Pharmaceutical Research
1573-904X
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Các bài báo tiêu biểu
Acute Renal Toxicity of Doxorubicin (Adriamycin)-Loaded Cyanoacrylate Nanoparticles
- 1995
Acute doxorubicin-loaded nanoparticle (DXNP) renal toxicity was explored in both
normal rats and rats with experimental glomerulo-nephritis. In normal rats, 2/6
rats given free doxorubicin (DX) (5 mg / kg) died within one week, whereas all
control animals and all rats having received free NP or DXNP survived. A 3 times
higher proteinuria appeared in animals treated with DXNP than in those treated
...
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...
Dissolution Testing as a Prognostic Tool for Oral Drug Absorption: Immediate Release Dosage Forms
Tập 15 Số 1 - Trang 11-22 - 1998
Dissolution tests are used for many purposes in the pharmaceutical industry: in
the development of new products, for quality control and, to assist with the
determination of bioequivalence. Recent regulatory developments such as the
Biopharmaceutics Classification Scheme have highlighted the importance of
dissolution in the regulation of post-approval changes and introduced the
possibility of subs...
Passive and Carrier-Mediated Intestinal Absorption Components of Two Angiotensin Converting Enzyme (ACE) Inhibitor Prodrugs in Rats: Enalapril and Fosinopril
Tập 6 Số 12 - Trang 1043-1047 - 1989
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...
Comparison of the Anticancer Effect of Free and HPMA Copolymer-Bound Adriamycin in Human Ovarian Carcinoma Cells
Tập 16 Số 7 - Trang 986-996 - 1999
Purpose. To study peculiarities and the mechanism of the anticancer effect of
free and HPMA copolymer-bound ADR in sensitive and resistant human ovarian
carcinoma cells. Methods. Sensitive A2780 and ADR resistant A2780/AD cells were
exposed to different doses of drugs during 12, 24, 36, 48, 60, and 72 hours.
Cell viability, drug accumulation, apoptosis, cellular metabolism, lipid
peroxidation, DNA...
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...
Supersaturation: Enhancement of Skin Penetration and Permeation of a Lipophilic Drug
Tập 18 Số 7 - Trang 1006-1011 - 2001
Purpose. To increase the dermal delivery of a lipophilic model compound (LAP),
and to deduce the underlying mechanism of enhanced absorption. Methods.
Penetration of LAP from mixtures of up to four degrees of saturation into the
stratum corneum was evaluated using a tape-stripping method; epidermal
permeation of the drug was measured in Franz diffusion cells. The relative
diffusion and stratum cor...
Polar Molecular Surface Properties Predict the Intestinal Absorption of Drugs in Humans
Tập 14 Số 5 - Trang 568-571 - 1997
Purpose. A theoretical method has been devised for prediction of drug absorption
after oral administration to humans. Methods. Twenty structurally diverse model
drugs, ranging from 0.3 to 100% absorbed, were investigated. The compounds also
displayed diversity in physicochemical properties such as lipophilicity,
hydrogen bonding potential and molecular size. The dynamic molecular surface
propertie...
5′-Amino Acid Esters of Antiviral Nucleosides, Acyclovir, and AZT Are Absorbed by the Intestinal PEPT1 Peptide Transporter
Tập 15 Số 8 - Trang 1154-1159 - 1998
Purpose. General use of nucleoside analogues in the treatment of viral
infections and cancer is often limited by poor oral absorption. Valacyclovir, a
water soluble amino acid ester prodrug of acyclovir has been reported to
increase the oral bioavailability of acyclovir but its absorption mechanism is
unknown. This study characterized the intestinal absorption mechanism of
5′-amino acid ester prod...
HPMC-Matrices for Controlled Drug Delivery: A New Model Combining Diffusion, Swelling, and Dissolution Mechanisms and Predicting the Release Kinetics
Tập 16 Số 11 - Trang 1748-1756 - 1999
Purpose. The purpose of this study was to investigate the drug release
mechanisms from hydroxypropyl methylcellulose (HPMC)-matrices, and to develop a
new model for quantitative predictions of controlled drug delivery. Methods. The
dissolved mass of pure HPMC-matrices and the drug release rate from propranolol
HCl-loaded HPMC-matrices were determined experimentally. Based on Fick's second
law of d...