Transport screening of drug cocktails through an in vitro blood-brain barrier: is it a good strategy for increasing the throughput of the discovery pipeline?

abstract：:Unsymmetrical aryl(heteroaryl)methyl isopropyl ester analogues of nifedipine, in which the 2-nitrophenyl group at C-4 is replaced by a 2- or 3-pyridyl substituent, were synthesized and evaluated as calcium-channel antagonists using guinea pig ileal longitudinal smooth muscle. The point of attachment of the C-4 pyridyl...

journal_title：Pharmaceutical research

authors： Akula MR,Matowe WC,Wolowyk MW,Knaus EE

更新日期：1990-09-01 00:00:00

abstract：PURPOSE:The purpose of this study was to assess the antifungal activity and renal and hepatic toxicity of amphotericin B (AmpB) following administration of Fungizone (FZ) and a heat-treated form of FZ (HFZ) to rats infected with Aspergillus fumigatus. METHODS:Infected rats were administered FZ and HFZ at a dosing regi...

journal_title：Pharmaceutical research

authors： Sivak O,Bartlett K,Wasan KM

更新日期：2004-09-01 00:00:00

abstract：PURPOSE:For determination of the transit time through various parts of the gastrointestinal (GI) tract, we developed a method that provides the location of disintegration and drug release. This method involves GI magnetomarkergraphy (GIMG) using a 129-channel Shimadzu vector biomagnetic measurement system (BMS). METHO...

journal_title：Pharmaceutical research

authors： Hu Z,Mawatari S,Shibata N,Takada K,Yoshikawa H,Arakawa A,Yosida Y

更新日期：2000-02-01 00:00:00

abstract：:Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling fac...

journal_title：Pharmaceutical research

authors： Niven RW,Byron PR

更新日期：1988-09-01 00:00:00

abstract：PURPOSE:The encapsulation of pancreatic β-cells in biocompatible matrix has generated great interest in diabetes treatment. Our work has shown improved microcapsules when incorporating the bile acid ursodeoxycholic acid (UDCA), in terms of morphology and cell viability although cell survival remained low. Thus, the stu...

journal_title：Pharmaceutical research

authors： Mooranian A,Negrulj R,Al-Salami H

更新日期：2016-05-01 00:00:00

abstract：PURPOSE:Topoisomerase II (Topo II) preferentially cuts DNA at alternating purine-pyrimidine repeats. Different Topo II poisons may affect Topo II to produce distinct drug-specific DNA cleavage patterns. GL331 is a new podophyllotoxin derivative exhibiting potent Topo II-poisoning activity. Therefore, the sequence selec...

journal_title：Pharmaceutical research

authors： Lee CC,Huang TS

更新日期：2001-06-01 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：:The stability of an antibiotic formulation (clindamycin phosphate in dextrose), which is stable at room temperature, was assessed by nonisothermal kinetic analysis at elevated temperatures. A preliminary study, conducted to establish apparent rate order, verified the appropriateness of a first-order kinetic model. The...

journal_title：Pharmaceutical research

authors： Kipp JE,Hlavaty JJ

更新日期：1991-05-01 00:00:00

abstract：PURPOSE:This work describes the synthesis of block co-polymeric micelles, methoxy-poly(ethylene glycol)-poly(D,L-lactide) (mPEG-PLA) to encapsulate Curcumin (CUR), thereby improving the dispersibility and chemical stability of curcumin, prolonging its cellular uptake and enhancing its bioavailability. METHODS:CUR-mPEG...

journal_title：Pharmaceutical research

authors： Kumari P,Swami MO,Nadipalli SK,Myneni S,Ghosh B,Biswas S

更新日期：2016-04-01 00:00:00

abstract：PURPOSE:To develop resource-sparing in silico approaches that aim to reduce experimental effort and material required by developability assessments (DA) of monoclonal antibody (mAb) drug candidates. METHODS:A battery of standardized biophysical experiments was performed on high concentration formulations of 16 drug pr...

journal_title：Pharmaceutical research

authors： Tomar DS,Singh SK,Li L,Broulidakis MP,Kumar S

更新日期：2018-08-20 00:00:00

abstract：:Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...

journal_title：Pharmaceutical research

authors： Rapaka RS,Porreca F

更新日期：1991-01-01 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 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:The relationship between rat intestinal permeability (Papp) of a range of hydrophilic probe molecules and probe geometry was examined. METHODS:Molecules studies included mannitol, the polyethylene glycols (PEGs) 400, 900, and 4000, the dextran conjugated dye Texas Red (MW 3000) and the polysaccharide inulin (M...

journal_title：Pharmaceutical research

authors： Lane ME,O'Driscoll CM,Corrigan OI

更新日期：1996-10-01 00:00:00

abstract：PURPOSE:It was the purpose of this study to develop a new oral drug delivery system for low molecular weight heparin (LMWH) providing an improved bioavailability and a prolonged therapeutic effect. METHODS:The permeation enhancing polycarbophil-cysteine conjugate (PCP-Cys) used in this study displayed 111.4 +/- 6.4 mi...

