Abstract:
:Microbial metabolism studies of the antimalarial drug arteether (1) have shown that arteether is metabolized by a number of microorganisms. Large-scale fermentation with Aspergillus niger (ATCC 10549) and Nocardia corallina (ATCC 19070) have resulted in the isolation of four microbial metabolites which have been characterized using two-dimensional nuclear magnetic resonance (2D-NMR) techniques. These metabolites have been identified as "AEM1" (2), 3 alpha-hydroxydeoxyarteether (3), 3 alpha-hydroxydeoxydihydroartemisinin (4), and deoxydihydroartemisinin (5).
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Lee IS,ElSohly HN,Hufford CDdoi
10.1023/a:1015845306124subject
Has Abstractpub_date
1990-02-01 00:00:00pages
199-203issue
2eissn
0724-8741issn
1573-904Xjournal_volume
7pub_type
杂志文章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:PURPOSE:Understanding the mechanism of protein-excipient interaction and illuminating the influencing factors on protein stability are key steps in the rational design of protein formulations. The objective of this study was to assess effects of preferential interaction type of excipient and surface aromatic hydrophobi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2152-0
更新日期:2017-07-01 00:00:00
abstract:PURPOSE:The specific interactions between three lectin-latex conjugates and different structures of rat intestinal mucosa have been studied ex vivo. METHODS:These systems were prepared by covalent coupling of different ligands, i.e., tomato lectin (TL), asparagus pea lectin (AL), mycoplasma gallisepticum lectin (ML), ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016405126656
更新日期:1996-11-01 00:00:00
abstract::The technique of Affinity capillary electrophoresis (ACE) is a useful tool to characterize complexation and partition equilibria. A wide range of applications in pharmaceutics has been presented: the determination of pKA values, of association constants between drugs and cyclodextrins or amphiphilic compounds as well ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:
更新日期:1999-11-01 00:00:00
abstract:PURPOSE:To study the oxidative degradation of drugs using a hydrophilic free radical initiator, 2,2'-Azobis(-amidinopropane) dihydrochloride (AAPH). METHODS:AAPH was used as the free radical initiator to study oxidation of three model compounds (A, B, and C), which represent different oxidizable moieties. In the solut...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-1199-x
更新日期:2005-02-01 00:00:00
abstract:PURPOSE:Relatively large (>5 microm) and porous (mass density <0.4 g/cm3) particles present advantages for the delivery of drugs to the lungs, e.g., excellent aerosolization properties. The aim of this study was, first, to formulate such particles with excipients that are either FDA-approved for inhalation or endogenou...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910200420
更新日期:1999-11-01 00:00:00
abstract:PURPOSE:The aim of this study was to test the ability of paclitaxel-loaded poly(butylcyanoacrylate) (PBCA) nanoparticles to overcome multidrug resistance (MDR) in human ovarian resistant cells (A2780/T) and investigate its possible mechanism. METHODS:We prepared paclitaxel-loaded PBCA nanoparticles by interfacial poly...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0346-9
更新日期:2011-04-01 00:00:00
abstract::One of the authors has his name incorrectly indexed in PubMed and SpringerLink as "Laird Forrest M" (last name "Laird Forrest"). His name should index as "Forrest M. Laird" with last name as "Forrest". ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,已发布勘误
doi:10.1007/s11095-018-2463-9
更新日期:2018-07-25 00:00:00
abstract:PURPOSE:Grapefruit juice (GJ) is known to increase the oral bioavailability of many CYP3A-substrates by inhibiting intestinal phase-I metabolism. However, the magnitude of AUC increase is often insignificant and highly variable. Since we earlier suggested that CYP3A and P-glycoprotein (P-gp) form a concerted barrier to...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011902625609
更新日期:1999-04-01 00:00:00
abstract:PURPOSE:This study was conducted to demonstrate the use of differential scanning calorimetry (DSC) in detecting and measuring beta-relaxation processes in amorphous pharmaceutical systems. METHODS:DSC was employed to study amorphous samples of poly(vinylpyrrolidone) (PVP), indomethacin (IM), and ursodeoxycholic acid (...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-9044-4
更新日期:2006-02-01 00:00:00
abstract:PURPOSE:The gadopentetic acid (Gd-DTPA)-loaded chitosan nanoparticles (Gd-nanoCPs) were prepared for gadolinium neutron-capture therapy (Gd-NCT) and characterized and evaluated as a device for intratumoral (i.t.) injection. METHODS:Gd-nanoCPs were prepared by a novel emulsion-droplet coalescence technique. The effects...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018995124527
更新日期:1999-12-01 00:00:00
abstract::To evaluate the effects of a neutron activation radiolabeling technique on an enteric-coated multiparticulate formulation of erythromycin, test quantities were produced under industrial pilot scale conditions. The pellets contained the stable isotope erbium oxide (Er-170), which was later converted by neutron activati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015826229323
更新日期:1990-03-01 00:00:00
abstract::The three-dimensional structures and molecular electrostatic potentials of the cis(Z) and trans(E)-isomers of flupenthixol and clopenthixol were examined by computer graphics and molecular mechanical and quantum mechanical calculations, and their internal molecular motions were studied by molecular dynamics simulation...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015842926345
更新日期:1991-04-01 00:00:00
abstract::Nanotechnology has continuously contributed to the fast development of diagnostic and therapeutic agents. Theranostic nanomedicine has encompassed the ongoing efforts on concurrent molecular imaging of biomarkers, delivery of therapeutic agents, and monitoring of therapy response. Among these formulations, polymer-bas...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-013-1103-7
更新日期:2014-06-01 00:00:00
