Cellular handling of a dexamethasone-anti-E-selectin immunoconjugate by activated endothelial cells: comparison with free dexamethasone.

abstract：PURPOSE:To determine the factors influencing "solid solubility" and phase separation kinetics of drugs from amorphous solid dispersions. METHODS:Solid dispersions of griseofulvin-poly(vinyl pyrrolidone) (PVP) and indoprofen-PVP were prepared using solvent evaporation technique. Dispersions demonstrating single Tg were...

journal_title：Pharmaceutical research

authors： Vasanthavada M,Tong WQ,Joshi Y,Kislalioglu MS

更新日期：2005-03-01 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:The purpose of the present study was to investigate changes of blood-brain barrier (BBB) and brain parenchymal protein expression due to type II diabetes mellitus (T2DM) induced by a high-fat diet (HFD) by using SWATH-based quantitative proteomics. METHODS:Mice were fed a HFD for 2 or 10 weeks, and then SWATH-...

journal_title：Pharmaceutical research

authors： Ogata S,Ito S,Masuda T,Ohtsuki S

更新日期：2019-07-31 00:00:00

abstract：:The relative effectiveness of two beta-cyclodextrin derivatives, i.e., dimethyl-beta-cyclodextrin (DM beta CD) and hydroxypropyl-beta-cyclodextrin (HP beta CD), in enhancing enteral absorption of insulin was evaluated in the lower jejunal/upper ileal segments of the rat by means of an in situ closed loop method. The i...

journal_title：Pharmaceutical research

authors： Shao Z,Li Y,Chermak T,Mitra AK

更新日期：1994-08-01 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：:One thousand milligrams of aspirin, as its lysine salt was administered intravenously, orally, and intramuscularly to nine male and nine female young healthy adult volunteers. After intravenous injection mean (+/- SD) values of clearance, steady-state volume of distribution, and terminal half-life were 12.2 +/- 2.2 ml...

journal_title：Pharmaceutical research

authors： Aarons L,Hopkins K,Rowland M,Brossel S,Thiercelin JF

更新日期：1989-08-01 00:00:00

abstract：:Defined size fractions of polyethyleneglycol powder (MW = 10,000) were mixed with defined size fractions of alpha-lactose monohydrate in order to study the effect of compaction as a function of the weight ratios of the two excipients. For a precise control of the compression cycle, tablets were compressed on a Univers...

journal_title：Pharmaceutical research

authors： Blattner D,Kolb M,Leuenberger H

更新日期：1990-02-01 00:00:00

abstract：PURPOSE:To show, using a model study, how electronic structure theory can be applied in combination with LC/UV/MS/MS for the prediction and identification of oxidative degradants. METHODS:The benzyloxazole 1, was used to represent an active pharmaceutical ingredient for oxidative forced degradation studies. Bond disso...

journal_title：Pharmaceutical research

authors： Reid DL,Calvitt CJ,Zell MT,Miller KG,Kingsmill CA

更新日期：2004-09-01 00:00:00

abstract：PURPOSE:Stable transformants expressing human multidrug resistance 1 (MDR1), monkey MDR1, canine MDR1, rat MDR1a, rat MDR1b, mouse mdr1a, and mouse mdr1b in LLC-PK1 were established to investigate species differences in P-glycoprotein (P-gp, ABCB1) mediated efflux activity. METHODS:The seven cDNAs of MDR1 from five an...

journal_title：Pharmaceutical research

authors： Takeuchi T,Yoshitomi S,Higuchi T,Ikemoto K,Niwa S,Ebihara T,Katoh M,Yokoi T,Asahi S

更新日期：2006-07-01 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：PURPOSE:The lack of effective delivery vehicles impedes in vivo applications of siRNA. The trimethyl chitosan-cysteine (TC) nanoparticles (NPs) were developed for in vivo delivery of tumor necrosis factor α (TNF-α) siRNA via oral gavage and intraperitoneal injection. METHODS:The nanoparticles formulated from TC conjug...

journal_title：Pharmaceutical research

authors： He C,Yin L,Tang C,Yin C

更新日期：2013-10-01 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：:Since many chiral pharmaceutical excipients, such as cellulose polymers and cyclodextrins, are used as stationary phases for the separation of enantiomers by high performance liquid chromatography (HPLC), it is hypothesized that one enantiomer of a chiral drug will be released faster than the other from a pharmaceutic...

journal_title：Pharmaceutical research

authors： Duddu SP,Vakilynejad M,Jamali F,Grant DJ

更新日期：1993-11-01 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：PURPOSE:The purpose of the present study was to investigate the transport of organic monocarboxylic acids mediated by the anion exchanger AE2, which has been already reported to be present at several tissue cell membranes, including intestinal brush border membrane in rabbit. METHODS:Membrane transport of organic mono...

