Abstract:
:Colonic absorption of recombinant human insulin-like growth factor I (rhIGF-I) was measured in vitro using both rat and minipig colon. The permeability coefficients were 8.03 +/- 1.03 and 4.75 +/- 0.43 x 10(-8) cm sec-1 in the rat and minipig, respectively. The steady-state flux in rat colon was linearly related to the donor concentration over the range 1 to 10 mg/mL. rhIGF-I was metabolically stable in contact with both mucosal and serosal surfaces of washed colon for 5 hr. The amount of IGF-I permeating through the tissue was quantitated by radioimmunoassay and the identity and integrity of the permeating species were confirmed by reverse-phase HPLC, sodium dodecyl sulfate-polyacrylamide gel electrophoresis, and Western blotting. In all cases the permeant was identical to authentic rhIGF-I. The integrity of the colonic tissue in vitro was demonstrated by the maintenance of electrophysiological parameters, a secretory response to serosal theophylline, and the ability of sodium azide, a metabolic inhibitor, to abolish the barrier properties and cause a large increase in flux.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Quadros E,Landzert NM,LeRoy S,Gasparini F,Worosila Gdoi
10.1023/a:1018999106684subject
Has Abstractpub_date
1994-02-01 00:00:00pages
226-30issue
2eissn
0724-8741issn
1573-904Xjournal_volume
11pub_type
杂志文章abstract::A method is described for the assay of phenobarbital N-glucosylation using UDP-D-[6-3H]glucose. The radioactive phenobarbital N-glucoside conjugates [(5R)-PBG, (5S)-PBG] formed during the incubations were resolved from each other and from uncharacterized radioactive products by semipreparative HPLC. The product ratio ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015889707922
更新日期:1992-05-01 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::New generation vaccines, particularly those based on recombinant proteins and DNA, are likely to be less reactogenic than traditional vaccines but are also less immunogenic. Therefore, there is an urgent need for the development of new and improved vaccine adjuvants. Adjuvants can be broadly separated into two classes...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/a:1016104910582
更新日期:2002-06-01 00:00:00
abstract::The dose dependency of carbamazepine pharmacokinetics was characterized in rats, a common test animal for antiepileptic drug efficacy. With a randomized Latin square schedule, 5, 10, and 20 mg/kg doses of carbamazepine were injected intravenously into six Sprague-Dawley rats followed by the administration of a 5 or 10...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015872901523
更新日期:1990-05-01 00:00:00
abstract:PURPOSE:Recent studies have demonstrated the potential for a triglyceride (TG) mimetic prodrug to promote the delivery of mycophenolic acid (MPA) to the lymphatic system. Here, the metabolic pathways that facilitate the lymphatic transport of the TG prodrug (1,3-dipalmitoyl-2-mycophenoloyl glycerol, 2-MPA-TG) were exam...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1579-9
更新日期:2015-05-01 00:00:00
abstract::Semitelechelic poly[N-(2-hydroxypropyl)methacrylamide]s (ST-PHPMA) containing one amino end-group and differing in molecular weight were synthesized by radical polymerization in the presence of 2-aminoethanethiol (AET) as chain transfer agent. These polymers were covalently attached via amide bonds to the surface of n...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016247206531
更新日期:1995-05-01 00:00:00
abstract:PURPOSE:A novel photo-activated targeted chemotherapy was developed by photochemical internalization (PCI) of glutathione-sensitive polymeric micelles incorporating camptothecin (CPT) prepared from thiolated CPT (CPT-DP) and thiolated poly(ethylene glycol)-b-poly(glutamic acid) (PEG-b-P(Glu-DP)) METHODS: PEG-b-P(Glu-DP...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9712-2
更新日期:2009-01-01 00:00:00
abstract::To achieve time-controlled or site-specific drug delivery in the gastrointestinal tract, a sigmoidal release system (SRS) was developed, which achieved a prolonged lag time, followed by rapid release. The theophylline beads with a thick Eudragit RS film coating showed very low drug release in water, whereas the releas...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018910114436
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:Studies were conducted to investigate dilute solutions of the monoclonal antibody (mAb) bevacizumab, mAb fragment ranibizumab and fusion protein aflibercept, develop common procedures for formulation of low concentration mAbs and identify a stabilizing formulation for anti-VEGF mAbs for use in in vitro permeati...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-018-2368-7
更新日期:2018-02-28 00:00:00
abstract:PURPOSE:To compare the permeation characteristics of amide bond-containing HIV-1 protease inhibitors and their pyrrolinone-containing counterparts across Caco-2 cell monolayers, a model of the intestinal mucosa. METHODS:Transepithelial transport and cellular uptake of three pairs of amide bond-containing and pyrrolino...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011966918959
更新日期:1998-05-01 00:00:00
abstract::Gene delivery vectors based on adeno-associated virus (AAV) are highly promising due to several desirable features of this parent virus, including a lack of pathogenicity, efficient infection of dividing and non-dividing cells, and sustained maintenance of the viral genome. However, several problems should be addresse...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-007-9431-0
更新日期:2008-03-01 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
abstract:PURPOSE:To evaluate the effect of re-directing the uptake mechanism of polyplexes containing oligodeoxynucleotide (ODN) decoys to nuclear factor kappa B (NF-kappaB) from absorptive-mediated to receptor-mediated endocytosis. MATERIALS AND METHODS:Complexes of ODNs and a co-polymer of biotin-polyethylenglycol and polyet...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-007-9389-y
更新日期:2008-03-01 00:00:00
