Structural effects on the binding of amine drugs with the diphenylmethyl functionality to cyclodextrins. I. A microcalorimetric study.

abstract：:Enoximone and piroximone are cardiotonic agents for use in patients with congestive heart failure. Electroanalytical studies revealed that the dihydroimidazolone functionality was oxidizable and that this property can be analytically useful. The compounds undergo a two-electron, irreversible oxidation in neutral to ac...

journal_title：Pharmaceutical research

authors： Housmyer CL,Lewis RL Jr

更新日期：1991-07-01 00:00:00

abstract：:A colorless, parallelepiped crystal of methyl (2R,3S)-N-benzoyl-3-phenylisoserinate belonging to the space group P2(1) with a = 5.414(4), b = 7.813(1), c = 17.802(7) A, beta = 90.87(4) degrees, Z = 2, V = 752.9 A3, Dcalc = 1.32 g cm-3, and mu calc = 1.02 cm-1 was selected and the structure solved using direct methods....

journal_title：Pharmaceutical research

authors： Peterson JR,Do HD,Rogers RD

更新日期：1991-07-01 00:00:00

abstract：PURPOSE:The aim of this study was to investigate the specific changes in body distribution of camptothecin (CA) through incorporation into solid lipid nanoparticles (SLN) by peroral route. METHODS:Camptothecin loaded solid lipid nanoparticles (CA-SLN) coated with poloxamer 188 were produced by high pressure homogeniza...

journal_title：Pharmaceutical research

authors： Yang S,Zhu J,Lu Y,Liang B,Yang C

更新日期：1999-05-01 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:Generation of valuable information about the biphasic geometrical configuration of porcine stratum corneum from Very Small Angle Neutron Scattering (VSANS) data and investigation of its effect on the corresponding effective diffusivity. METHODS:Spectra of porcine stratum corneum are mathematically transformed ...

journal_title：Pharmaceutical research

authors： Charalambopoulou GC,Karamertzanis P,Kikkinides ES,Stubos AK,Kanellopoulos NK,Papaioannou AT

更新日期：2000-09-01 00:00:00

abstract：PURPOSE:A major challenge facing nanoparticle-based delivery of chemotherapy agents is the natural and unavoidable accumulation of these particles in healthy tissue resulting in local toxicity and dose-limiting side effects. To address this issue, we have designed and characterized a new prodrug nanoparticle with contr...

journal_title：Pharmaceutical research

authors： Schutt C,Ibsen S,Zahavy E,Aryal S,Kuo S,Esener S,Berns M,Esener S

更新日期：2017-10-01 00:00:00

abstract：:A procedure is described that is suitable for the radioimmunoassay (RIA) of 9-[(l,3-dihydroxy-2-propoxy)-methyl]guanine (DHPG) in plasma or serum at concentrations as low as 0.7 ng/ml (2.75 × 10(-9) M). Antiserum was prepared by coupling DHPG monohemisuccinate to bovine serum albumin and immunizing rabbits with the re...

journal_title：Pharmaceutical research

authors： Nerenberg C,McClung S,Martin J,Fass M,La Fargue J,Kushinsky S

更新日期：1986-04-01 00:00:00

abstract：PURPOSE:Gastrointestinal deposition of nanoparticles was examined after oral administration to mice suffering from an experimental gastric ulcer model. Local drug delivery could reduce side effects and would be a distinct improvement compared to existing therapeutic approaches, e.g. in the local therapy of Helicobacter...

journal_title：Pharmaceutical research

authors： Hassani S,Pellequer Y,Lamprecht A

更新日期：2009-05-01 00:00:00

abstract：PURPOSE:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RES...

journal_title：Pharmaceutical research

authors： Mackic JB,Stins M,Jovanovic S,Kim KS,Bartus RT,Zlokovic BV

更新日期：1999-09-01 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：:During the past two decades the nanomedicine field has experienced significant progress. To date, over sixty nanoparticle (NP) formulations have been approved in the US and EU while many others are in clinical or preclinical development, indicating a concerted effort to translate promising bench research to commercial...

journal_title：Pharmaceutical research

authors： Clogston JD,Hackley VA,Prina-Mello A,Puri S,Sonzini S,Soo PL

更新日期：2019-12-11 00:00:00

abstract：:Physiologically-based pharmacokinetic (PBPK) models explicitly incorporate tissue-specific blood flows, partition coefficients, and metabolic processes. Since PBPK models are derived using physiologic parameters and interactions of the compound with tissue components, these models are considered to be "bottom up" as o...

journal_title：Pharmaceutical research

authors： Korzekwa K,Nagar S

更新日期：2017-03-01 00:00:00

abstract：PURPOSE:Three types of acyl tetragastrin (TG), acetyl-TG (C2-TG), butyryl-TG (C4-TG) and caproyl-TG (C6-TG) were synthesized and their in vitro intestinal permeability characteristics were examined using Caco-2 monolayers. METHODS:The disappearance of acyl-TGs from the apical side of Caco-2 monolayers was estimated by...

journal_title：Pharmaceutical research

authors： Fujita T,Kawahara I,Quan Y,Hattori K,Takenaka K,Muranishi S,Yamamoto A

更新日期：1998-09-01 00:00:00

abstract：:The interaction of dicumarol and phenothiazine neuroleptics binding to alpha 1-acid glycoprotein (AGP) was investigated by circular dichroism (CD) and equilibrium dialysis. The induced CD spectra of the dicumarol-AGP complex were affected differently by the different substituents of the phenothiazine molecule. The sig...