abstract::The intrasubject and intersubject variabilities for CGS 16617, an angiotensin converting enzyme inhibitor, were evaluated in an open-label, repeat single-dose bioavailability trial. Eight healthy male volunteers each received a 20-mg oral dose of CGS 16617 as an aqueous solution on four separate occasions. Components ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015954609527
更新日期:1989-04-01 00:00:00
abstract:PURPOSE:Evaluate the ability of (-)-6-aminocarbovir ((-)-6AC) to improve the CNS exposure to (-)-carbovir ((-)-CBV). METHODS:Activation of (-)-6AC in vitro was assessed by incubations of rat brain tissue homogenates. The in vivo brain exposure to (-)-CBV was then examined in rats after iv infusions of either (-)-CBV (...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016229624703
更新日期:1995-06-01 00:00:00
abstract::High molecular weight drugs in general, and peptides in particular, are usually delivered by parenteral route because they are poorly absorbed or degraded in the gastrointestinal tract. To optimize therapy, it is desirable to search for nonparenteral routes of administration and to deliver the drug in a controlled-rel...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018948924992
更新日期:1993-06-01 00:00:00
abstract:PURPOSE:This study was carried out to examine the blood-brain barrier (BBB) transport of human basic fibroblast growth factor (bFGF) and investigate its mechanism. METHODS:The BBB transport of 125I-bFGF was measured by several in vivo methods including intravenous administration, in situ internal carotid artery perfus...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570509232
更新日期:2000-01-01 00:00:00
abstract::The binding of 1-anilino-8-naphthalenesulfonate (ANS) to bovine serum albumin (BSA), human serum albumin (HSA), and human plasma has been studied by potentiometric titration utilizing a laboratory constructed ion selective electrode (ISE) of ANS. Three classes of ANS binding sites were found on BSA, HSA, and plasma at...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015855613083
更新日期:1991-07-01 00:00:00
abstract:PURPOSE:A rapid immune response is required to prevent death from Anthrax, caused by Bacillus anthracis. METHOD:We formulated a vaccine carrier comprised of acetalated dextran microparticles encapsulating recombinant protective antigen (rPA) and resiquimod (a toll-like receptor 7/8 agonist). RESULTS:We were able to p...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-0975-x
更新日期:2013-05-01 00:00:00
abstract:PURPOSE:To examine whether the glass transition temperature (Tg) of freeze-dried formulations containing polymer excipients can be accurately predicted by molecular dynamics simulation using software currently available on the market. Molecular dynamics simulations were carried out for isomaltodecaose, a fragment of de...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1023831102203
更新日期:2003-06-01 00:00:00
abstract::Lidocaine was administered to healthy volunteers at different sites in the rectum. Unchanged drug and monoethylglycinexylidide (MEGX) concentrations were measured in plasma with a newly developed gas chromatographic method. Lidocaine was given rectally by means of an osmotic system (Osmet(®)) which delivered 25 mg/h a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016380104424
更新日期:1984-05-01 00:00:00
abstract:PURPOSE:S-(4-Nitrobenzyl)-6-thioinosine (NBMPR) is routinely used at concentrations of 0.10 μM and 0.10 mM to specifically inhibit transport of nucleosides mediated by equilibrative nucleoside transporters 1 (ENT1) and 2 (ENT2), respectively. We recently showed that NBMPR (0.10 mM) might also inhibit placental active e...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-2782-5
更新日期:2020-02-21 00:00:00
abstract:PURPOSE:To develop a statistical model for predicting effect of food on the extent of absorption (area under the curve of time-plasma concentration profile, AUC) of drugs based on physicochemical properties. MATERIALS AND METHODS:Logistic regression was applied to establish the relationship between the effect of food ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9236-1
更新日期:2007-06-01 00:00:00
abstract:PURPOSE:The purpose of this study was to develop a new computational fluid dynamics (CFD)-based model of the complex transport and droplet drying kinetics within a laboratory-scale spray dryer, and relate CFD-predicted drying parameters to powder aerosolization metrics from a reference dry powder inhaler (DPI). METHOD...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-02806-y
更新日期:2020-05-21 00:00:00
abstract:PURPOSE:HSP90 (Heat shock protein 90kD) has been validated as a therapeutic target in Castrate Resistant Prostate Cancer. Unfortunately, HSP90 inhibitors suffer from dose-limiting toxicities that hinder their clinical applications. Previously developed polymeric delivery systems for HSP90 inhibitors had either low drug...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2249-5
更新日期:2017-12-01 00:00:00
abstract:PURPOSE:The aim of this study is to investigate the effects of 50% ethyl acetate extracts of grapefruit juice (GFJ) and orange juice (OJ) on the transport activity of P-glycoprotein (P-gp) in the rat small intestine. METHODS:The efflux of P-gp substrates from rat everted sac in the absence or presence of verapamil, GF...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016100715125
更新日期:2002-06-01 00:00:00
abstract:PURPOSE:Phase II metabolism involves the conjugation of a polar moiety, such as sulfate or glucuronic acid, to a (relatively) nonpolar xenobiotic. Although it might be expected that such conjugates may exhibit amphiphilic character (e.g., surface activity and potential to form micelles), no detailed study of the micell...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1022672608657
更新日期:2003-03-01 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:This study was conducted to investigate the cause of incomplete protein release from photopolymerized poly(ethylene glycol) (PEG) hydrogels and verify the protein-protection mechanism provided by iminodiacetic acid (IDA). METHODS:The in vitro release of bovine serum albumin (BSA) from PEG hydrogels prepared un...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-9395-x
更新日期:2006-03-01 00:00:00