Abstract:
PURPOSE:To study the reaction of artelinic acid with chemical model systems of cytochrome P-450 as a means of obtaining authentic samples of the putative metabolites necessary for identification of the mammalian metabolites of artelinic acid. METHODS:Artelinic acid was reacted with different organic complexes of iron(II). The reaction products were isolated and characterized by NMR and thermospray mass spectroscopy. RESULTS:Five compounds which are putative metabolites of artelinic acid were isolated from these reactions and unambiguously identified, while the identity of two other compounds await final confirmation. CONCLUSIONS:Standards of possible metabolites of artelinic acid can be produced by the reaction of the compound with ferrous complexes that may simulate cytochrome P-450 catalyzed metabolism of xenobiotics. This approach may provide a simple and versatile method for the formation of metabolites of artemisinin compounds which is more advantageous than previous approaches with fungal-based systems.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Idowu OR,Lin AJ,Grace JM,Peggins JOdoi
10.1023/a:1012185124972subject
Has Abstractpub_date
1997-10-01 00:00:00pages
1449-54issue
10eissn
0724-8741issn
1573-904Xjournal_volume
14pub_type
杂志文章abstract:PURPOSE:Simple uncoated compressed tablets with a central hole (donut-shape) are proposed to provide a constant drug release over a long period of time (> 20 hrs). The effect of hole size and drug solubility on the release kinetics is investigated. METHODS:The donut-shaped polyethylene oxide (PEO, Mw = 4 x 10(6)) tabl...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016218716951
更新日期:1995-07-01 00:00:00
abstract:PURPOSE:Novel therapeutics are greatly needed that target specific pathological receptors and pathways involved in Neuropathic Pain (NP). Extending our previous work published in this Journal on Group I metabotropic glutamate receptor (mGluR) modulators, we now investigate the therapeutic potential of niclosamide in mo...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2027-9
更新日期:2016-12-01 00:00:00
abstract:PURPOSE:To study Cereport (RMP-7, bradykinin B2 agonist) effects on human brain microvascular endothelial cell (HBMEC) monolayer permeability. METHODS:HBMEC grown on transwell membranes were exposed to Cereport. The monolayer permeability was determined with [14C]-inulin (MW. 5,200) and [3H]-dextran (MW. 70,000). RES...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018938722768
更新日期:1999-09-01 00:00:00
abstract:PURPOSE:The current study was designed to develop thiolated-graphene quantum dots (SH-GQDs) as a theranostic nanocarrier and evaluate its potential for the optimal scavenging of reactive oxygen species (ROS) in macrophages. METHODS:SH-GQDs were prepared by hydrothermal pyrolysis of carbon source (citric acid) in the p...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2000-7
更新日期:2016-11-01 00:00:00
abstract:PURPOSE:To study the influence of crystallizing and non-crystallizing cosolutes on the crystallization behavior of trehalose in frozen solutions and to monitor the phase behavior of trehalose dihydrate and mannitol hemihydrate during drying. METHODS:Trehalose (a lyoprotectant) and mannitol (a bulking agent) are widely...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0221-8
更新日期:2010-11-01 00:00:00
abstract:PURPOSE:To identify the key formulation factors controlling the initial drug and polymer dissolution rates from an amorphous solid dispersion (ASD). METHODS:Ketoconazole (KTZ) ASDs using PVP, PVP-VA, HMPC, or HPMC-AS as polymeric matrix were prepared. For each drug-polymer system, two types of formulations with the sa...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1969-2
更新日期:2016-10-01 00:00:00
abstract::Moexipril [2-[(1-ethoxycarbonyl)-3-phenylpropyl]amino-1-oxopropyl]-6, 7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (S,S,S)], an ester prodrug of an ACE inhibitor, was formulated in controlled-release preparations with a range of in vitro release rates, to provide a prolonged input of drug in vivo. Howe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015919413103
更新日期:1989-09-01 00:00:00
abstract:PURPOSE:The preparation of drug/cyclodextrin complexes is a suitable method to improve the dissolution of poor soluble drugs. The efficacy of the Controlled Particle Deposition (CPD) as a new developed method to prepare these complexes in a single stage process using supercritical carbon dioxide is therefore compared w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9177-0
更新日期:2007-03-01 00:00:00