abstract:PURPOSE:Empirical formulae relate the mean size of primary droplets from jet and ultrasonic nebulizers to a fluid's physicochemical properties. Although the size selective "filtering" effects of baffling and evaporation may modify the secondary aerosol produced, this research sought to evaluate whether viscosity and su...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016205520044
更新日期:1995-11-01 00:00:00
abstract::The topical antifungal Sch-39304 is a racemic compound comprised of two enantiomers, Sch-42427 and Sch-42426, only one of which (Sch-42427) is pharmacologically active. The pure enantiomers have a lower melting point and, therefore, a higher solubility than the racemic compound. Because of these differences in physico...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018945618264
更新日期:1993-01-01 00:00:00
abstract:PURPOSE:To prepare acylated exenatide analogues and investigate their biological properties for guiding the development of PLGA formulations of exenatide. METHODS:The acylated exenatide analogues were prepared by reaction with glycolic acid (GA), one constitutional unit of PLGA, and characterized by HPLC-MS/MS and Cir...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1298-2
更新日期:2014-08-01 00:00:00
abstract::Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015935031933
更新日期:1990-10-01 00:00:00
abstract::Coprecipitates of fluorescein and magnesium hydroxide demonstrate delayed absorption relative to fluorescein solutions when administered to the airways of the isolated perfused rat lung (IPRL). Perfusate concentration vs time profiles showed that dissolution and not epithelial permeability was the rate-controlling fac...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015942013413
更新日期:1988-09-01 00:00:00
abstract:PURPOSE:Since the absorption of ceftriaxone (CTO) in the intestine is restricted by its natural physiological characteristics, we developed a series of small synthetic compounds derived from bile acids to promote the absorption of CTO in the gastrointestinal tract. METHODS:Several bile acid derivatives were screened b...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-012-0932-0
更新日期:2013-04-01 00:00:00
abstract::Human monocytes/macrophages (MO/MAC) were isolated from peripheral blood and cultivated on hydrophobic Teflon membranes. This culture system is suitable for HIV infection of MO/MAC in vitro. After transfer into 24-well plates the mature macrophages (infected or uninfected) were used for measurements of phagocytosis. T...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015852732512
更新日期:1992-04-01 00:00:00
abstract::The efficacy of topical formulations of acidic fibroblast growth factor (aFGF) in healing of full-thickness wounds has been studied in a diabetic db+/db+ mouse model. The effect of several formulation variables, dose, and application frequency was examined. It was found that wound healing in diabetic animals treated w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018993610801
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:This study compared gene expression profiles in mouse lungs after administration of the cationic polymers polyethyleneimine (PEI) or chitosan alone or formulated with a luciferase reporter plasmid (PEI-pLuc, chitosan-pLuc). METHODS:The polymers and formulations were administered intratracheally to Balb/c mice ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9563-7
更新日期:2006-03-01 00:00:00
abstract::The effects of process and storage conditions of solid-state emulsions were studied. Oil-in-water emulsions may be prepared from solid state emulsions by adding an aqueous phase to the solid. Solid-state emulsions are prepared by processing an oil phase and an aqueous solution of matrix material via a solvent removal ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018983227234
更新日期:1993-07-01 00:00:00
abstract:PURPOSE:Nonlinear conjugation metabolic rate of valproic acid (VPA) has been speculated previously from plasma elimination and liver concentration of VPA in guinea pigs. The purposes of the present study were to assess our speculation by direct measurement of VPA glucuronidation rate in vitro. METHODS:VPA at various c...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016028707130
更新日期:1996-08-01 00:00:00
abstract:PURPOSE:To compare the ability of alkyl-aryl isothiocyanates (ITCs) to increase the activities of the Phase 2 detoxification enzymes NAD[P]H:quinone acceptor oxidoreductase 1 (NQO1) and glutathione S-transferases (GST) in rat tissues in vivo and in cells in vitro. MATERIALS AND METHODS:Twelve alkyl-aryl ITCs and the f...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9595-2
更新日期:2008-09-01 00:00:00
abstract::The influence of varying protein and fat content in milk of New Zealand White rabbits on the milk-to-plasma drug concentration (M/P) ratio of diazepam was studied. At various time points after littering, a bolus dose (1.5 mg/kg) followed by a 26-hr infusion (1.8 mg/h) of diazepam was administered to freely moving rabb...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015809418284
更新日期:1992-10-01 00:00:00
abstract:PURPOSE:Drug transfer into milk is a general concern during lactation. Because data are limited in human subjects, particularly for new drugs, experimental animal models of lactational drug transfer are critical. This study analyzed drug transfer into milk in a mouse model, as well as the contribution of similar and di...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-013-1085-5
更新日期:2013-09-01 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::Cyclosporine (CsA) is commercially available for oral administration as a solution in olive oil with alcohol and an emulsifier. To improve its variable absorption and low patient acceptability, several oral formulations were prepared and tested in vitro and in vivo in dogs. A tablet formulation prepared by direct comp...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015815614959
更新日期:1991-04-01 00:00:00
abstract:PURPOSE:The purpose of this investigation was to determine the influence on the antimicrobial activity of cetylpyridinium chloride of the various components of the formulation of each of six candy based lozenges. METHODS:In vivo activity was investigated using six volunteers by determining the reduction in colony form...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章
doi:10.1023/a:1016002322692
更新日期:1996-04-01 00:00:00