Abstract:
:The influence of the jejunal bloodflow on the absorption of theophylline was investigated. The bloodflow through a segment under investigation was varied by changing the systemic blood pressure by means of a donor blood infusion into the jugular vein or by an infusion of isoprenaline or levarterenol into a femoral vein, and was measured by collecting the venous outflow from the intestinal segment. Above a bloodflow of approximately 0.40 µl/min/cm the flux/ flow ratio is reduced, and it is proposed that above this flow the intestinal epithelium provides the rate limiting step in the absorption of theophylline. When the bloodflow was held low for a prolonged time, the flux of theophylline decreased. The absorptive site bloodflow was calculated to be 18 % of the total bloodflow through the segment under investigation.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Schurgers N,de Blaey CJdoi
10.1023/A:1016374508542subject
Has Abstractpub_date
1984-01-01 00:00:00pages
23-7issue
1eissn
0724-8741issn
1573-904Xjournal_volume
1pub_type
杂志文章abstract::A two-step analytic procedure to determine the rate and extent of metabolite production following administration of the parent compound is described. The procedure provides the rate and extent of metabolite production as a function of time by application of the general model independent approach of deconvolution. The ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015951426191
更新日期:1988-06-01 00:00:00
abstract:PURPOSE:To investigate plasmid DNA interactions with liposomes prepared from dimyristoylglyceroethylphosphocholine (EDMPC) and DOPE using high sensitivity differential scanning calorimetry (HSDSC). MATERIALS AND METHODS:Large unilamellar liposomes of EDMPC with DOPE (mol ratio 0-50%) were prepared. Plasmid DNA was add...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9325-1
更新日期:2007-10-01 00:00:00
abstract:PURPOSE:Novel multidrug resistance (mdr) modulators have been proved as inhibitors of P-glycoprotein (P-gp). We first investigated the in vitro effects of selected compounds in human cancer cells on multidrug resistance reversal effects compared to drug standards and on P-gp induction to characterize the potential of t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9736-7
更新日期:2009-01-01 00:00:00
abstract:PURPOSE:Since the molecular mechanism of the cell cycle was established, various theoretical models of this process have been developed. A recent study revealed significant variability in cell cycle duration between mother and daughter cells, but this observation has not been incorporated into the theoretical models. ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-019-2570-2
更新日期:2019-02-22 00:00:00
abstract:PURPOSE:To study the biorelevant drug release from novel starch-based polyvinyl alcohol capsules (S-PVA-C). The effect of the shell material is studied by considering microstructural formulation changes during hydration. METHODS:Two different self-emulsifying systems containing either fenofibrate or probucol were fill...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1152-y
更新日期:2014-01-01 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 study the pulmonary absorption and tolerability of various formulations of the decapeptide cetrorelix acetate in rats by a new aerosol delivery system (ASTA-ADS) for intratracheal application. METHODS:Using the ASTA-ADS, cetrorelix liquid formulations (aqueous solutions for ultrasonic nebulization) were fir...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011028227155
更新日期:2001-06-01 00:00:00
abstract:PURPOSE:This study examined the rheological and textural characteristics (hardness, compressibilty, adhesiveness and cohesiveness) of bioadhesive oral gels containing the antimicrobial agent chlorhexidine. METHODS:Textural analysis was performed using a Stable Micro Systems texture analyser (model TA-XT 2) in texture ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1012091231023
更新日期:1997-04-01 00:00:00
abstract:PURPOSE:A pattern fitting procedure using X-ray powder diffraction patterns was applied to study the crystallization kinetics of amorphous griseofulvin. From the optimized parameters obtained by pattern fitting, a change in the quantity and quality of griseofulvin crystals with crystallization was also investigated. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9204-1
更新日期:2007-05-01 00:00:00
abstract:PURPOSE:Recombinant human serum albumin (rHSA), secreted by a Pichia pastoris expression system, was purified by a fast and efficient method, the essential feature of which is strong but reversible binding of the protein to Blue Sepharose. The structural characteristics, stability, and ligand-binding properties of the ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1013391001141
更新日期:2001-12-01 00:00:00
abstract:PURPOSE:Long-acting injectables (LAIs) are increasingly recognized as an effective therapeutic approach for treating chronic conditions. Many LAIs are formulated to create a poorly soluble depot from which the active agent is delivered over time. This long residing depot can cause localized chronic-active inflammation ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1308-4
更新日期:2014-08-01 00:00:00
abstract::The dermal route is an attractive route for vaccine delivery due to the easy skin accessibility and a dense network of immune cells in the skin. The development of microneedles is crucial to take advantage of the skin immunization and simultaneously to overcome problems related to vaccination by conventional needles (...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-017-2223-2
更新日期:2017-11-01 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::The pulmonary deposition and pharmacokinetics of human growth hormone (hGH), administered by aerosol and instillate, in formulations containing 99mTc-DTPA (for gamma scintigraphic imaging) have been studied in five male New Zealand White rabbits. Gamma scintigraphy indicated that the peripheral:central deposition tend...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016292232513