journal_title：Pharmaceutical research

authors： Yabuuchi H,Tamai I,Sai Y,Tsuji A

更新日期：1998-03-01 00:00:00

abstract：:Some geminal bisphosphonates are used clinically for a number of important bone/calcium related diseases; however, side effects and lack of selectivity impede their wide use. This work reports the synthesis and evaluation of bisacylphosphonates (e.g., adipoyl- and suberoylbisphosphonate). These compounds were found to...

journal_title：Pharmaceutical research

authors： Golomb G,Schlossman A,Saadeh H,Levi M,Van Gelder JM,Breuer E

更新日期：1992-01-01 00:00:00

abstract：PURPOSE:The objective of this work is to understand the sequence specificity of HAV peptides and to improve their selectivity in regulating E-cadherin-E-cadherin interactions in the intercellular junctions. METHODS:Peptide 1 was modified using an alanine scanning method to give peptides 2-6. The ability of these pepti...

journal_title：Pharmaceutical research

authors： Makagiansar IT,Avery M,Hu Y,Audus KL,Siahaan TJ

更新日期：2001-04-01 00:00:00

abstract：:Various diesters of 9-[(1,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) were screened in order to identify a derivative with improved oral absorption. The solubilities and dissolution rates decreased with increasing chain length and branching of the ester group. However, the dipropionate ester showed an anomalously fas...

journal_title：Pharmaceutical research

authors： Benjamin EJ,Firestone BA,Bergstrom R,Fass M,Massey I,Tsina I,Lin YY

更新日期：1987-04-01 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:To investigate the potential of a novel lipid carrier, comprising beads of alpha-cyclodextrin and soybean oil, for topical drug delivery. Adapalene was chosen as a model drug to explore the ability of the beads to encapsulate and release a highly lipophilic compound. MATERIALS AND METHODS:Adapalene-loaded bead...

journal_title：Pharmaceutical research

authors： Trichard L,Delgado-Charro MB,Guy RH,Fattal E,Bochot A

更新日期：2008-02-01 00:00:00

abstract：PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...

journal_title：Pharmaceutical research

authors： Liang R,Li X,Zhang R,Shi Y,Wang A,Chen D,Sun K,Liu W,Li Y

更新日期：2014-08-01 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: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：:Five aliphatic 5'-esters of 5-iodo-2'deoxyuridine (IDU) were synthesized via an acid chloride alcoholysis reaction. The solubility in pH 7.4 phosphate buffer, lipophilicity as determined by partition experiments in octanol/pH 7.4 buffer, and cytotoxicity of these potential prodrugs were evaluated. The esters showed a ...

journal_title：Pharmaceutical research

authors： Narurkar MM,Mitra AK

更新日期：1988-11-01 00:00:00

abstract：PURPOSE:Delivery of therapeutics to neurons is paramount to treat neurological conditions, including many lysosomal storage disorders. However, key aspects of drug-carrier behavior in neurons are relatively unknown: the occurrence of non-canonical endocytic pathways (present in other cells); whether carriers that trave...

journal_title：Pharmaceutical research

authors： Hsu J,Hoenicka J,Muro S

更新日期：2015-04-01 00:00:00

abstract：PURPOSE:In the present work, we developed water-in-oil (w/o) nanoemulsions for the intravesical administration of cisplatin. METHODS:The nanoemulsions were made up of soybean oil as the oil phase and Span 80, Tween 80, or Brij 98 as the emulsifier system. alpha-Terpineol and oleic acid were incorporated as permeation ...

journal_title：Pharmaceutical research

authors： Hwang TL,Fang CL,Chen CH,Fang JY

更新日期：2009-10-01 00:00:00

abstract：PURPOSE:The trial-and-error approach is still predominantly used in pharmaceutical development of nanosuspensions. Physicochemical dispersion stability is a primary focus and therefore, various analytical bulk methods are commonly employed. Clearly less attention is directed to surface changes of nanoparticles even tho...

journal_title：Pharmaceutical research

authors： Aleandri S,Schönenberger M,Niederquell A,Kuentz M

更新日期：2018-02-21 00:00:00

abstract：:The technique of Affinity capillary electrophoresis (ACE) is a useful tool to characterize complexation and partition equilibria. A wide range of applications in pharmaceutics has been presented: the determination of pKA values, of association constants between drugs and cyclodextrins or amphiphilic compounds as well ...

journal_title：Pharmaceutical research

authors： Neubert RH,Schwarz MA,Mrestani Y,Plätzer M,Raith K

更新日期：1999-11-01 00:00:00

abstract：:The in situ rat gut technique was used to study the effects of hypothermia on the intestinal absorption of a 1 mg/ml solution of sodium pentobarbital in 0.01 M phosphate buffer (pH 6.0). Male Sprague-Dawley rats weighing between 300 and 370 g were exposed to an atmosphere of helox (helium:oxygen, 80:20) at 0-4 degrees...

journal_title：Pharmaceutical research

authors： Stavchansky S,Tung IL

更新日期：1987-06-01 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