Abstract:
:Leucine enkephalin (YGGFL) undergoes rapid degradation in sheep nasal mucosa to yield GGFL which is further degraded to FL. The activity of the nasal mucosal homogenate against YGGFL and GGFL (t1/2 12 and 7 min) was significantly greater than that observed with a nasal wash fluid (t1/2 40 and 13 min). The effect of cyclodextrins on the rate of degradation of FGG and YGGFL by leucine aminopeptidase (LAP) and of GGF by carboxypeptidase A (CPA) was monitored. Little effect was observed with FGG (with LAP) but the half-life of YGGFL (with LAP) was extended from approximately 44 min to approximately 75 min in the presence of a 25-fold excess of beta-cyclodextrin. The stability of GGF (with CPA) was also enhanced; an effect was observable with a 5-fold excess of cyclodextrin and the half-life could be extended by 40-75%. An equation is presented which allows the estimation of the concentration of free peptide in the peptide-cyclodextrin solutions.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Irwin WJ,Dwivedi AK,Holbrook PA,Dey MJdoi
10.1023/a:1018946829225subject
Has Abstractpub_date
1994-12-01 00:00:00pages
1698-703issue
12eissn
0724-8741issn
1573-904Xjournal_volume
11pub_type
杂志文章abstract::The conditions under which the absorption enhancer palmitoyl L-carnitine chloride (PCC) improved the bioavailability of the poorly absorbed antibiotic cefoxitin throughout the rat intestine has been studied. Cefoxitin alone was appreciably absorbed only in the duodenum (31% vs less than 7% elsewhere). PCC solutions (3...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018977021183
更新日期:1992-02-01 00:00:00
abstract::A new transdermal therapeutic system (TTS) for nitroglycerin is presented that controls release of the active substance by means of desorption and diffusion. The drug release, in the dosage range examined under sink conditions, is independent of electrolytes and pH of the aqueous acceptor medium, but it does depend on...
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:Cynarin, a potential immunosuppressant that blocks the interaction between the CD28 of T-cell receptor and CD80 of antigen presenting cells, was found in Echinacea purpurea by a new pharmaceutical screening method: After Flowing Through Immobilized Receptor (AFTIR; Dong et al., J Med Chem, 49: 1845-1854, 2006)....
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-008-9754-5
更新日期:2009-02-01 00:00:00
abstract:PURPOSE:The Caco-2 association of lectin-grafted PLGA-nanospheres was investigated compared to plain and BSA-coated spheres. METHODS:Nanospheres made from fluorescent-labeled PLGA were coated with wheat germ agglutinin (WGA) or BSA and incubated with Caco-2 monolayers varying the concentration of nanospheres, the time...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000045247.09724.26
更新日期:2004-10-01 00:00:00
abstract:PURPOSE:A patient was denoted to be generic brittle (GB) if they had a negative opinion about generics (e.g. prior history of a switch problem) or took the innovator brand of their most problematic anti-epileptic drug (AED) when generic was available. The aim of this hypothesis-generating study was to assess possible g...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-2781-6
更新日期:2020-02-26 00:00:00
abstract:PURPOSE:The acne skin is characteristic of a relatively lower pH microenvironment compared to the healthy skin. The aim of this work was to utilize such pH discrepancy as a site-specific trigger for on-demand topical adapalene delivery. METHODS:The anti-acne agent, adapalene, was encapsulated in acid-responsive polyme...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1398-z
更新日期:2014-11-01 00:00:00
abstract:PURPOSE:To quantitatively compare in vitro dissolution data in biorelevant and compendial media, to investigate whether in vitro differences are reflected in the simulated plasma profile and to specify under which circumstances prediction of the plasma profile of orally administered lipophilic drugs can be achieved. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1011071401306
更新日期:2001-03-01 00:00:00
abstract::A method to provide near-constant sustained release of high molecular weight, water-soluble proteins from polyanhydride microspheres is described. The polyanhydrides used were poly(fatty acid dimer) (PFAD), poly(sebacic acid) (PSA), and their copolymers [P(FAD-SA)]. P(FAD-SA) microspheres containing proteins of differ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018929531410
更新日期:1993-04-01 00:00:00
abstract:PURPOSE:To study the degradation of oxaliplatin in chloride media and evaluate the cytotoxicity of oxaliplatin in normal and chloride-deficient medium. METHODS:The products of the reaction of oxaliplatin with chloride were separated on a Hypercarb S column with a mobile phase containing 40% methanol in 0.05 M ammonia ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000026444.67883.83
更新日期:2004-05-01 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 purpose of this study was to investigate the delivery of itraconazole (ITZ) particles to a murine lung model by nebulization. METHODS:Three ITZ formulations were prepared and characterized in the dry state using contact angle, dissolution, X-ray powder diffraction, scanning electron microscopy, and Brunaue...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-9904-6
更新日期:2006-05-01 00:00:00
abstract:PURPOSE:To describe a computational tool to calculate molecular descriptors of potential application in ADME virtual screening of antitumor Pt(II) drug candidates. METHODS:The multistep computational procedure consists in (a) building and optimization (PM3) of the 3D structures of the investigated complexes, (b) param...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0317-1
更新日期:2011-03-01 00:00:00
abstract:PURPOSE:In vitro in vivo correlation (IVIVC) is a biopharmaceutical tool recommended for use in formulation development. When validated, IVIVC can be used to set dissolution limits and, based on the dissolution limits, as a surrogate for an in vivo study. The purpose of this paper is to study the various methods used t...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1349-8
