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 of the N-glucosides of (5R)-PBG/(5S)-PBG was 2.9 for the crude liver homogenate and 3.0 +/- 0.5 for the microsomes. Magnesium was necessary for optimal activity. The Km values for formation of (5R)-PBG, (5S)-PBG, and (5R + 5S)-PBG were 1.55 +/- 0.35, 1.27 +/- 0.14, and 1.47 +/- 0.21 mM, respectively. The Vmax values for formation of (5R)-PBG, (5S)-PBG, and (5R + 5S)-PBG were 1.34 +/- 0.05 x 10(-6), 0.43 +/- 0.01 x 10(-6), and 1.77 +/- 0.04 x 10(-6) mumol/min/mg microsomal protein, respectively. It was observed that at concentrations greater than 5 mM sodium phenobarbital, inhibition of formation of phenobarbital N-glucosides occurred. The product ratio of (5R)-PBG/(5S)-PBG is comparable to that observed in the urinary excretion studies with the mouse and opposite to that observed in urinary excretion studies in humans.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Soine WH,Safi H,Westkaemper RBdoi
10.1023/a:1015889707922subject
Has Abstractpub_date
1992-05-01 00:00:00pages
613-6issue
5eissn
0724-8741issn
1573-904Xjournal_volume
9pub_type
杂志文章abstract:PURPOSE:To investigate the possible pathways for transport of wheat germ agglutinin conjugated PEG-PLA nanoparticles (WGA-NP) into the brain after nasal administration. METHODS:The nose-to-brain pathways were investigated using WGA-NP containing 6-coumarin (as a fluorescent marker) and (125)I-labeled WGA-NP. Ex vivo i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0641-0
更新日期:2012-02-01 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::Alpha- and beta-cyclodextrins and their hydroxypropyl derivatives were converted by the reaction with chlorosulfonic acid in pyridine to the corresponding sulfates. Cyclodextrin sulfates were shown by fast-atom bombardment mass spectrometry (negative ion mode, triethanolamine matrix) to be mixtures with nearly symmetr...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015854402122
更新日期:1991-09-01 00:00:00
abstract:PURPOSE:We describe the AERX aerosol delivery system, a new, bolus inhalation device that is actuated at preprogrammed values of inspiratory flow rate and inhaled volume. We report on its in vitro characterization using a particular set of conditions used in pharmacokinetic and scintigraphic studies. METHODS:Multiple ...
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
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
abstract:PURPOSE:This paper attempts to correlate the hydrophobic contribution constants (faa) of 21 amino acids in small peptides with commonly used physiochemical parameters. These faa constants can then be used to predict hydrophobicity change in peptides when any one of the amino acid residue is substituted with another. M...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1016008102587
更新日期:1996-08-01 00:00:00
abstract:PURPOSE:The purpose of this study was to evaluate glucose responsiveness in HepG2 human hepatoma cells transduced by a recombinant adeno-associated virus (rAAV) vector containing the insulin gene promoter. and to investigate the effect of protamine sulfate on rAAV-mediated gene delivery. METHODS:Recombinant AAV vector...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1010923924844
更新日期:2001-07-01 00:00:00
abstract:PURPOSE:The objective of this study was to evaluate nanoparticle uptake by the Caco-2 monolayer model in vitro. Special emphasis was placed on the localization and the quantification of the uptake of fluorescently labeled polystyrene and poly(lactic-co-glycolic acid) (PLGA) nanoparticles. METHODS:Intracellular fluores...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015393710253
更新日期:2002-05-01 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 investigate how likely two extended release formulations are to be bioequivalent when they demonstrate f2 similarity. METHOD:Dissolution profiles were simulated using the Weibull model and varying model parameters around those of a reference profile. The f2 values were calculated for the comparisons of each...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-011-0377-x
更新日期:2011-05-01 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:PURPOSE:Tissue partitioning is an important component of drug distribution and half-life. Protein binding and lipid partitioning together determine drug distribution. METHODS:Two structure-based models to predict partitioning into microsomal membranes are presented. An orientation-based model was developed using a mem...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-2085-z
更新日期:2017-03-01 00:00:00
abstract::The bioavailability of dipyridamole, a poorly soluble weak base, was evaluated in 11 healthy, older subjects (> or = 65 years), 6 with a low fasting gastric pH (control) and 5 with a fasting gastric pH > 5 (achlorhydric), in a randomized, crossover design. Subjects received 50 mg dipyridamole as a single oral dose bot...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1018918316253
更新日期:1994-01-01 00:00:00
abstract:PURPOSE:To characterize the pharmacokinetic/pharmacodynamic (PK/PD) properties of a new polyethylene glycol (PEG) conjugate formulation of interferon (IFN)-beta la following subcutaneous (SC) administration in monkeys. METHODS:Single SC injections of 0.3, 1, and 3 million international units (MIU)/kg of PEG-IFN-beta 1...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-004-9009-z
更新日期:2005-01-01 00:00:00
abstract:PURPOSE:Pulmonary antibiotic delivery is recommended as maintenance therapy for cystic fibrosis (CF) patients who experience chronic infections. However, abnormally thick and sticky mucus present in the respiratory tract of CF patients impairs mucus penetration and limits the efficacy of inhaled antibiotics. To overcom...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-016-1921-5
