Pharmaceutical Research
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A Solid-State NMR Study of Protein Hydration and Stability
Pharmaceutical Research - 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...... hiện toàn bộ
What is the True Solubility Advantage for Amorphous Pharmaceuticals?
Pharmaceutical Research - Tập 17 Số 4 - Trang 397-404 - 2000
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
Pharmaceutical Research - Tập 19 Số 11 - Trang 1713-1719 - 2002
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
Hydrophilic Matrices for Controlled Drug Delivery: An Improved Mathematical Model to Predict the Resulting Drug Release Kinetics (the “sequential Layer” Model)
Pharmaceutical Research - 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 ...... hiện toàn bộ
Acute Renal Toxicity of Doxorubicin (Adriamycin)-Loaded Cyanoacrylate Nanoparticles
Pharmaceutical Research - - 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 ...... hiện toàn bộ
Ritonavir: An Extraordinary Example of Conformational Polymorphism
Pharmaceutical Research - 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...... hiện toàn bộ
In Vitro Evaluation of Polymerized Liposomes as an Oral Drug Delivery System
Pharmaceutical Research - 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...... hiện toàn bộ
Photo-Oxidation Mechanisms in Liquid Pharmaceutical Formulations: The Overlooked Role of Singlet Oxygen Presented as a Case Study
Pharmaceutical Research - - 2022
Oxidation is one of the most common degradation pathways for active pharmaceutical ingredients (APIs) in pharmaceutical formulations, mostly involving 1-electron processes via peroxy radicals and 2-electron processes by peroxides. In liquid pharmaceutical formulations, several factors can impact oxidative instabilities including pH, excipient impurities, headspace oxygen, and the potential for pho...... hiện toàn bộ
β-Adrenergic Receptor Polymorphisms: Cardiovascular Disease Associations and Pharmacogenetics
Pharmaceutical Research - Tập 19 Số 12 - Trang 1779-1787 - 2002
The β-adrenergic receptors (βAR) play important roles in cardiovascular function and disease, and both agonists and antagonists are widely used in various settings for treatment of cardiovascular disease. Both the β1AR and β2AR genes have several polymorphisms that are common in the population and result in encoding of different amino acids. More importantly, in vitro functional studies suggest th...... hiện toàn bộ
Tubular Localization and Tissue Distribution of Peptide Transporters in Rat Kidney
Pharmaceutical Research - Tập 15 Số 8 - Trang 1244-1249 - 1998
Purpose. To define the tubular localization and tissue distribution of PEPT1 (low-affinity, high-capacity transporter) and PEPT2 (high-affinity, low-capacity transporter) in rat kidney. Methods. mRNA expression of PEPT1 and PEPT2 was assessed with reverse transcription-polymerase chain reaction (RT-PCR) methods using cDNA prepared from microdissected nephron segments in rat. Tissue localization of...... hiện toàn bộ
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