Abstract:
PURPOSE:The development of a physiologically based absorption model for orally administered drugs in rats is described. METHODS:Unlike other models that use a multicompartmental approach, the GI tract is modeled as a continuous tube with spatially varying properties. The mass transport through the intestinal lumen is described via an intestinal transit function. The only substance-specific input parameters of the model are the intestinal permeability coefficient and the solubility in the intestinal fluid. With this physiologic and physicochemical information, the complete temporal and spatial absorption profile can be calculated. RESULTS:A first performance test using portal concentration data published in the literature yielded an excellent agreement between measured and simulated temporal absorption profiles in the portal vein. Furthermore, the dose dependence of a compound with solubility-limited fraction dose absorbed in rats (chlorothiazide) could be adequately described by the model. CONCLUSIONS:The continuous absorption model is well suited to simulate drug flow and absorption in the GI tract of rats.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Willmann S,Schmitt W,Keldenich J,Dressman JBdoi
10.1023/b:pham.0000003373.72652.c0subject
Has Abstractpub_date
2003-11-01 00:00:00pages
1766-71issue
11eissn
0724-8741issn
1573-904Xjournal_volume
20pub_type
杂志文章abstract::Lecithin-stabilized triglyceride emulsions are subject to hydrolysis by pancreatic lipase. The time profiles of these reactions are characterized by a lag-phase and a zero-order phase. Lag phases are more pronounced with long-chain triglycerides. Ca2+ is effective in reducing the lag-phase and activating lipase. Kinet...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015956104500
更新日期:1989-06-01 00:00:00
abstract:PURPOSE:To examine the effect of particle size and morphology on aerosol dispersion using jet-milled and spray-dried mannitol particles in narrow size distributions within the respirable range. METHODS:Particle size and morphology were examined by laser diffraction and scanning electron microscopy, respectively. Aeros...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000033007.27278.60
更新日期:2004-07-01 00:00:00
abstract::Although much effort has been devoted to opioid research since the identification of enkephalins, understanding of the physiological importance and mechanisms of action of endogenous opioids lags behind understanding of opiate alkaloids such as morphine. In recent years, several novel approaches have been refined with...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1015809702296
更新日期:1991-01-01 00:00:00
abstract:PURPOSE:To provide a systematic biophysical approach towards a better understanding of impact of conjugation chemistry on higher order structure and physical stability of an antibody drug conjugate (ADC). METHODS:ADC was prepared using thiol-maleimide chemistry. Physical stabilities of ADC and its parent IgG1 mAb were...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1274-2
更新日期:2014-07-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-1882-y
更新日期:2005-03-01 00:00:00
abstract:PURPOSE:Effects of polyvinylpyrrolidone (PVP) molecular weight on the solid-state intermolecular interactions among probucol/PVP/sodium dodecyl sulfate (SDS) ternary ground mixtures (GM) and the formation of nanoparticles were investigated by solid-state NMR spectroscopy. MATERIALS AND METHODS:Ternary GMs of probucol ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9089-z
更新日期:2006-11-01 00:00:00
abstract::The use of nanoparticulate pharmaceutical carriers to enhance the in vivo efficiency of many drugs well established itself over the past decade both in pharmaceutical research and clinical setting. The current level of engineering pharmaceutical nanocarriers in some cases allows for drug delivery systems (DDS) to demo...
journal_title:Pharmaceutical research
pub_type: 社论
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000041449.46054.b4
更新日期:2004-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007570030368
更新日期:2000-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-008-9620-5
更新日期:2008-10-01 00:00:00
abstract::The pharmacokinetics of cefixime, a new orally active cephalosporin, was studied after an intravenous dose of 50 mg/kg to four beagle dogs. Cefixime was shown to exhibit concentration dependent serum protein binding and saturable tubular reabsorption. The drug was excreted mainly in the urine, the net result of glomer...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016309923717
更新日期:1986-06-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1600-3
更新日期:2015-06-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2018-06-25 00:00:00
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pub_type: 杂志文章
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更新日期:2020-08-05 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016254230155
更新日期:1995-07-01 00:00:00
abstract:PURPOSE:Modulating sialylation of therapeutic glycoproteins may be used to influence their clearance and systemic exposure. We studied the effect of low and high sialylated IL4-10 fusion protein (IL4-10 FP) on in vitro and in vivo bioactivity and evaluated the effect of differential sialylation on pharmacokinetic param...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2744-y
更新日期:2019-12-26 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015917023949
更新日期:1988-03-01 00:00:00
abstract::A reverse-phase HPLC method for the analysis of tryptic digests of recombinant porcine growth hormone (pGH) has been developed and validated. Digestion was performed at 4 degrees C for a 20-hr period with TPCK-treated trypsin at a 1:20 (w/w) trypsin:pGH ratio. Gradient elution HPLC, using an Aquapore RP300 C8 column, ...
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pub_type: 杂志文章
doi:10.1023/a:1018927426268
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2002-05-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012058323754
更新日期:1997-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2006-06-01 00:00:00
abstract:PURPOSE:Delivery of apoptosis-inducing compounds to hepatic stellate cells (HSC) may be an effective strategy to reverse liver fibrosis. The aim of this study was therefore to examine the selective targeting of the apoptosis-inducing drug 15-deoxy-delta12,14-prostaglandin J2 (15dPGJ2) with two different HSC-carriers: h...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9175-2
更新日期:2007-03-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016361921803
更新日期:1985-01-01 00:00:00
abstract:PURPOSE:Cisplatin, is recognized as a first line therapeutic for the treatment of non-small cell lung cancer (NSCLC). Cisplatin resistance is identified as the most detrimental complication during treatment and has been associated with upregulation of several genes, such as the anti-apoptotic gene survivin. In this stu...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2016-z
更新日期:2016-12-01 00:00:00
abstract:PURPOSE:Knowledge about the uptake mechanism and subsequent intracellular routing of non-viral gene delivery systems is important for the development of more efficient carriers. In this study we compared two established cationic polymers pDMAEMA and PEI with regard to their transfection efficiency and mechanism of cell...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9287-3
更新日期:2007-08-01 00:00:00
abstract:PURPOSE:In this study, we aimed to illustrate the utility of fractional radiofrequency (RF) that generated microchannels in the skin, allowing delivery of peptide and siRNA via the skin. The mechanisms involved in the correlation between macromolecule permeation and skin structure were also elucidated. METHODS:The mor...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1568-z
更新日期:2015-05-01 00:00:00
abstract:PURPOSE:The objective of this study is to evaluate the feasibility of using coated microneedles to deliver vaccines into the oral cavity to induce systemic and mucosal immune responses. METHOD:Microneedles were coated with sulforhodamine, ovalbumin and two HIV antigens. Coated microneedles were inserted into the inner...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1335-1
更新日期:2014-09-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9301-9
更新日期:2007-09-01 00:00:00