更新日期:2014-09-01 00:00:00
abstract:PURPOSE:For determination of the transit time through various parts of the gastrointestinal (GI) tract, we developed a method that provides the location of disintegration and drug release. This method involves GI magnetomarkergraphy (GIMG) using a 129-channel Shimadzu vector biomagnetic measurement system (BMS). METHO...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章
doi:10.1023/a:1007561129221
更新日期:2000-02-01 00:00:00
abstract:PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2011-4
更新日期:2016-12-01 00:00:00
abstract:PURPOSE:The purpose of the present study is to explore whether a poly-L-arginine (poly-L-Arg)-induced increase in tight junctions (TJ) permeability of fluorescein isothiocyanate-labeled dextran (MW 4.4 kDa, FD-4) is associated with the Ca2+-dependent signaling and occurs following the phosphorylation/dephosphorylation ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000003383.86238.d1
更新日期:2003-11-01 00:00:00
abstract:PURPOSE:To examine the presence of multiplicity for the biliary excretion of xenobiotic conjugates, we studied the disposition of glycyrrhizin (GR), which has glucuronide within its molecular structure and has the ability to inhibit the biliary excretion of liquiritigenin (LG) glucuronides. METHODS:GR was administered...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016033124819
更新日期:1996-12-01 00:00:00
abstract::The pharmacokinetics of 2',3'-dideoxyinosine (ddI) were examined in rats given intravenous doses of 8, 40, or 200 mg/kg. The concentrations of ddI in whole blood and plasma were identical. The concentration decline was multiexponential, with mean half-lives of 2 and 20 min for the first and second phases, respectively...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015866714224
更新日期:1992-08-01 00:00:00
abstract:PURPOSE:The aim was to evaluate fluorescent molecular rotors (DCVJ and CCVJ), which are mainly sensitive to viscosity, for the characterization of polysorbate-containing IgG formulations and compare them to the polarity-sensitive dyes ANS, Bis-ANS and Nile Red. METHODS:IgG formulations with polysorbate 20 or 80 were s...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-009-0020-2
更新日期:2010-02-01 00:00:00
abstract::Knowledge Management (KM) is a key enabler for achieving quality in a lifecycle approach for production of biopharmaceuticals. Due to the important role that it plays towards successful implementation of Quality by Design (QbD), an analysis of KM solutions is needed. This work provides a comprehensive review of the in...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1007/s11095-016-2043-9
更新日期:2017-02-01 00:00:00
abstract::The simultaneous diffusion and metabolism of the D- and L-isomers of the aminopeptidase substrate, leucine-p-nitroanilide (LPNA), were examined in vitro in the hamster cheek pouch. L-LPNA was completely hydrolyzed during diffusion across the cheek pouch, whereas D-LPNA crossed the cheek pouch intact. The metabolic bar...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015949614437
更新日期:1989-11-01 00:00:00
abstract:PURPOSE:One of the drawbacks of polycationic and cationic liposomal gene transfer is its sensitivity to serum. Gene therapy requires the transfectant-DNA complex to be resistant to serum as well as blood. Since Ca2+ has proved to be an efficient cofactor of polycationic gene transfer, we decided to investigate its effe...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1007581700996
更新日期:2000-02-01 00:00:00
abstract:PURPOSE:1. The assessment of the role of hair follicles and sweat glands in skin resistance and percutaneous iontophoretic flux of 9-desglycinamide, 8-arginine vasopressin (DGAVP) by comparing two skin species: human stratum corneum which contained hair follicles, sweat and sebaceous glands, and shed snake skin which l...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016243706415
更新日期:1995-10-01 00:00:00
abstract:PURPOSE:Preparation of Nanographene oxide (NGO) - Gelatin hybrids for efficient treatment of Neuroblastoma. METHODS:Nanohybrids were prepared via non-covalent interactions. Spectroscopic tools have been used to discriminate the chemical states of NGO prior and after gelatin coating, with UV visible spectroscopy reveal...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-014-1604-z
更新日期:2015-06-01 00:00:00
abstract:PURPOSE:To investigate the potential of chitosan nanoparticles as a system for improving the systemic absorption of insulin following nasal instillation. METHODS:Insulin-loaded chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate anions. They were characterized for their size a...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018908705446
更新日期:1999-10-01 00:00:00
abstract:PURPOSE:Propofol is a widely used anesthetic agent with highly desirable fast "on" and "off" effects. It is currently formulated as lipid emulsions, which are known to support microbial growth. In this study, a novel, lipid-free nanodispersion formulation of propofol was characterized. METHODS:The formulation was eval...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-1872-0
更新日期:2005-03-01 00:00:00
abstract::The fluxes of nitroglycerine (NG) through human abdominal epidermis from different individuals were measured in vitro at 32°C. The mean NG flux for the entire group was 16.9 µg/cm(2) × hr, with a standard deviation of 47.7%. There are no significant differences in the means and the variances of NG fluxes between males...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/A:1016381017357
更新日期:1986-02-01 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:PURPOSE:The development of a new two-dimensional (2D) model to predict follicular permeation, with integration into a recently reported multi-scale model of transdermal permeation is presented. METHODS:The follicular pathway is modelled by diffusion in sebum. The mass transfer and partition properties of solutes in li...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2209-0
更新日期:2017-10-01 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