Intranasal delivery--modification of drug metabolism and brain disposition.

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 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：PURPOSE:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...

journal_title：Pharmaceutical research

authors： Steen-Louws C,Boross P,Prado J,Meeldijk J,Langenhorst JB,Huitema ADR,den Hartog MT,Boon L,Lafeber FPJG,Hack CE,Eijkelkamp N,Popov-Celeketic J

更新日期：2019-12-26 00:00:00

abstract：PURPOSE:To synthesize a trifluorinated bile acid that can be used for (19)F magnetic resonance imaging (MRI) of bile acid enterohepatic circulation, characterize its in vitro transporter affinity, stability, and (19)F-MRI signal, and assess its ability to concentrate in the gallbladder of C57BL/6 mice. METHODS:Target ...

journal_title：Pharmaceutical research

authors： Vivian D,Cheng K,Khurana S,Xu S,Whiterock V,Witter D,Lentz KA,Santone KS,Raufman JP,Polli JE

更新日期：2013-05-01 00:00:00

abstract：PURPOSE:This study aims to conduct an impact investigation in the hydrophobic-hydrophilic balance as an important factor for dissolution improvement of a hydrophilic carrier-based solid dispersion system. METHODS:Polymeric carriers with different hydrophobic to hydrophilic ratios were used to prepare several electrosp...

journal_title：Pharmaceutical research

authors： Teoh XY,Yeoh Y,Yoong LK,Chan SY

更新日期：2020-01-07 00:00:00

abstract：:A liposomal formulation of methylprednisolone (L-MPL) was developed to improve localization of this immunosuppressant in lymphatic tissues. Liposomes containing MPL were formulated from a mixture of phosphatydylcholine and phosphatydylglycerol (molar ratio, 9:1) and sized by extrusion through a 0.1-micron membrane. Ma...

journal_title：Pharmaceutical research

authors： Mishina EV,Straubinger RM,Pyszczynski NA,Jusko WJ

更新日期：1993-10-01 00:00:00

abstract：PURPOSE:The effect of the molecular weight of dextran on the molecular mobility and protein stability of freeze-dried serum gamma-globulin (BGG) formulations was studied. The stabilizing effect of higher molecular weight dextran is discussed in relation to the molecular mobility of the formulations. METHODS:The molecu...

journal_title：Pharmaceutical research

authors： Yoshioka S,Aso Y,Kojima S

更新日期：1997-06-01 00:00:00

abstract：PURPOSE:To characterize the electrochemical behavior of the photodegradation product of nifedipine, i.e., 2,6-dimethyl-4-(2-nitrosophenyl)-3,5-pyridine-carboxylic acid dimethyl ester (NPD) in different electrolytic media. We also evaluated the interaction between free radicals generated from NPD and xeno/endobiotics. ...

journal_title：Pharmaceutical research

authors： Núñez-Vergara LJ,Bollo S,Fuentealba J,Sturm JC,Squella JA

更新日期：2002-04-01 00:00:00

abstract：PURPOSE:Solid dispersions (SDs) represent the most common formulation technique used to increase the dissolution rate of a drug. In this work, the three most common methods used to prepare SDs, namely spray-drying, solvent-casting and freeze-drying, have been compared in order to investigate their effect on increasing ...

journal_title：Pharmaceutical research

authors： De Mohac LM,Caruana R,Cavallaro G,Giammona G,Licciardi M

更新日期：2020-02-19 00:00:00

abstract：PURPOSE:The passage of molecules across cell membranes is a crucial step in many physiological processes. We therefore seek physical models of this process, in order to predict permeation for new molecules, and to better understand the important interactions which determine the rate of permeation. METHODS:Several sets...

journal_title：Pharmaceutical research

authors： Platts JA,Abraham MH,Hersey A,Butina D

更新日期：2000-08-01 00:00:00

abstract：PURPOSE:The aim was to replace the traditional 21-day Caco-2 permeability protocol by a more high-throughput assay. METHODS:Caco-2 cells were seeded at high density in 96-well plates in novel cell culture boxes. After 7 days, drug permeability studies were performed. Samples were analyzed by a new UV detection method....