更新日期:1995-03-01 00:00:00
abstract:PURPOSE:Overexpression of hyaluronan (HA) receptors on cancer cells results in enhanced endocytotic uptake of the drug conjugate. An N-(2-hydroxypropyl)methacrylamide (HPMA)-HA polymeric drug delivery system was used for targeted delivery of doxorubicin to cancer cells. METHODS:HA-doxorubicin (DOX) bioconjugates (HA-D...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015170907274
更新日期:2002-04-01 00:00:00
abstract:PURPOSE:This study was conducted to investigate in vivo the impact of interferon-alpha (IFN)-alpha on P-glycoprotein (P-gp) activity in rats by studying how its administration modifies the bioavailability of digoxin, a fairly pure P-gp substrate. METHODS:Human recombinant IFN-alpha was given to rats (n = 5-7 per group...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-7415-5
更新日期:2005-11-01 00:00:00
abstract::Dihydropyridine ⇄ pyridinium salt-based brain-selective delivery systems were synthesized for the progestins, ethisterone, norethindrone, and norgestrel. After initial lipophilicity and in vitro studies indicated the feasibility of applying these compounds to brain-specific delivery, in vivo distribution studies were ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016359301852
更新日期:1986-10-01 00:00:00
abstract::Cholinesterases are ubiquitous carboxylesterase type B enzymes capable of hydrolyzing the neurotransmitter acetylcholine which are transiently expressed in multiple germline, embryonic, and tumor cells. The acute poisoning effects of various organophosphorous compounds are generally attributed to their irreversible co...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1015867021628
更新日期:1990-01-01 00:00:00
abstract::The transport characteristics of the renin inhibitor ((3S,4S)-4-[N-morpholinoacetyl-(1-naphthyl)-L-alanyl-N-methyl-(4-t hiazolyl)-L- alanyl]amino-3-hydroxy-5-cyclohexyl-1-(4-pyridyl)-1-pentanone; CH3-18) in rat small intestinal brush-border membrane vesicles (BBMV) were examined by a rapid filtration technique. The up...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018900124257
更新日期:1994-10-01 00:00:00
abstract:PURPOSE:To describe the pharmacokinetics of SK&F 107647, a synthetic hematoregulatory peptide, in healthy volunteers and in patients with adenocarcinoma. METHODS:SK&F 107647 pharmacokinetics were evaluated in 2 dose-escalation studies. Volunteers received SK&F 107647 as single 15-minute iv infusion doses of 1, 10, 100...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007512617139
更新日期:2000-04-01 00:00:00
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 chara...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015845306124
更新日期:1990-02-01 00:00:00
abstract:PURPOSE:Ultrasound can be used to release a therapeutic payload encapsulated within a perfluorocarbon (PFC) emulsion via acoustic droplet vaporization (ADV), a process whereby the PFC phase is vaporized and the agent is released. ADV-generated microbubbles have been previously used to selectively occlude blood vessels ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0277-5
更新日期:2010-12-01 00:00:00
abstract:PURPOSE:It was the aim of this study to synthesize and characterize a novel chitosan-glutathione (GSH) conjugate providing improved mucoadhesive and permeation-enhancing properties. METHODS:Mediated by carbodiimide and N-hydroxysuccinimide, glutathione was covalently attached to chitosan via the formation of an amide ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-005-6248-6
更新日期:2005-09-01 00:00:00
abstract:PURPOSE:The objective of this study was to elucidate the different mechanisms of action of different excipients on the oxidation of Met1, Met122, Met127, and Met138 in granulocyte colony-stimulating factor (G-CSF) by using hydrogen peroxide as the oxidant. METHODS:The oxidation of Met1, Met127, and Met138 was quantifi...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-9019-x
更新日期:2005-01-01 00:00:00
abstract:PURPOSE:A double-mutant E224A/E262A full-length botulinum neurotoxin (BoNT) Type A with structural similarity to native BoNT/A but lacking the endopeptidase activity provides an ideal surrogate for testing pharmacokinetics and immunochemical characteristics of BoNT. METHODS:We determined lethality (LD50) of deactivate...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1816-x
更新日期:2016-03-01 00:00:00
abstract::The effect of freezing on formation of soluble and insoluble aggregates of human growth hormone (hGH) was studied. The amount of soluble aggregates was affected very little by freezing regardless of the cooling rate. In contrast, the formation of insoluble aggregates (particulates), as determined by light scattering i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015888704365
更新日期:1991-11-01 00:00:00
abstract:PURPOSE:Highly lipophilic basic drugs, the antiestrogens AE 1 (log P = 5.82) and AE 2 (log P = 7.8) shall be delivered transdermally. METHODS:Transdermal permeation of drugs, enhancers, and solvents from various fluid formulations were characterized by in-vitro permeation studies through excised skin of hairless mice....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015314314796
更新日期:2002-05-01 00:00:00
abstract:PURPOSE:To investigate the effects of small aliphatic pendent groups conjugated through an acid-sensitive linker to the core of brushed block copolymer micelles on particle properties. METHODS:The brushed block copolymers were synthesized by conjugating five types of 2-alkanone (2-butanone, 2-hexanone, 2-octanone, 2-d...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1060-1
更新日期:2013-08-01 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:PURPOSE:We present a smart intradermal interface suitable for skin-attached drug delivery devices. Our solution enables injections or infusions that are less invasive compared to subcutaneous injections and are leakage-free at the location of penetration. METHODS:The intradermal interface is based on a 31-gauge cannul...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0319-z
更新日期:2011-03-01 00:00:00