Pharmaceutical Research

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Evidence for Overlapping Substrate Specificity Between Large Neutral Amino Acid (LNAA) and Dipeptide (hPEPTl) Transporters for PD 158473, an NMDA Antagonist
Pharmaceutical Research - Tập 16 Số 3 - Trang 391-395 - 1999
Surendran, Narayanan, Covitz, Kuang-Ming Y., Han, Hyo-kyung, Sadee, Wolfgang, Oh, Doo-Man, Amidon, Gordon L., Williamson, Rufus M., Bigge, Christopher F., Stewart, Barbra H.
Purpose. The objective of this research was to investigate the substrate specificity of large neutral amino acid carrier (LNAA) and di/tripeptide (hPEPTl) transporters with respect to PD 158473, an NMDA antagonist. Methods. Cellular uptake studies were carried out using two types of Chinese Hamster Ovary (CHO). CHO-K1 cells represent the wild type with inherent large neutral amino acid (LNAA) acti...... hiện toàn bộ
Peptide Acylation by Poly(α-Hydroxy Esters)
Pharmaceutical Research - Tập 19 Số 2 - Trang 175-181 - 2002
Lucke, Andrea, Kiermaier, Josef, Göpferich, Achim
Purpose. Poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLGA) microspheres were investigated concerning the possible acylation of incorporated peptides. Methods. Atrial natriuretic peptide (ANP) and salmon calcitonin (sCT) were encapsulated into PLA and PLGA microspheres. Peptide integrity was monitored by HPLC-MS analysis during microsphere degradation for four weeks. sCT fragmentatio...... hiện toàn bộ
An Evaluation of the Use of Modulated Temperature DSC as a Means of Assessing the Relaxation Behaviour of Amorphous Lactose
Pharmaceutical Research - Tập 17 Số 6 - Trang 696-700 - 2000
Craig, Duncan Q. M., Barsnes, Merete, Royall, Paul G., Kett, Vicky L.
Purpose. To evaluate the use of Modulated Temperature DSC(MTDSC) as a means of assessing the relaxation behaviour ofamorphous lactose via measurement of the heat capacity, glasstransition (Tg) and relaxation endotherm. Methods. Samples of amorphous lactose were prepared by freezedrying. MTDSC was conducted using a TA Instruments 2920 MDSCusing a heating rate of 2°C/minute, a modulation amplitude o...... hiện toàn bộ
Tubular Localization and Tissue Distribution of Peptide Transporters in Rat Kidney
Pharmaceutical Research - Tập 15 Số 8 - Trang 1244-1249 - 1998
Smith, David E., Pavlova, Anna, Berger, Urs V., Hediger, Matthias A., Yang, Tianxin, Huang, Yuning G., Schnermann, Jürgen B.
Purpose. To define the tubular localization and tissue distribution of PEPT1 (low-affinity, high-capacity transporter) and PEPT2 (high-affinity, low-capacity transporter) in rat kidney. Methods. mRNA expression of PEPT1 and PEPT2 was assessed with reverse transcription-polymerase chain reaction (RT-PCR) methods using cDNA prepared from microdissected nephron segments in rat. Tissue localization of...... hiện toàn bộ
Intestinal Transport of β-Lactam Antibiotics: Analysis of the Affinity at the H+/Peptide Symporter (PEPT1), the Uptake into Caco-2 Cell Monolayers and the Transepithelial Flux
Pharmaceutical Research - Tập 16 Số 1 - Trang 55-61 - 1999
Bretschneider, Beate, Brandsch, Matthias, Neubert, Reinhard
Purpose. This study on the intestinal transport of β-lactam antibiotics was undertaken to investigate the correlation between cellular transport parameters and the bioavailability. Methods. Transport of 23 β-lactam antibiotics was characterized by measuring their ability to inhibit the uptake of glycylsarcosine into Caco-2 cells, their uptake into the cells and their total flux across the cell mon...... hiện toàn bộ
Passive and Carrier-Mediated Intestinal Absorption Components of Two Angiotensin Converting Enzyme (ACE) Inhibitor Prodrugs in Rats: Enalapril and Fosinopril
Pharmaceutical Research - Tập 6 Số 12 - Trang 1043-1047 - 1989
Friedman, Doron I., Amidon, Gordon L.
The intestinal absorption mechanism of two ACE inhibitor prodrugs, enalapril and fosinopril, was investigated in rats using a single-pass perfusion method. A modified boundary layer solution was applied to determine the apparent intestinal wall permeability. The prodrug enalapril is well absorbed from rat jejunum, whereas the parent drug, enalaprilat, is poorly absorbed. The permeability of enalap...... hiện toàn bộ
Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats
Pharmaceutical Research - Tập 11 Số 6 - Trang 909-913 - 1994
Morita, Takahiro, Yamamoto, Akira, Takakura, Yoshinobu, Hashida, Mitsuru, Sezaki, Hitoshi
The effects of protease inhibitors, Na-glycocholate, bacitracin, bestatin, nafamostat mesilate and soybean trypsin inhibitor (STI) on the pulmonary absorption of (Asu1,7)-eel calcitonin (ECT, molecular weight 3363) were investigated in rats. The pulmonary absorption of ECT was estimated by measuring its hypocalcemic effect. When ECT alone was administered into the lung, the pharmacological availab...... hiện toàn bộ
In Vivo Evaluation of a Colon-Specific Drug Delivery System: An Absorption Study of Theophylline from Capsules Coated with Azo Polymers in Rats
Pharmaceutical Research - Tập 12 Số 2 - Trang 244-247 - 1995
Van den Mooter, Guy, Samyn, Celest, Kinget, Renaat
Azo polymers based upon 2-hydroxyethyl methacrylate, methyl methacrylate, and methacrylic acid, and containing N,N′-bis [(methacryloyloxyethyl)oxy(carbonylamino)]azobenzene as azo aromatic agent were evaluated in vivo as coatings for colon-specific drug delivery. The gastrointestinal absorption of theophylline from capsules coated with the azo polymers was examined in the proximal part of the smal...... hiện toàn bộ
In Vivo and in Vitro Assessment of Baseline Blood-Brain Barrier Parameters in the Presence of Novel Nanoparticles
Pharmaceutical Research - Tập 20 Số 5 - Trang 705-713 - 2003
Lockman, Paul R., Koziara, Joanna, Roder, Karen E., Paulson, Jennifer, Abbruscato, Thomas J., Mumper, Russell J., Allen, David D.
Purpose. Nanoparticles have advantage as CNS drug delivery vehicles given they disguise drug permeation limiting characteristics. Conflicting toxicological data, however, is published with regard to blood-brain barrier integrity and gross mortality. Methods. To address this issue two novel nanoparticle types: “emulsifying wax/Brij 78”and Brij 72/Tween 80 nanoparticles were evaluated in vivo for ef...... hiện toàn bộ
Influence of Drugs and Nutrients on Transporter Gene Expression Levels in Caco-2 and LS180 Intestinal Epithelial Cell Lines
Pharmaceutical Research - Tập 20 Số 8 - Trang 1119-1124 - 2003
Li, Qing, Sai, Yoshimichi, Kato, Yukio, Tamai, Ikumi, Tsuji, Akira
Purpose. The aim of this study was to investigate the influences of various drugs and nutrients on the expression levels of intestinal drug transporters PEPT1, MDR1, MRP2 and MRP3, and drug-metabolizing enzyme CYP3A4. Methods. Quantitative reverse transcriptase polymerase chain reaction was used to quantitate transporter and CYP3A4 mRNAs. Western blotting was used to determine protein levels of P-...... hiện toàn bộ
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