journal_title：Pharmaceutical research

authors： Miyoshi T,Yamamichi R,Maruyama T,Otagiri M

更新日期：1992-07-01 00:00:00

abstract：PURPOSE:This study examined the rheological and textural characteristics (hardness, compressibilty, adhesiveness and cohesiveness) of bioadhesive oral gels containing the antimicrobial agent chlorhexidine. METHODS:Textural analysis was performed using a Stable Micro Systems texture analyser (model TA-XT 2) in texture ...

journal_title：Pharmaceutical research

authors： Jones DS,Woolfson AD,Brown AF

更新日期：1997-04-01 00:00:00

abstract：:Primaquine, an 8-aminoquinoline antimalarial, is shown to undergo unexpectedly rapid aromatic proton exchange with the medium. At a pH less than 4, the exchange of C-5 is so fast as to be unmeasurable by proton nmr methods. At a pH of 6-6.5 the half-time for exchange is 4 to 5 minutes. This unexpectedly high rate of e...

journal_title：Pharmaceutical research

authors： McChesney JD,Sarangan S

更新日期：1984-07-01 00:00:00

abstract：PURPOSE:Highly lipophilic basic drugs, the antiestrogens AE 1 (log P = 5.82) and AE 2 (log P = 7.8) shall be delivered transdermally. METHODS:Transdermal permeation of drugs, enhancers, and solvents from various fluid formulations were characterized by in-vitro permeation studies through excised skin of hairless mice....

journal_title：Pharmaceutical research

authors： Funke AP,Schiller R,Motzkus HW,Günther C,Müller RH,Lipp R

更新日期：2002-05-01 00:00:00

abstract：:In this study the intestinal degradation and absorption of a synthetic pentapeptide, metkephamid, were investigated in the rat by determination of its wall permeabilities in the small and large intestine and the extent and mechanism of its intestinal degradation. The peptide was metabolized in the gut wall through con...

journal_title：Pharmaceutical research

authors： Langguth P,Merkle HP,Amidon GL

更新日期：1994-04-01 00:00:00

abstract：:The present review discusses drugs and counter ions suitable for ion pair transport (IPT). Ion pairing is shown to effectively increase the lipophilicity and transport rate of polar drugs across lipid membranes. The proposed mechanisms of IPT are discussed in detail. A marked change in drug properties upon ion pair fo...

journal_title：Pharmaceutical research

authors： Neubert R

更新日期：1989-09-01 00:00:00

abstract：PURPOSE:To study the degradation of oxaliplatin in chloride media and evaluate the cytotoxicity of oxaliplatin in normal and chloride-deficient medium. METHODS:The products of the reaction of oxaliplatin with chloride were separated on a Hypercarb S column with a mobile phase containing 40% methanol in 0.05 M ammonia ...

journal_title：Pharmaceutical research

authors： Jerremalm E,Hedeland M,Wallin I,Bondesson U,Ehrsson H

更新日期：2004-05-01 00:00:00

abstract：PURPOSE:Interleukin-10 (IL-10) is an anti-inflammatory molecule that has achieved interest as a therapeutic for neuropathic pain. In this work, the potential of plasmid DNA-encoding IL-10 (pDNA-IL-10) slowly released from biodegradable microparticles to provide long-term pain relief in an animal model of neuropathic pa...

journal_title：Pharmaceutical research

authors： Soderquist RG,Sloane EM,Loram LC,Harrison JA,Dengler EC,Johnson SM,Amer LD,Young CS,Lewis MT,Poole S,Frank MG,Watkins LR,Milligan ED,Mahoney MJ

更新日期：2010-05-01 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：: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：PURPOSE:The objective of this study was to develop and characterize long-circulating, biodegradable, and biocompatible nanoparticulate formulation as an intracellular delivery vehicle. METHODS:Poly(ethylene glycol) (PEG)-modified gelatin was synthesized by reacting Type-B gelatin with PEG-epoxide. The nanoparticles, p...

journal_title：Pharmaceutical research

authors： Kaul G,Amiji M

更新日期：2002-07-01 00:00:00

abstract：PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...

journal_title：Pharmaceutical research

authors： Chen H,Zhang Z,Almarsson O,Marier JF,Berkovitz D,Gardner CR

更新日期：2005-03-01 00:00:00

abstract：PURPOSE:To improve the delivery of liposomes to tumors using P-selectin glycoprotein ligand 1 (PSGL1) mediated binding to selectin molecules, which are upregulated on tumorassociated endothelium. METHODS:PSGL1 was orientated and presented on the surface of liposomes to achieve optimal selectin binding using a novel st...

journal_title：Pharmaceutical research

authors： Carlisle R,Seymour LW,Coussios CC

更新日期：2013-02-01 00:00:00

abstract：PURPOSE:The aim of the study is to suppress the progress of estrogen-dependent breast cancer by inhibiting the membrane transporter, which mediates the internalization of estrone-3-sulfate as estrogen precursor in the cancer cells. METHODS:The uptake of estrone-3-sulfate by estrogen-dependent breast cancer MCF-7 cells...

journal_title：Pharmaceutical research

authors： Nozawa T,Suzuki M,Yabuuchi H,Irokawa M,Tsuji A,Tamai I

更新日期：2005-10-01 00:00:00

abstract：PURPOSE:This study aimed to characterize the transepithelial transport of miltefosine (HePC), the first orally effective drug against visceral leishmaniasis, across the intestinal barrier to further understand its oral absorption mechanism. MATERIALS AND METHODS:Caco-2 cell monolayers were used as an in vitro model of...

journal_title：Pharmaceutical research

authors： Ménez C,Buyse M,Dugave C,Farinotti R,Barratt G

更新日期：2007-03-01 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：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