journal_title：Pharmaceutical research

authors： Alsenz J,Haenel E

更新日期：2003-12-01 00:00:00

abstract：PURPOSE:To evaluate the potential effects of PEGylated pH-sensitive liposomes on the intracellular activity of a new peptide recently characterized as a novel inhibitor of the human thymidylate synthase (hTS) over-expressed in many drug-resistant human cancer cell lines. METHODS:Peptide-loaded pH-sensitive PEGylated (...

journal_title：Pharmaceutical research

authors： Sacchetti F,Marverti G,D'Arca D,Severi L,Maretti E,Iannuccelli V,Pacifico S,Ponterini G,Costi MP,Leo E

更新日期：2018-09-12 00:00:00

abstract：:The dose dependency of carbamazepine pharmacokinetics was characterized in rats, a common test animal for antiepileptic drug efficacy. With a randomized Latin square schedule, 5, 10, and 20 mg/kg doses of carbamazepine were injected intravenously into six Sprague-Dawley rats followed by the administration of a 5 or 10...

journal_title：Pharmaceutical research

authors： Remmel RP,Sinz MW,Cloyd JC

更新日期：1990-05-01 00:00:00

abstract：PURPOSE:The aim of this work was to investigate the influence of the oily nucleus composition on physico-chemical properties and anesthetic activity of poly (lactide-co-glycolide) nanocapsules with benzocaine. METHODS:Nanocapsules containing benzocaine were prepared with three different oily nucleus composition and ch...

journal_title：Pharmaceutical research

authors： de Melo NF,Grillo R,Guilherme VA,de Araujo DR,de Paula E,Rosa AH,Fraceto LF

更新日期：2011-08-01 00:00:00

abstract：PURPOSE:We present a smart intradermal interface suitable for skin-attached drug delivery devices. Our solution enables injections or infusions that are less invasive compared to subcutaneous injections and are leakage-free at the location of penetration. METHODS:The intradermal interface is based on a 31-gauge cannul...

journal_title：Pharmaceutical research

authors： Vosseler M,Jugl M,Zengerle R

更新日期：2011-03-01 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 purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...

journal_title：Pharmaceutical research

authors： Massarella JW,Nazareno LA,Passe S,Min B

更新日期：1996-03-01 00:00:00

abstract：PURPOSE:To design and synthesize fatty acid-RGD peptide amphiphiles with ADA linker for their potential delivery of hydrophobic drugs like paclitaxel targeted to α(v)β(3) integrin overexpressing tumors. METHODS:Four amphiphiles - C16 or C18 fatty acid-RGD peptide and ADA linker were designed and synthesized. CMC, size...

journal_title：Pharmaceutical research

authors： Javali NM,Raj A,Saraf P,Li X,Jasti B

更新日期：2012-12-01 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：:A new magnetic microsphere carrier has been formulated that may localize drugs by both biochemical and physical means. The microspheres, prepared from the polysaccharide chitosan, are designed to bind to anionic glycosaminoglycan receptors on the surface of capillary endothelial cells. The microspheres were formulated...

journal_title：Pharmaceutical research

authors： Gallo JM,Hassan EE

更新日期：1988-05-01 00:00:00

abstract：PURPOSE:The purpose of this study was to obtain an in vitro/in vivo correlation for the sustained release of a protein from poly(ethylene glycol) terephthalate (PEGT)/poly(butylene terephthalate) (PBT) microspheres. METHODS:Radiolabeled lysozyme was encapsulated in PEGT/PBT microspheres via a water-in-oil-in-water emu...

journal_title：Pharmaceutical research

authors： van Dijkhuizen-Radersma R,Wright SJ,Taylor LM,John BA,de Groot K,Bezemer JM

