Pharmaceutical Research
1573-904X
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Các bài báo tiêu biểu
Ritonavir: An Extraordinary Example of Conformational Polymorphism
Tập 18 Số 6 - Trang 859-866 - 2001
Purpose. In the summer of 1998, Norvir semi-solid capsules supplies were
threatened as a result of a new much less soluble crystal form of ritonavir.
This report provides characterization of the two polymorphs and the structures
and hydrogen bonding network for each form. Methods. Ritonavir polymorphism was
investigated using solid state spectroscopy and microscopy techniques including
solid state...
Inhibition of the Friend Retrovirus by Antisense Oligonucleotides Encapsulated in Liposomes: Mechanism of Action
Tập 10 Số 10 - Trang 1427-1433 - 1993
Proliferation of the Friend retrovirus was specifically inhibited by the env
mRNA complementary oligonucleotide encapsulated in pH-sensitive liposomes. This
observation was made using the focus immunoassay (FIA) and the reverse
transcriptase test. The key finding of the present study was the dramatic impact
on liposome penetration. For chronic or de novo infection, the point at which
the penetrati...
P-Glycoprotein Inhibition Leads to Enhanced Disruptive Effects by Anti-Microtubule Cytostatics at the In Vitro Blood-Brain Barrier
Tập 18 Số 5 - Trang 587-592 - 2001
Purpose. To investigate whether P–glycoprotein (Pgp) protects the in vitro BBB
against the cytotoxic effects of anti–tumour drugs. Methods. In an in vitro BBB
coculture model the influence of the anti–microtubule drugs vinblastine,
colchicine, paclitaxel and the non–antimicrotubule drugs doxorubicin,
fluorouracil and etoposide in the absence or presence of Pgp modulators on the
trans–endothelial e...
Proteolysis of Human Calcitonin in Excised Bovine Nasal Mucosa: Elucidation of the Metabolic Pathway by Liquid Secondary lonization Mass Spectrometry (LSIMS) and Matrix Assisted Laser Desorption lonization Mass Spectrometry (MALDI)
Tập 13 Số 11 - Trang 1679-1685 - 1996
Purpose. Two calcitonins, i.e. human calcitonin (hCT) and, for comparison,
salmon calcitonin (sCT), were chosen as peptide models to investigate nasal
mucosal metabolism. Methods. The susceptibility of hCT and sCT to nasal mucosal
enzymes was assessed by in-and-out reflection kinetics experiments in an in
vitro model based on the use of freshly excised bovine nasal mucosa, with the
mucosal surface...
A Solid-State NMR Study of Protein Hydration and Stability
Tập 15 Số 12 - Trang 1816-1821 - 1998
Purpose. The mobility of protein in powders at different hydration levels was
studied in relation to aggregation and activity. Methods. Magic angle spinning
13C, 15N, 1H, 2H, and 17O NMR techniques were used to determine changes in the
mobility of surface residues in proteins as a function of hydration and related
to changes in activity. NMR relaxation measurements of high frequency (ω0, T1)
and l...
Effect of Some Penetration Enhancers on Epithelial Membrane Lipid Domains: Evidence from Fluorescence Spectroscopy Studies
Tập 11 Số 2 - Trang 288-294 - 1994
The effect of the penetration enhancers Azone, oleic acid, 1-dodecanol, dodecyl
N,N-dimethylaminoacetate (DDAA), and dodecyl N,N-dimethylaminoisopropionate
(DDAIP) on epithelial membrane lipids was examined using human buccal cell
membranes as a model for epithelial lipid bilayer. Buccal epithelial cells (BEC)
were labeled with l,6-diphenyl-l,3,5-hexatriene (DPH),
l-(4-(trimethylammonio)phenyl)-6-...
Kinetics of Drug Decomposition by Heat Conduction Calorimetry
Tập 6 Số 1 - Trang 20-27 - 1989
The application of heat conduction calorimetry to the determination of
decomposition mechanisms and rates for drugs is shown to be a rapid and
generally useful method. The application of the method to determine the nature
of the decomposition reaction, sources of systematic errors in the method, the
equations relating the calorimetric signal to the kinetics of the reaction, and
some examples of re...
Influence of Drugs and Nutrients on Transporter Gene Expression Levels in Caco-2 and LS180 Intestinal Epithelial Cell Lines
Tập 20 Số 8 - Trang 1119-1124 - 2003
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-...
Formulation and Physical Characterization of Large Porous Particles for Inhalation
Tập 16 Số 11 - Trang 1735-1742 - 1999
Purpose. Relatively large (>5 µm) and porous (mass density < 0.4 g/cm3)
particles present advantages for the delivery of drugs to the lungs, e.g.,
excellent aerosolization properties. The aim of this study was, first, to
formulate such particles with excipients that are either FDA-approved for
inhalation or endogenous to the lungs; and second, to compare the aerodynamic
size and performance of the...
Carrier-Mediated Intestinal Transport of Drugs
- 1996
Recent advances in the field of carrier-mediated intestinal absorption of of
amino acids, oligopeptides, monosaccharides, monocarboxylic acids, phosphate,
bile acids and several water-soluble vitamins across brush-border and
basolateral membranes are summarized. An understanding of the molecular and
functional characteristics of the intestinal membrane transporters will be
helpful in the utilizati...