Pharmaceutical Research
1573-904X
Cơ quản chủ quản: N/A
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Các bài báo tiêu biểu
Development of a Remote Electrode System for Monitoring the Water Content of Materials Inside a Glass Vial
Tập 19 Số 3 - Trang 337-344 - 2002
Purpose: This article explores the use of a remote electrode dielectric measurement system to monitor the water content of hydrated ovalbumin inside a glass vial. Methods: The intrinsic dielectric properties of hydrated ovalbumin were characterized first using conventional parallel plate electrodes. The second stage was to simulate a remote electrode measurement by placing nonconductive, nondisper......
In Vitro Evaluation of Polymerized Liposomes as an Oral Drug Delivery System
Tập 12 Số 4 - Trang 576-582 - 1995
The physical characteristics of polymerized liposomes for potential use as an oral drug delivery system were examined in vitro. The trap efficiency in monomeric liposomes composed of 1,2-di (2,4-octadecadienoyl) phosphatidylcholine was increased from 3% for original multilamellar vesicles to 35% for freeze-thaw treated liposomes. Polymerized liposomes with azobis (isobutyronitrile) and azobis (2-a......
Hydrophilic Matrices for Controlled Drug Delivery: An Improved Mathematical Model to Predict the Resulting Drug Release Kinetics (the “sequential Layer” Model)
Tập 17 Số 10 - Trang 1290-1298 - 2000
Purpose. The aims of this study were (i) to elucidate the transport mechanisms involved in drug release from hydrophilic matrices; and (ii) to develop an improved mathematical model allowing quantitative predictions of the resulting release kinetics. Methods. Our previously presented model has been substantially modified, by adding: (i) inhomogeneous swelling; (ii) poorly water-soluble drugs; and ......
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
Tập 16 Số 1 - Trang 55-61 - 1999
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......
Efficiency of Cytoplasmic Delivery by pH-Sensitive Liposomes to Cells in Culture
Tập 7 Số 8 - Trang 824-834 - 1990
The intracellular processing of pH-sensitive liposomes composed of cholesterylhemisuccinate (CHEMS) and dioleoylphosphatidylethanolamine (DOPE) by eukaryotic cell lines has been compared to non-pH-sensitive liposomes made of CHEMS and dioleoylphosphatidylcholine (DOPC). The pH-sensitive liposomes can deliver encapsulated fluorescent molecules [calcein, fluoresceinated dextran, fluoresceinated poly......
The Stability of Insulin in Crystalline and Amorphous Solids: Observation of Greater Stability for the Amorphous Form
Tập 14 Số 10 - Trang 1379-1387 - 1997
Purpose. Generalizations based upon behavior of small molecules have established that a crystalline solid is generally much more stable toward chemical degradation than is the amorphous solid. This study examines the validity of this generalization for proteins using biosynthetic human insulin as the model protein. Methods. Amorphous insulin was prepared by freeze drying the supernate from a suspe......
Improvement of the Pulmonary Absorption of (Asu1,7)-Eel Calcitonin by Various Protease Inhibitors in Rats
Tập 11 Số 6 - Trang 909-913 - 1994
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......
Evidence for an Interaction Between the β-Blocker Pafenolol and Bile Salts in the Intestinal Lumen of the Rat Leading to Dose-Dependent Oral Absorption and Double Peaks in the Plasma Concentration–Time Profile
Tập 10 Số 6 - Trang 879-883 - 1993
Pafenolol is a β-blocker with unusual oral absorption properties. The blood concentration–time profile exhibits two peaks, and the bioavailability is low and dose dependent because of incomplete and nonlinear intestinal uptake. We addressed the question whether the intestinal absorption of pafenolol was affected by bile depletion in the gut lumen of rats. Further, the hypothesis that variable gast......
In Vitro and In Situ Absorption of SDZ-RAD Using a Human Intestinal Cell Line (Caco-2) and a Single Pass Perfusion Model in Rats: Comparison with Rapamycin
Tập 15 Số 11 - Trang 1666-1672 - 1998
Purpose. To compare the intestinal absorption and active efflux protein susceptibility of a new immunosuppressive agent (SDZ-RAD) with that of its analog rapamycin. Methods. Caco-2 cell monolayers were used to examine bidirectional transport of the two compounds at low micromolar concentrations. Single pass rat intestinal perfusion was also used to examine steady state permeability. Results. Rapam......