更新日期：2004-03-01 00:00:00

abstract：PURPOSE:We investigated the characteristics of transport of an organic anion, p-aminohippurate (PAH), at the apical membrane in a kidney epithelial cell line OK. METHODS:Efflux and uptake of [14C]PAH across the apical membrane were measured using OK cell monolayers grown on microporous membrane filters. RESULTS:PAH e...

journal_title：Pharmaceutical research

authors： Habu Y,Yano I,Hashimoto Y,Saito H,Inui K

更新日期：2002-12-01 00:00:00

abstract：PURPOSE:The objective of this study was to compare two different nebulizers: Eflow rapid® and Pari LC star® by scintigraphy and PK modeling to simulate epithelial lining fluid concentrations from measured plasma concentrations, after nebulization of CMS in baboons. METHODS:Three baboons received CMS by IV infusion and...

journal_title：Pharmaceutical research

authors： Marchand S,Bouchene S,de Monte M,Guilleminault L,Montharu J,Cabrera M,Grégoire N,Gobin P,Diot P,Couet W,Vecellio L

更新日期：2015-10-01 00:00:00

abstract：PURPOSE:To develop a liposomal system with high drug loading (DL) for intravenous (i.v.) delivery of a poorly water-soluble basic drug, asulacrine (ASL). METHODS:A thin-film hydration and extrusion method was used to fabricate the PEGylated liposomal membranes followed by a freeze and thaw process. A novel active drug...

journal_title：Pharmaceutical research

authors： Zhang W,Wang G,Falconer JR,Baguley BC,Shaw JP,Liu J,Xu H,See E,Sun J,Aa J,Wu Z

更新日期：2015-04-01 00:00:00

abstract：PURPOSE:Cynarin, a potential immunosuppressant that blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells, was found in Echinacea purpurea by a new pharmaceutical screening method: After Flowing Through Immobilized Receptor (AFTIR; Dong et al., J Med Chem, 49: 1845-1854, 2006)....

journal_title：Pharmaceutical research

authors： Dong GC,Chuang PH,Chang KC,Jan PS,Hwang PI,Wu HB,Yi M,Zhou HX,Chen HM

更新日期：2009-02-01 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：PURPOSE:A theory and computer programs running on Microsoft Excel for Windows for calculation of solution pH, buffer formula, and buffer capacity at a given ionic strength and temperature were developed. The theory does not limit the category of buffer components, the number of buffer components, or the number of ioniz...

journal_title：Pharmaceutical research

authors： Okamoto H,Mori K,Ohtsuka K,Ohuchi H,Ishii H

更新日期：1997-03-01 00:00:00

abstract：:Nonstereospecific studies have indicated that the pharmacokinetics of propranolol (PR) are altered in inflammatory conditions such as arthritis. However, as the kinetics and dynamics of PR are stereoselective, we examined the effect of adjuvant arthritis (AA) on the disposition of the individual enantiomers. A novel n...

journal_title：Pharmaceutical research

authors： Piquette-Miller M,Jamali F

更新日期：1993-02-01 00:00:00

abstract：:Physicochemical effects caused by intestinal fluids on drugs in the gastrointestinal (GI) tract can be a contributing factor in food induced changes in bioavailability. To identify physicochemical properties of gemfibrozil that may be altered by endogenous and dietary lipids, in vitro studies were conducted in model s...

journal_title：Pharmaceutical research

authors： Luner PE,Babu SR,Radebaugh GW

更新日期：1994-12-01 00:00:00

abstract：PURPOSE:To assess the uridine diphosphate (UDP)-glucuronosyltransferase (UGT) isozymes involved in the glucuronidation of niflumic acid in human liver. METHODS:The glucuronidation activity of niflumic acid was determined in liver microsomes and recombinant UGT isozymes by incubation of niflumic acid with UDP-glucuroni...

journal_title：Pharmaceutical research

authors： Mano Y,Usui T,Kamimura H

更新日期：2006-07-01 00:00:00