Synthesis and in vitro evaluation of a novel chitosan-glutathione conjugate.

abstract：:Assessment of bioavailability/bioequivalence generally relies on the comparison of rate and extent of drug absorption between products. Rate of absorption is commonly expressed by peak concentration (C(max)) and time to peak concentration (T(max)), although these parameters are indirect measures of absorption rate. Re...

journal_title：Pharmaceutical research

authors： Chen ML,Davit B,Lionberger R,Wahba Z,Ahn HY,Yu LX

更新日期：2011-08-01 00:00:00

abstract：:The topical antifungal Sch-39304 is a racemic compound comprised of two enantiomers, Sch-42427 and Sch-42426, only one of which (Sch-42427) is pharmacologically active. The pure enantiomers have a lower melting point and, therefore, a higher solubility than the racemic compound. Because of these differences in physico...

journal_title：Pharmaceutical research

authors： Wearley L,Antonacci B,Cacciapuoti A,Assenza S,Chaudry I,Eckhart C,Levine N,Loebenberg D,Norris C,Parmegiani R

更新日期：1993-01-01 00:00:00

abstract：PURPOSE:To examine the iontophoretic delivery of ALA as a function of pH and to determine the principal mechanisms responsible for its electrotransport. METHODS:Anodal iontophoretic transport of ALA was measured as a function of its concentration and pH of the donor solution. Experiments were performed in vitro using ...

journal_title：Pharmaceutical research

authors： Lopez RF,Bentley MV,Delgado-Charro MB,Guy RH

更新日期：2001-03-01 00:00:00

abstract：PURPOSE:The sensitivity and effectiveness of indirect metrics proposed for the assessment of comparative absorption rates in bioequivalence studies [Cmax, Tmax, partial AUC (AUCp), feathered slope (SLf), intercept metric (I)] were originally tested by assuming first-order absorption. The present study re-evaluates thei...

journal_title：Pharmaceutical research

authors： Ring A,Tothfalusi L,Endrenyi L,Weiss M

更新日期：2000-05-01 00:00:00

abstract：:Knowledge of comparative solubility profiles of a base and its hydrochloride salt is important in selecting one form over the other for dosage form design. The studies with two model bases, namely, tiaramide and papaverine, showed that, except during phase transition from a base to a salt or vice versa, the pH-solubil...

journal_title：Pharmaceutical research

authors： Serajuddin AT,Mufson D

更新日期：1985-03-01 00:00:00

abstract：:Gallopamil is a calcium-channel antagonist with reported activity in experimental animals three to five times higher than that of verapamil. An automated high-performance liquid chromatographic (HPLC) method with fluorescence detection is described for the simultaneous determination of gallopamil and its metabolite no...

journal_title：Pharmaceutical research

authors： McLean AM,Babcock-Atkinson E,Rein K,Ruggirello DA,Gonzalez MA,Noonan PK

更新日期：1987-08-01 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：:The mechanical properties of dry and wet polymeric films prepared from various aqueous polymeric dispersions were evaluated by a puncture test. They were studied with respect to type of polymer dispersion [cellulosic: Aquacoat and Surelease; acrylic: Eudragit NE, L, RS, and RL 30 D], plasticizer type (water-soluble or...

journal_title：Pharmaceutical research

authors： Bodmeier R,Paeratakul O

更新日期：1994-06-01 00:00:00

abstract：PURPOSE:Monocarboxylate transporter (MCT) inhibition represents a potential treatment strategy for γ-hydroxybutyric acid (GHB) overdose by blocking its renal reabsorption in the kidney. This study further evaluated the effects of a novel, highly potent MCT inhibitor, AR-C155858, on GHB toxicokinetics/toxicodynamics (TK...

