Ritonavir: An Extraordinary Example of Conformational Polymorphism Tập 18 Số 6 - Trang 859-866 - 2001
Bauer, John, Spanton, Stephen, Henry, Rodger, Quick, John, Dziki, Walter, Porter, William, Morris, John
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... hiện toàn bộ
What is the True Solubility Advantage for Amorphous Pharmaceuticals? Tập 17 Số 4 - Trang 397-404 - 2000
Hancock, Bruno C., Parks, Michael
Purpose. To evaluate the magnitude of the solubility advantage foramorphous
pharmaceutical materials when compared to their crystallinecounterparts.Methods.
The thermal properties of several drugs in their amorphousand crystalline states
were determined using differential scanningcalorimetry. From these properties
the solubility advantage for theamorphous form was predicted as a function of
temper... hiện toàn bộ
Poly(d,l-Lactide-Co-Glycolide) Encapsulated Poly(Vinyl Alcohol) Hydrogel as a Drug Delivery System Tập 19 Số 11 - Trang 1713-1719 - 2002
Mandal, Tarun K., Bostanian, Levon A., Graves, Richard A., Chapman, Sharlene R.
Purpose. The efficiency of encapsulation of water-soluble drugs in biodegradable
polymer is often low and occasionally these microcapsules are associated with
high burst effect. The primary objective of this study is to develop a novel
microencapsulation technique with high efficiency of encapsulation and low burst
effect. Method. Pentamidine was used as a model drug in this study.
Pentamidine/pol... hiện toàn bộ
Induction of Apoptosis in WEHI 231 Cells by Cationic Liposomes Tập 17 Số 5 - Trang 515-520 - 2000
Aramaki, Yukihiko, Takano, Shuhei, Arima, Hidetoshi, Tsuchiya, Seishi
Purpose. Liposomes are of considerable interest as drug carriers
andimmunoadjuvants. However, few investigators have studied thechanges exerted
by liposomes in the cells with which they interact.The purpose of this study was
to investigate whether liposomes induceapoptosis in B cells. Methods. The mouse
immature B cell line WEHI 231 cells and mousesplenic B cells were treated with
liposomes, and t... hiện toàn bộ
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
Lang, Steffen R., Staudenmann, Werner, James, Peter, Manz, Hans-Jörg, Kessler, Rudolf, Galli, Bruno, Moser, Hans-Peter, Rummelt, Andreas, Merkle, Hans P.
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... hiện toàn bộ
A Solid-State NMR Study of Protein Hydration and Stability Tập 15 Số 12 - Trang 1816-1821 - 1998
Separovic, F., Lam, Y. H., Ke, X., Chan, H.-K.
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... hiện toàn bộ
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
Minko, Tamara, Kopečková, Pavla, Kopeček, Jindřich
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... hiện toàn bộ
Effect of Some Penetration Enhancers on Epithelial Membrane Lipid Domains: Evidence from Fluorescence Spectroscopy Studies Tập 11 Số 2 - Trang 288-294 - 1994
Turunen, T. Marjukka, Urtti, Arto, Paronen, Petteri, Audus, Kenneth L., Rytting, J. Howard
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-... hiện toàn bộ
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
Han, Hyo-kyung, de Vrueh, Remco L. A., Rhie, Julie K., Covitz, Kuang-Ming Y., Smith, Philip L., Lee, Chao-Pin, Oh, Doo-Man, Sadee, Wolfgang, Amidon1, Gordon L.
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... hiện toàn bộ