylomicrons for Oral Lymphatic Targeting of Berberine Chloride: Novel Flow-Blockage Assay in Tissue-Based and Caco-2 Cell Line Models.

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：PURPOSE:To analyze the mechanics of some pharmaceutical agglomerates during uniaxial confined compression by using compression parameters derived from the Heckel, Kawakita and Adams equations, and to study the influence of these compression parameters on the tablet-forming ability of agglomerates. METHODS:Force and di...

journal_title：Pharmaceutical research

authors： Nicklasson F,Alderborn G

更新日期：2000-08-01 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:Under different charging conditions, particles can be either attracted or repulsed by each other, causing powder agglomeration or segregation. Such behavior can be detrimental in many processes aimed at achieving particulate mixture homogeneity. Consequently, the effects of electrostatic charges on mixing kinet...

journal_title：Pharmaceutical research

authors： Desrosiers Lachiver E,Abatzoglou N,Cartilier L,Simard JS

更新日期：2006-05-01 00:00:00

abstract：PURPOSE:To gain information on the chemical stability pattern and the kinetics of the degradation of recombinant hirudin variant HV1 (rHir), a thrombin-specific inhibitor protein of 65 amino acids, in aqueous solution as a function of pH. METHODS:Stability of rHir was monitored at 50 degrees C in the framework of a cl...

journal_title：Pharmaceutical research

authors： Gietz U,Alder R,Langguth P,Arvinte T,Merkle HP

更新日期：1998-09-01 00:00:00

abstract：PURPOSE:Hydrogen/deuterium (H/D) exchange over a range of temperatures suggests a protein structural/mobility transition in the solid state below the system glass transition temperature (Tg). The purpose of this study was to determine whether solid-state protein stability correlates with the difference between storage ...

journal_title：Pharmaceutical research

authors： Fang R,Obeidat W,Pikal MJ,Bogner RH

更新日期：2020-08-13 00:00:00

abstract：PURPOSE:The lack of water-solubility hampers the use of many potent pharmaceuticals. Polymeric micelles are self-assembled nanocarriers with versatile properties that can be engineered to solubilize, target, and release hydrophobic drugs in a controlled-release fashion. Unfortunately, their large-scale use is limited b...

journal_title：Pharmaceutical research

authors： Fournier E,Dufresne MH,Smith DC,Ranger M,Leroux JC

更新日期：2004-06-01 00:00:00

abstract：PURPOSE:To show that atomic force microscopy (AFM) can be used to directly study the electrostatic charging and dissipation of single pharmaceutical particles. MATERIALS AND METHODS:Particles of lactose attached to AFM cantilevers were charged on a glass surface at a relative humidity (RH) of 0.1%. By recording force-...

journal_title：Pharmaceutical research

authors： Bunker MJ,Davies MC,James MB,Roberts CJ

更新日期：2007-06-01 00:00:00

abstract：:This review describes the design and current development of leukotriene biosynthesis inhibitors as potential antiinflammatory agents. Knowledge of the enzymatic mechanism of 5-lipoxygenase led to specific inhibitors of this enzyme which catalyzes a key step in the leukotriene pathway. Competitive inhibitors include ir...

journal_title：Pharmaceutical research

authors： Cashman JR

更新日期：1985-11-01 00:00:00

abstract：PURPOSE:The prognosis for glioma patients is poor, and development of new treatments is critical. Previously, we engineered polymer-based vaccines that control GM-CSF, CpG-oligonucleotide, and tumor-lysate presentation to regulate immune cell trafficking and activation, which promoted potent immune responses against pe...

journal_title：Pharmaceutical research

authors： Ali OA,Doherty E,Bell WJ,Fradet T,Hudak J,Laliberte MT,Mooney DJ,Emerich DF

更新日期：2011-05-01 00:00:00

abstract：PURPOSE:To test the hypothesis that modification of release pattern of nonsteroidal anti-inflammatory drugs (NSAIDs) formulations shifts gastrointestinal (GI) toxicity of the drugs from the upper GI region to the distal intestine. METHODS:We assessed tiaprofenic acid (TA)-induced upper and lower increased GI permeabil...

journal_title：Pharmaceutical research

authors： Vakily M,Khorasheh F,Jamali F

更新日期：1999-01-01 00:00:00

abstract：:Turbidimetric or light scattering assays can be used to determine the extent of aggregation in protein formulations. Using low molecular weight urokinase (LMW-UK) as a model protein, the effect of polymeric additives on heat-induced aggregation was evaluated. Previous work has shown that under 60 degrees C heat treatm...

journal_title：Pharmaceutical research

authors： Vrkljan M,Foster TM,Powers ME,Henkin J,Porter WR,Staack H,Carpenter JF,Manning MC

更新日期：1994-07-01 00:00:00

abstract：:A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...

journal_title：Pharmaceutical research

authors： Wolff M,Cordes G,Luckow V

更新日期：1985-01-01 00:00:00

abstract：:The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...

journal_title：Pharmaceutical research

authors： Hashimoto N,Fujioka T,Toyoda T,Muranushi N,Hirano K

更新日期：1994-10-01 00:00:00

abstract：:The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...

journal_title：Pharmaceutical research

authors： Leone M,Mönkäre J,Bouwstra JA,Kersten G

更新日期：2017-11-01 00:00:00

abstract：PURPOSE:Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation. METHODS:Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several...