journal_title：Pharmaceutical research

authors： Vijay N,Morse BL,Morris ME

更新日期：2015-06-01 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：:The bioavailability of a new sustained-release potassium chloride (KCl) tablet, designed for once-a-day dosing, was compared to a KCl elixir using urinary excretion data. The study utilized 25 male volunteers dosed in a crossover design in a dietary/activity-controlled environment. The regimens consisted of a total of...

journal_title：Pharmaceutical research

authors： Betlach CJ,Arnold JD,Frost RW,Leese PT,Gonzalez MA

更新日期：1987-10-01 00:00:00

abstract：PURPOSE:To investigate the mechanisms involved in transport of sulfasalazine in Caco-2 cells. METHODS:Permeability coefficients of sulfasalazine and its analogs across Caco-2 cell monolayers were measured as a function of direction of transport, energy and concentration dependence, and in the presence of inhibitors of...

journal_title：Pharmaceutical research

authors： Liang E,Proudfoot J,Yazdanian M

更新日期：2000-10-01 00:00:00

abstract：PURPOSE:Good glycaemic control is essential to minimize the risk for diabetes-induced complications. Also, compliance is likely to be higher if the procedure is simple and painless. This study was designed to validate painless intradermal delivery via a patch-like microneedle array. MATERIALS AND METHODS:Diabetes was ...

journal_title：Pharmaceutical research

authors： Nordquist L,Roxhed N,Griss P,Stemme G

更新日期：2007-07-01 00:00:00

abstract：:Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...

journal_title：Pharmaceutical research

authors： Abdallah HY,Mayersohn M

更新日期：1991-04-01 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

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：PURPOSE:Using human lung cancer cells, we evaluated the involvement of plasminogen activator inhibitor-1 (PAI-1) in the anti-invasive action of cannabidiol, a non-psychoactive cannabinoid. METHODS:Invasion was quantified by a modified Boyden chamber assay. PAI-1 protein in cell culture media and PAI-1 mRNA were determ...

journal_title：Pharmaceutical research

authors： Ramer R,Rohde A,Merkord J,Rohde H,Hinz B

更新日期：2010-10-01 00:00:00

abstract：PURPOSE:To identify the molecules responsible for amyloid beta-peptide (1-40) (Abeta(1-40)) uptake by the liver, which play a major role in the systemic clearance of Abeta(1-40). METHODS:The liver uptake index method was used to examine the mechanisms of Abeta(1-40) uptake by the liver in vivo. RESULTS:[125I]Abeta(1-...

journal_title：Pharmaceutical research

authors： Tamaki C,Ohtsuki S,Iwatsubo T,Hashimoto T,Yamada K,Yabuki C,Terasaki T

更新日期：2006-07-01 00:00:00

abstract：PURPOSE:This study aimed to assess impact of different vehicles for laser-assisted skin drug delivery. We also tried to uncover the mechanisms by which different vehicles affect laser-aided skin permeation. METHODS:Full-surface ablative (conventional) and fractional lasers were used to irradiate nude mouse skin. Imiqu...

journal_title：Pharmaceutical research

authors： Lee WR,Shen SC,Aljuffali IA,Li YC,Fang JY

更新日期：2014-02-01 00:00:00

abstract：PURPOSE:Tumor vascular normalization by antiangiogenic agents may increase tumor perfusion but reestablish vascular barrier properties in CNS tumors. Vascular priming via nanoparticulate carriers represents a mechanistically distinct alternative. This study investigated mechanisms by which sterically-stabilized liposom...

journal_title：Pharmaceutical research

authors： Roy Chaudhuri T,Arnold RD,Yang J,Turowski SG,Qu Y,Spernyak JA,Mazurchuk R,Mager DE,Straubinger RM

更新日期：2012-12-01 00:00:00

abstract：PURPOSE:Hydroxylation of the antidepressant and smoking deterrent drug bupropion is a clinically important bioactivation and elimination pathway. Bupropion hydroxylation is catalyzed selectively by cytochrome P4502B6 (CYP2B6). CYP2B6-catalyzed bupropion hydroxylation has been used as an in vitro and in vivo phenotypic ...

