Abstract：
:Nonstereospecific studies have indicated that the pharmacokinetics of propranolol (PR) are altered in inflammatory conditions such as arthritis. However, as the kinetics and dynamics of PR are stereoselective, we examined the effect of adjuvant arthritis (AA) on the disposition of the individual enantiomers. A novel normal-phase stereospecific HPLC assay for PR was developed involving chiral derivatization with S-(naphthyl)ethyl isocyanate and fluorescence detection. Oral and iv doses of racemic PR were administered to control and AA rats (n = 6). AA had no significant effect on either clearance or S:R ratio after iv doses. On the other hand, after oral doses, clearance was significantly decreased in AA. Although significant for both enantiomers, this effect was more pronounced on the less active R-enantiomer. The AUC R:S ratio was, therefore, significantly altered (AA, 14 +/- 3.0; control, 4.3 +/- 1.2). Increased total (S+R) plasma concentrations of PR in AA, possibly due to a reduced intrinsic clearance, therefore, reflect mainly increased concentrations of the less active R-enantiomer.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Piquette-Miller M,Jamali Fdoi
10.1023/a:1018907431893subject
Has Abstractpub_date
1993-02-01 00:00:00pages
294-9issue
2eissn
0724-8741issn
1573-904Xjournal_volume
10pub_type
杂志文章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：:Fibers were spun by the downward configuration of the wet spinning technique. This configuration is capable of encapsulating nonspherical and/or coarse particles. We examined encapsulation of propranolol hydrochloride and the ability of the fibers to act as a sustained-release delivery system for propranolol hydrochlo...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015982521706
更新日期：1989-12-01 00:00:00
abstract：PURPOSE:This study aimed to assess impact of different vehicles for laser-assisted skin drug delivery. We also tried to uncover the mechanisms by which different vehicles affect laser-aided skin permeation. METHODS:Full-surface ablative (conventional) and fractional lasers were used to irradiate nude mouse skin. Imiqu...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-013-1167-4
更新日期：2014-02-01 00:00:00
abstract：:Using brine shrimp lethality to direct fractionation, extracts of the bark of Annona bullata Rich. (Annonaceae) have yielded 16 alpha-hydroxy-(-)-kauranoic acid as a bioactive plant constituent. This previously known diterpene showed significant (ED50 8.25 x 10(-2) micrograms/ml) and selective cytotoxicity against A-5...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015819422479
更新日期：1990-04-01 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：PURPOSE:Design of intravaginal rings (IVRs) for delivery of antiretrovirals is often guided by in vitro release under sink conditions, based on the assumption that in vivo release will follow a similar release profile. METHODS:We conducted a dose-ranging study in the female reproductive tract of pigtail macaques using...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-017-2224-1
更新日期：2017-10-01 00:00:00
abstract：PURPOSE:Drug particle physical properties are critical for the efficiency of a drug delivered to the lung. The purpose of this study was to produce ultrafine sumatriptan succinate particles for inhalation. METHODS:Sumatriptan succinate particles were produced via reactive precipitation without any surfactants. Several...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9586-3
更新日期：2008-09-01 00:00:00
abstract：PURPOSE:To elucidate the catalytic mechanism of the esterase-like activity of serum albumin (SA), the reactivity of SA from six species was investigated using p-nitrophenyl esters as model substrates. METHODS:The effect of pH and the energetic and thermodynamic profiles of SA were determined for all species for p-nitr...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/b:pham.0000016241.84630.06
更新日期：2004-02-01 00:00:00
abstract：PURPOSE:To investigate the ability of various polymers to inhibit the crystallization of amorphous felodipine from amorphous molecular dispersions in the presence of absorbed moisture. METHODS:Spin coated films of felodipine with poly(vinylpyrrolidone) (PVP), hydroxypropylmethylcellulose acetate succinate (HPMCAS) and...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-007-9331-3
更新日期：2008-04-01 00:00:00
abstract：PURPOSE:To examine the inhibitory potential of enalapril [and other angiotensin converting enzyme (ACE) inhibitors] on glycylsarcosine (GlySar) transport by the high-affinity renal peptide transporter. METHODS:Studies were performed in rabbit renal brush border membrane vesicles in which the uptake of radiolabeled Gly...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018847818766