abstract:PURPOSE:Nanocrystalline drug-polymer dispersions are of significant interest in pharmaceutical delivery. The purpose of this work is to demonstrate the applicability of methods based on two-dimensional (2D) and multinuclear solid-state NMR (SSNMR) to a novel nanocrystalline pharmaceutical dispersion of ebselen with pol...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0713-9
更新日期:2012-07-01 00:00:00
abstract:PURPOSE:To evaluate different dissolution testing methods and subsequently develop a simple to perform but reproducible and discriminating dissolution technique for inhalative powders. METHODS:From a dry powder a fraction of aerosolized particles with an aerodynamic particle size below 5 μm was collected on regenerate...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0744-2
更新日期:2012-08-01 00:00:00
abstract::The electrochemical properties of human cadaver skin were studied in a diffusion cell with impedance spectroscopy as a function of time in the absence and presence of penetration enhancers dodecyl N,N-dimethylamino acetate and Azone. An improved electrochemical model of skin is presented, and combining the novel model...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018984121415
更新日期:1993-03-01 00:00:00
abstract:BACKGROUND:Little is known about the affinity and stability of 99mTc-labeled 2-methoxyisobutylisonitrile (99mTc-MIBI) and tetrofosmin (99mTc-TF) for imaging of multiple drug resistance transporters in cancer. We examined the affinity of 99mTc-labeled compounds for these transporters and their stability. METHODS:99mTc-...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2548-5
更新日期:2018-11-29 00:00:00
abstract:PURPOSE:To assess the effects of co-delivering osteoinductive DNA and/or small interfering RNA in directing the osteogenic differentiation of human adipose-derived stem cells (hADSCs) using a combinatorial, non-viral gene delivery approach. METHODS:hADSCs were transfected using combinations of the following genes: BMP...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0406-9
更新日期:2011-06-01 00:00:00
abstract::The limitations of traditional gas adsorption models for describing water vapor sorption by amorphous pharmaceutical solids are described and an alternative approach based on polymer solution theories is proposed. The approach is tested by comparing a priori predicted isotherms with literature data for the poly(vinylp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018901325842
更新日期:1993-09-01 00:00:00
abstract::The effect of γ-cyclodextrin and its four derivatives on the solubility of progesterone in phosphate buffer pH 7.4 was investigated. γ-Cyclodextrin forms a complex precipitating from solution at low cyclodextrin concentrations. No precipitation of complexes was observed with the γ-cyclodextrin derivatives. This change...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016301919928
更新日期:1985-11-01 00:00:00
abstract:PURPOSE:To investigate cellular uptake pathways of novel anionic siRNA-lipoplexes as a function of formulation composition. METHODS:Anionic formulations with anionic lipid/Ca(2+)/siRNA ratio of 1.3/2.5/1 (AF1) and 1.3/0.3/1 (AF2) were utilized. Uptake mechanisms were investigated using uptake inhibition and co-localiz...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0952-9
更新日期:2013-04-01 00:00:00
abstract:PURPOSE:This work explores the distribution of water and its effects on molecular mobilities in poly(vinylpyrrolidone) (PVP) glasses using molecular dynamics (MD) simulation technology. METHODS:PVP glasses containing 0.5% and 10% w/w water and a small amount of ammonia and Phe-Asn-Gly were generated. Physical aging pr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-5277-5
更新日期:2005-08-01 00:00:00
abstract:PURPOSE:To assess the efficacy of lipid-protein-sugar particles (LPSPs) in providing prolonged duration local anesthesia by percutaneous injection. METHODS:Bupivacaine-containing LPSPs were characterized and optimized in vitro. Male Sprague-Dawley rats were given sciatic nerve blocks with bupivacaine-containing LPSPs....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1026470831256
更新日期:2000-10-01 00:00:00
abstract:PURPOSE:The purpose of this study was to stabilize the vinca alkaloids, vincristine sulfate (VCR) and vinblastine sulfate (VBL), in poly(lactide-co-glycolide) (PLGA) microspheres and to release the drugs in a sustained manner for more than a month. METHODS:An oil-in-oil emulsion-solvent extraction method was used to e...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007522013835
更新日期:2000-06-01 00:00:00
