Pharmaceutical Research
1573-904X
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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 ...
Application of Microdialysis in Pharmacokinetic Studies
Tập 14 Số 3 - Trang 267-288 - 1997
The objective of this review is to survey the recent literature regarding the
various applications of microdialysis in pharmacokinetics. Microdialysis is a
relatively new technique for sampling tissue extracellular fluid that is gaining
popularity in pharmacokinetic and pharmacodynamic studies, both in experimental
animals and humans. The first part of this review discusses various aspects of
the ...
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...
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...
The Oral Absorption of Micro- and Nanoparticulates: Neither Exceptional Nor Unusual
Tập 14 Số 3 - Trang 259-266 - 1997
This mini-review covers some of the historical and recent arguments over the
experimental evidence on the uptake by and translocation from the intestinal
mucosa of microparticulates after oral administration. It is concluded that
there is now no dispute over the fact that this is a normal occurrence.
Particulate uptake does take place, not only via the M-cells in the Peyer's
patches and the isolat...
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...
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...
Pulmonary Delivery of Salmon Calcitonin Dry Powders Containing Absorption Enhancers in Rats
Tập 13 Số 1 - Trang 80-83 - 1996
Purpose. To evaluate the effects of absorption enhancers in dry powders and in
liquids, pulmonary absorption of salmon calcitonin (sCT) in various formulations
was measured. Methods. The dry powder of sCT was prepared by a freeze-drying
method with a jet mill. After intratracheal administration of sCT dry powder and
liquid (solution) preparations to rats, plasma sCT levels and calcium levels
were ...
Moisture-Induced Aggregation of Lyophilized Insulin
Tập 11 Số 1 - Trang 21-29 - 1994
A critical problem in the storage and delivery of pharmaceutical proteins is
aggregation in the solid state induced by elevated temperature and moisture.
These conditions are particularly relevant for studies of protein stability
during accelerated storage or for proteins loaded in polymeric delivery devices
in vivo. In the present investigation, we have found that, when exposed to an
environment ...
Use of Solid Corrugated Particles to Enhance Powder Aerosol Performance
Tập 18 Số 11 - Trang 1570-1577 - 2001
Purpose. To study the dispersion performance of non-porous corrugated particles,
with a focus on the effect of particle surface morphology on aerosolization of
bovine serum albumin (BSA) powders. Methods. The solid-state characteristics of
the spray-dried BSA powders, one consisting of smooth spherical particles and
another corrugated particles, were characterized by laser diffraction, X-ray
powde...