更新日期:2016-08-01 00:00:00
abstract:PURPOSE:Predicting human skin permeability of chemical compounds accurately and efficiently is useful for developing dermatological medicines and cosmetics. However, previous work have two problems; 1) quality of databases used, and 2) methods for prediction models. In this paper, we attempt to solve these two problems...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-015-1629-y
更新日期:2015-07-01 00:00:00
abstract:PURPOSE:To develop a new intradermal antigen delivery system by coating microneedle arrays with lipid bilayer-coated, antigen-loaded mesoporous silica nanoparticles (LB-MSN-OVA). METHODS:Synthesis of MSNs with 10-nm pores was performed and the nanoparticles were loaded with the model antigen ovalbumin (OVA), and coate...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2177-4
更新日期:2017-08-01 00:00:00
abstract:PURPOSE:We reported that suramin produced chemosensitization at nontoxic doses. This benefit was lost at the approximately 10-fold higher, maximally tolerated doses (MTD). The aim of the current study was to identify in patients the chemosensitizing suramin dose that delivers 10-50 microM plasma concentrations over 48 ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-006-0165-1
更新日期:2006-06-01 00:00:00
abstract::The aim of this investigation was to assess whether immunosuppression induced by total-body irradiation (TBI) affects the pharmacodynamics of centrally acting drugs. Female Sabra rats were exposed to a single dose of gamma irradiation (5.3 Gy). Four days later, when both the cellular and the humoral immune responses w...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1018928329824
更新日期:1994-05-01 00:00:00
abstract::Solution calorimetry has been employed to evaluate the stability constants and enthalpy changes associated with complex formation between alpha-, beta, or gamma-cyclodextrin (CD) and a group of amine compounds having the diphenylmethyl functionality. Data from thermal titrations of the compounds were analyzed using no...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1015880218535
更新日期:1991-07-01 00:00:00
abstract::Polymeric biomaterials have extensively been used in medicinal applications. However, factors that determine their biocompatibility are still not very clear. This article reviews various effects of the chemical structure and the surface properties of polymeric biomaterials on their biocompatibility, including protein ...
journal_title:Pharmaceutical research
pub_type: 杂志文章,评审
doi:10.1023/b:pham.0000036909.41843.18
更新日期:2004-08-01 00:00:00
abstract:PURPOSE:The clinical utility of anthracyclines like idarubicin (IDA) is limited by the occurrence of multidrug resistance and cardiotoxicity. Previous studies have demonstrated that the multidrug transporter P-glycoprotein (P-gp) is present in the heart and have suggested that it exerts a protective function. We sought...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1013022212738
更新日期:2001-11-01 00:00:00
abstract:PURPOSE:To devise experimental and computational models to predict aqueous drug solubility. METHODS:A simple and reliable modification of the shake flask method to a small-scale format was devised, and the intrinsic solubilities of 17 structurally diverse drugs were determined. The experimental solubility data were us...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/a:1014224900524
更新日期:2002-02-01 00:00:00
abstract:PURPOSE:Melanoma is an aggressive neoplasm with a propensity for metastases and resistance to therapy. Previously, we showed that (-)-epigallocatechin-3-gallate (EGCG), the major polyphenolic antioxidant present in green tea, resulted in a significant decrease in the viability and growth of melanoma and induction of ap...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0054-5
更新日期:2010-06-01 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:PURPOSE:This prospective study aimed to evaluate the effects of genetic polymorphisms in sulindac-related metabolizing enzyme genes including FMO3 and AOX1 on the population pharmacokinetics of sulindac in 58 pregnant women with preterm labor. METHODS:Plasma samples were collected at 1.5, 4, and 10 h after first oral ...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-020-2765-6
更新日期:2020-01-28 00:00:00
abstract:PURPOSE:The aim of this work is to design new chitosan conjugates able to self-organize in aqueous solution in the form of micrometer-size platelets. When mixed with amphotericin B deoxycholate (AmB-DOC), micro-platelets act as a drug booster allowing further improvement in AmB-DOC anti-Candida albicans activity. METH...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-017-2117-3
更新日期:2017-05-01 00:00:00
abstract:PURPOSE:The purpose of this study was to determine the potential effect of probenecid on the pharmacokinetics of zalcitabine in HIV-positive patients. METHODS:Twelve patients received single oral 1.5 mg doses of zalcitabine alone and during probenecid treatment (500 mg at 8 and 2 hours before and 4 hours after zalcita...
journal_title:Pharmaceutical research
pub_type: 临床试验,杂志文章,随机对照试验
doi:10.1023/a:1016009029536
更新日期:1996-03-01 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:PURPOSE:To examine the transport characteristics of the multidrug resistance-associated protein (MRP) substrate fluorescein across the isolated rat small intestinal segments. METHODS:The transport of fluorescein was studied in side-by-side diffusion chambers under short-circuited conditions at physiological pH. RESUL...
journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1023/b:pham.0000022410.89709.c3
更新日期:2004-04-01 00:00:00