abstract:PURPOSE AND METHODS:Data from 358 pharmacist-patient encounters in 12 community pharmacies were used to investigate the association of prescription status, patient age, patient gender, and patient question asking with the content of pharmacist-patient communication. RESULTS:There was an association between prescriptio...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012084207399
更新日期:1997-02-01 00:00:00
abstract:PURPOSE:Although flomoxef (FMOX) has attracted substantial attention as an antibiotic against extended-spectrum beta-lactamase-producing Escherichia coli (ESBL-producing E. coli), the pharmacokinetics/pharmacodynamics (PK/PD) characteristics of FMOX against ESBL-producing E. coli is unclear. The aim of this study was t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02977-8
更新日期:2021-01-06 00:00:00
abstract:PURPOSE:To determine the different conformations of the acyloxyalkoxy-linked cyclic prodrug 1 of the model hexapeptide 2 in solution and to investigate the relationship between these solution conformations and the cellular permeability characteristics of this prodrug. METHODS:Two-dimensional Homonuclear Hartmann-Hahn ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016484522113
更新日期:1996-11-01 00:00:00
abstract:PURPOSE:Proteasome inhibition induces endoplasmic reticulum (ER) stress and compensatory autophagy to relieve ER stress. Disturbance of intracellular calcium homeostasis can lead to ER stress and alter the autophagy process. It has been suggested that inhibition of the proteasome disrupts intracellular calcium homeosta...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1139-8
更新日期:2013-09-01 00:00:00
abstract:PURPOSE:Platinum-based therapies are the first line treatments for most types of cancer including ovarian cancer. However, their use is associated with dose-limiting toxicities and resistance. We report initial translational studies of a theranostic nanoemulsion loaded with a cisplatin derivative, myrisplatin and pro-a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1660-z
更新日期:2015-08-01 00:00:00
abstract::Antibody drug conjugates (ADCs) are a class of therapeutics that combine the target specificity of an antibody with the potency of a chemotherapeutic. This therapeutic strategy can significantly expand the therapeutic index of a chemotherapeutic by minimizing the systemic exposure and associated toxicity of the chemot...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-012-0800-y
更新日期:2012-09-01 00:00:00
abstract::Equations for the steady-state volumes of distribution (Vss) and the mean residence times in the body (MRT) are derived for a drug and its metabolite subject to reversible metabolism and separately infused intravenously at a constant rate to steady state of both compounds. The Vss and MRT parameters are functions of t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015874329265
更新日期:1990-06-01 00:00:00
abstract::Hyaluronan (HA: hyaluronic acid) is produced in the interstitium and reaches the blood circulation through the lymph. It is rapidly eliminated by means of specific receptors on liver endothelium. The elimination characteristics of intravenously administered HA were studied in 10 conscious sheep at the normal plasma HA...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015982204926
更新日期:1989-08-01 00:00:00
abstract:PURPOSE:This study was designed to investigate the stability of recombinant FVIII (rFVIII) in solution at different pHs and to probe the cause(s) of rFVIII inactivation under accelerated storage conditions. METHODS:Aqueous stability samples of full-length rFVIII at different pHs were incubated at 40 degrees C for seve...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023271405005
更新日期:2003-04-01 00:00:00
abstract:PURPOSE:This study was conducted to assess the pharmacokinetics and pharmacodynamics of 7-nitroindazole (7-NI), a selective inhibitor of neuronal nitric oxide synthase (NOS). METHODS:Male Sprague-Dawley rats were equipped with peritoneal/ venous cannulae and a microdialysis probe in the hippocampal cortex. Rats receiv...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1013042817281
更新日期:2001-11-01 00:00:00
abstract:PURPOSE:Chemically modified heparin-DOCA was prepared and found to have markedly lower anticoagulant activity than heparin. In the present study, we elucidated the antiangiogenic and antitumoral activities of heparin-DOCA derivative. METHODS:To evaluate the antiangiogenic and antitumoral effects of heparin-DOCA, capil...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9139-6
更新日期:2007-01-01 00:00:00