journal_title：Pharmaceutical research

authors： Kast CE,Guggi D,Langoth N,Bernkop-Schnürch A

更新日期：2003-06-01 00:00:00

abstract：PURPOSE:We have already demonstrated that the HMG-CoA reductase inhibitor, pravastatin is actively taken up by isolated rat hepatocytes via a multispecific anion transporter (Yamazaki et al., Am. J. Physiol. 264, G36-44, (1993)). We further attempted the quantitative evaluation of this uptake in different experimental ...

journal_title：Pharmaceutical research

authors： Ishigami M,Tokui T,Komai T,Tsukahara K,Yamazaki M,Sugiyama Y

更新日期：1995-11-01 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：PURPOSE:The intratumoral heterogeneity observed in breast cancer (BC), in particular with regard to cell surface receptor expression, can hinder the success of many targeted cancer therapies. The development of novel therapeutic agents that target more than one receptor can overcome this inherent property of tumors and...

journal_title：Pharmaceutical research

authors： Houdaihed L,Evans JC,Allen C

更新日期：2020-01-21 00:00:00

abstract：:Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...

journal_title：Pharmaceutical research

authors： Thanoo BC,Doll WJ,Mehta RC,Digenis GA,DeLuca PP

更新日期：1995-12-01 00:00:00

abstract：PURPOSE:Chitosan-based polymeric micelles (CBPMs) are considered as promising carriers for delivery of anticancer drugs, imaging agents and genes. To optimize the physicochemical, pharmaceutical and biological properties of CBPMs, the molecular mechanisms behind the self-assembly behavior of chitosan (CHI) amphiphilic ...

journal_title：Pharmaceutical research

authors： Mahmoudzadeh M,Fassihi A,Dorkoosh F,Heshmatnejad R,Mahnam K,Sabzyan H,Sadeghi A

更新日期：2015-12-01 00:00:00

abstract：PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...

journal_title：Pharmaceutical research

authors： Vogt FG,Williams GR

更新日期：2012-07-01 00:00:00

abstract：:Penetration of various compounds through shed snake skin was measured in vitro to examine the effect of lipophilicity and molecular size of a compound on permeability through this model membrane. The permeabilities were found to be controlled by the lipophilicity and the molecular size of the permeant. The smaller and...

journal_title：Pharmaceutical research

authors： Itoh T,Magavi R,Casady RL,Nishihata T,Rytting JH

更新日期：1990-12-01 00:00:00

abstract：:The release of lithium carbonate incorporated into polymethylmethacrylate, polyvinyl chloride, hydrogenated vegetable oil, and carbomer matrix tablets was studied in vitro. The formulation containing 10% carbomer showed a sustained-release profile comparable to that of a standard, commercially available, sustained-rel...

journal_title：Pharmaceutical research

authors： Ciftçi K,Capan Y,Oztürk O,Hincal AA

更新日期：1990-04-01 00:00:00

abstract：:The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...

journal_title：Pharmaceutical research

authors： Valsami GN,Macheras PE,Koupparis MA

更新日期：1991-07-01 00:00:00

abstract：:An alternative procedure for the simultaneous determination of trimethoprim and sulfamethoxazole in an intravenous pharmaceutical formulation is presented. Infrared spectra of 14 calibration and 6 validation samples were collected using Fourier transform-infrared/attenuated total reflectance (FT-IR/ATR). Partial least...

journal_title：Pharmaceutical research

authors： Hartauer KJ,Guillory JK

更新日期：1989-07-01 00:00:00

abstract：UNLABELLED:PURPOSE; The aim of this study was to investigate asparagine (Asn) deamidation and aspartate (Asp) isomerization and to measure the content of isoaspartate (isoAsp) in recombinant human interleukin-11 (rhIL-11). METHODS:The rhIL-11 control and heat stressed samples were characterized with trypsin and endopr...

journal_title：Pharmaceutical research

authors： Zhang W,Czupryn JM,Boyle PT Jr,Amari J

更新日期：2002-08-01 00:00:00

abstract：PURPOSE:To evaluate the transcellular mechanism of novel enhancers absorption enhancement of human growth hormone (hGH), by examining the involvement of a P-glycoprotein-like efflux system, changes in membrane fluidity, and membrane damage. METHODS:Caco-2 cell monolayers were grown on Snapwell filter supports and plac...

journal_title：Pharmaceutical research

authors： Wu SJ,Robinson JR

更新日期：1999-08-01 00:00:00

abstract：PURPOSE:The purpose of this study was (i) to develop glancing angle x-ray powder diffractometry (XRD) as a method for profiling phase transformations as a function of tablet depth; and (ii) to apply this technique to (a) study indomethacin crystallization during dissolution of partially amorphous indomethacin tablets a...

journal_title：Pharmaceutical research

authors： Debnath S,Predecki P,Suryanarayanan R

更新日期：2004-01-01 00:00:00

abstract：PURPOSE:The objective of this study was to evaluate nanoparticle uptake by the Caco-2 monolayer model in vitro. Special emphasis was placed on the localization and the quantification of the uptake of fluorescently labeled polystyrene and poly(lactic-co-glycolic acid) (PLGA) nanoparticles. METHODS:Intracellular fluores...

journal_title：Pharmaceutical research

authors： Pietzonka P,Rothen-Rutishauser B,Langguth P,Wunderli-Allenspach H,Walter E,Merkle HP

更新日期：2002-05-01 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