journal_title：Pharmaceutical research

authors： Coles R,Kharasch ED

更新日期：2008-06-01 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:The purpose of this study was to investigate the effects of formulation factors including varying wax concentration, drug loading and drug particle size, on drug release characteristics from both pure oil and gel formulations prepared with a combination of derivatized vegetable oil (Labrafil 1944 CS) and glycer...

journal_title：Pharmaceutical research

authors： Gao ZH,Shukla AJ,Johnson JR,Crowley WR

更新日期：1995-06-01 00:00:00

abstract：PURPOSE:The in vitro inhibitory effect of Docetaxel (DTX) and Everolimus (EVR) alone and together in poly(ethylene glycol)-block-poly(D,L-lactic acid) (PEG-b-PLA) nanocarriers on angiogenic processes and acute toxicity in mice was evaluated. METHODS:PEG-b-PLA DTX and/or EVR nanocarriers were characterized for size, dr...

journal_title：Pharmaceutical research

authors： Mishra GP,Doddapaneni BS,Nguyen D,Alani AW

更新日期：2014-03-01 00:00:00

abstract：:The mechanism of release from sustained-release adinazolam mesylate tablets was assessed by the Higuchi equation and by analysis of drug release profiles through 60% released using the Peppas equation. Computed values of the diffusional exponent, n, ranged from 0.59 to 0.66. Values of n in this range are consistent wi...

journal_title：Pharmaceutical research

authors： Skoug JW,Borin MT,Fleishaker JC,Cooper AM

更新日期：1991-12-01 00:00:00

abstract：PURPOSE:Preparation of Nanographene oxide (NGO) - Gelatin hybrids for efficient treatment of Neuroblastoma. METHODS:Nanohybrids were prepared via non-covalent interactions. Spectroscopic tools have been used to discriminate the chemical states of NGO prior and after gelatin coating, with UV visible spectroscopy reveal...

journal_title：Pharmaceutical research

authors： Makharza S,Vittorio O,Cirillo G,Oswald S,Hinde E,Kavallaris M,Büchner B,Mertig M,Hampel S

更新日期：2015-06-01 00:00:00

abstract：:Microbial metabolism studies of the semisynthetic antimalarial anhydrodihydroartemisinin (1), have shown that it is metabolized by a number of microorganisms. Large scale fermentation with Streptomyces lavendulae L-105 and Rhizopogon species (ATCC 36060) have resulted in the isolation of four microbial metabolites. Th...

journal_title：Pharmaceutical research

authors： Khalifa SI,Baker JK,Rogers RD,el-Feraly FS,Hufford CD

更新日期：1994-07-01 00:00:00

abstract：:Moisture sorption characteristics and the effect of moisture content on the compression properties of two dextrose-based directly compressible diluents, namely, Emdex (diluent A) and Sweetrex (diluent B) were studied. Both diluents sorbed moisture rapidly at relative humidities greater than 60%. For both the diluents,...

journal_title：Pharmaceutical research

authors： Shukla AJ,Price JC

更新日期：1991-03-01 00:00:00

abstract：:Four lipophilic, low molecular weight drugs solubilized in phosphatidylcholine-bile salt mixed micelles were injected s.c. into the hind legs of sheep and their cumulative recoveries in lymph draining from the site of application were determined. Surprisingly, the cumulative recoveries (percentage of dose) varied betw...

journal_title：Pharmaceutical research

authors： Supersaxo A,Hein WR,Steffen H

更新日期：1991-10-01 00:00:00

abstract：:Liver fibrosis is a pathological condition originating from liver damage that leads to excess accumulation of extracellular matrix (ECM) proteins in the liver. Viral infection, chronic injury, local inflammatory responses and oxidative stress are the major factors contributing to the onset and progression of liver fib...

journal_title：Pharmaceutical research

authors： Kumar V,Mahato RI

更新日期：2015-02-01 00:00:00