journal_title：Pharmaceutical research

authors： Yang ZY,Le Y,Hu TT,Shen Z,Chen JF,Yun J

更新日期：2008-09-01 00:00:00

abstract：:Primaquine (I), a 6-methoxy-8-aminoqumoline derivative used for the treatment of malaria has previously been shown to be metabolized to 8-(3-carboxy-l-methyl-propylamino)-6-methoxyquinoline by both micro-organisms and laboratory rats. Reported herein is the synthesis of this novel metabolite. ...

journal_title：Pharmaceutical research

authors： McChesney JD,Sarangan S

更新日期：1984-03-01 00:00:00

abstract：PURPOSE:Prostaglandin E(1) (PGE(1)) is an effective treatment for peripheral vascular diseases. The encapsulation of PGE(1) in nanoparticles for its sustained-release would improve its therapeutic effect and quality of life (QOL) of patients. METHODS:In order to encapsulate PGE(1) in nanoparticles prepared with a poly...

journal_title：Pharmaceutical research

authors： Takeda M,Maeda T,Ishihara T,Sakamoto H,Yuki K,Takasaki N,Nishimura F,Yamashita T,Tanaka K,Takenaga M,Igarashi R,Higaki M,Yamakawa N,Okamoto Y,Ogawa H,Otsuka M,Mizushima Y,Mizushima T

更新日期：2009-07-01 00:00:00

abstract：PURPOSE:The purpose of this study was to evaluate glucose responsiveness in HepG2 human hepatoma cells transduced by a recombinant adeno-associated virus (rAAV) vector containing the insulin gene promoter. and to investigate the effect of protamine sulfate on rAAV-mediated gene delivery. METHODS:Recombinant AAV vector...

journal_title：Pharmaceutical research

authors： Yang YW,Hsieh YC

更新日期：2001-07-01 00:00:00

abstract：PURPOSE:To investigate the effect of polyelectrolytes on the formation and physicochemical properties of chitosan nanoparticles (CS-NPs) used for the delivery of an anticancer drug, doxorubicin (DOX). METHOD:Three DOX-loaded CS-NPs were formulated with tripolyphosphate (CS-TP/DOX NPs), dextran sulfate (CS-DS/DOX NPs),...

journal_title：Pharmaceutical research

authors： Ramasamy T,Tran TH,Cho HJ,Kim JH,Kim YI,Jeon JY,Choi HG,Yong CS,Kim JO

更新日期：2014-05-01 00:00:00

abstract：PURPOSE:The purpose of this study was to evaluate an effect of the proteolytic enzyme papain on permeation of low molecular weight heparin (LMWH) in vitro and in vivo. MATERIALS AND METHODS:In vitro permeation studies were performed using rat small intestine as permeation barrier. In order to determine the ratio of pa...

journal_title：Pharmaceutical research

authors： Grabovac V,Schmitz T,Föger F,Bernkop-Schnürch A

更新日期：2007-05-01 00:00:00

abstract：PURPOSE:To identify and quantify, in vitro and in vivo (in humans), the charge-carrying species during transdermal iontophoresis of lidocaine hydrochloride as a function of the concentration of drug relative to that of sodium chloride in the anodal solution. METHODS:In vitro experiments in standard diffusion cells qua...

journal_title：Pharmaceutical research

authors： Marro D,Kalia YN,Delgado-Charro MB,Guy RH

更新日期：2001-12-01 00:00:00

abstract：:A new high-performance liquid chromatographic (HPLC) assay suitable for pharmacokinetic studies of enantiomers of fenoprofen (FEN) was developed. Following the addition of internal standard (IS; racemic ketoprofen), the plasma or urine constituents are extracted into a mixture of isooctane:isopropanol (95:5), back ext...

journal_title：Pharmaceutical research

authors： Mehvar R,Jamali F

更新日期：1988-01-01 00:00:00

abstract：PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...

journal_title：Pharmaceutical research

authors： Lee WR,Shen SC,Sun CK,Aljuffali IA,Suen SY,Lin YK,Wang JJ,Fang JY

更新日期：2015-05-01 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：PURPOSE:The aim was to evaluate fluorescent molecular rotors (DCVJ and CCVJ), which are mainly sensitive to viscosity, for the characterization of polysorbate-containing IgG formulations and compare them to the polarity-sensitive dyes ANS, Bis-ANS and Nile Red. METHODS:IgG formulations with polysorbate 20 or 80 were s...

journal_title：Pharmaceutical research

authors： Hawe A,Filipe V,Jiskoot W

更新日期：2010-02-01 00:00:00

abstract：:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cy...

journal_title：Pharmaceutical research

authors： Irwin WJ,Dwivedi AK,Holbrook PA,Dey MJ

更新日期：1994-12-01 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：:An empirical mass-transfer model for enteric-coating dissolution that uses in vivo dissolution data to characterize the pH-dependent solubility properties of the polymer film and a mass-transfer coefficient determined from in vivo dissolution or disintegration studies is developed. Once the in vivo mass-transfer coeff...

journal_title：Pharmaceutical research

authors： Ebel JP,Jay M,Beihn RM

更新日期：1993-02-01 00:00:00

abstract：PURPOSE:The lack of an in vivo diagnostic test for AD has prompted the targeting of amyloid plaques with diagnostic imaging probes. We describe the development of a contrast agent (CA) for magnetic resonance microimaging that utilizes the F(ab')2 fragment of a monoclonal antibody raised against fibrillar human Abeta42 ...

journal_title：Pharmaceutical research

authors： Ramakrishnan M,Wengenack TM,Kandimalla KK,Curran GL,Gilles EJ,Ramirez-Alvarado M,Lin J,Garwood M,Jack CR Jr,Poduslo JF

更新日期：2008-08-01 00:00:00