更新日期：1999-05-01 00:00:00
abstract：PURPOSE:To investigate the properties of phenylboronic acid-functional poly(amido amine) polymers (BA-PAA) in forming multilayered thin films with poly(vinyl alcohol) (PVA) and chondroitin sulfate (ChS), and to evaluate their compatibility with COS-7 cells. METHODS:Copolymers of phenylboronic acid-functional poly(amid...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-015-1688-0
更新日期：2015-09-01 00:00:00
abstract：PURPOSE:This study focuses on the formulation optimization, in vitro and in vivo performance of differently sized nano-crystalline liquid suspensions and spray-dried powders of a poorly soluble BCS class II compound i.e. Danazol. METHODS:A DoE approach was utilized to optimize stabilizer concentration and formulate da...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-014-1567-0
更新日期：2015-05-01 00:00:00
abstract：PURPOSE:Typical methods to study pMDI sprays employ particle sizing or visible light diagnostics, which suffer in regions of high spray density. X-ray techniques can be applied to pharmaceutical sprays to obtain information unattainable by conventional particle sizing and light-based techniques. METHODS:We present a t...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1869-5
更新日期：2016-05-01 00:00:00
abstract：PURPOSE:To investigate whether conjunctival epithelial cells express transport processes for opioid peptides. METHODS:We monitored the uptake of [(3)H]deltorphin II and [(3)H]DADLE, two hydrolysis-resistant synthetic opioid peptides, in the rabbit conjunctival epithelial cell line CJVE and elucidated the characteristi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-008-9709-x
更新日期：2009-05-01 00:00:00
abstract：PURPOSE:To synthesize a trifluorinated bile acid that can be used for (19)F magnetic resonance imaging (MRI) of bile acid enterohepatic circulation, characterize its in vitro transporter affinity, stability, and (19)F-MRI signal, and assess its ability to concentrate in the gallbladder of C57BL/6 mice. METHODS:Target ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0963-6
更新日期：2013-05-01 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: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：PURPOSE:The purpose of the study is to characterize glycine crystallization during freezing of aqueous solutions as a function of the glycine salt form (i.e., neutral glycine, glycine hydrochloride, and sodium glycinate), pH, and ionic strength. METHODS:Crystallization was studied by thermal analysis, microscopy, x-ra...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1016223101872
更新日期：1995-10-01 00:00:00
abstract：PURPOSE:Doxorubicin was chemically conjugated to a terminal end group of poly(D,L-lactic-co-glycolic acid) [PLGA] and the doxorubicin-PLGA conjugate was formulated into nanoparticles to sustain the release of doxorubicin. METHODS:A hydroxyl terminal group of PLGA was activated by p-nitrophenyl chloroformate and reacte...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1018908421434
更新日期：1999-07-01 00:00:00
abstract：PURPOSE:It was the purpose of this study to develop a new oral drug delivery system for low molecular weight heparin (LMWH) providing an improved bioavailability and a prolonged therapeutic effect. METHODS:The permeation enhancing polycarbophil-cysteine conjugate (PCP-Cys) used in this study displayed 111.4 +/- 6.4 mi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1023803706746
更新日期：2003-06-01 00:00:00
abstract：:Chemical enhancers and vehicles were tested for their ability to improve the percutaneous absorption of leuprolide, a nonapeptide (luteinizing hormone releasing hormone analogue; MW 1209.4). In vitro permeabilities in nude mouse, snake, and cadaver skin were evaluated in either Franz diffusion cells or a Bronaugh flow...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015860324161
更新日期：1992-12-01 00:00:00
abstract：PURPOSE:The combination of morphine and gabapentin seems promising for the treatment of postoperative and neuropathic pain. Despite the well characterised pharmacodynamic interaction, little is known about possible pharmacokinetic interactions. The aim of this study was to evaluate whether co-administration of the two ...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-016-1988-z
更新日期：2016-11-01 00:00:00
abstract：:A new magnetic microsphere carrier has been formulated that may localize drugs by both biochemical and physical means. The microspheres, prepared from the polysaccharide chitosan, are designed to bind to anionic glycosaminoglycan receptors on the surface of capillary endothelial cells. The microspheres were formulated...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/a:1015978704810
更新日期：1988-05-01 00:00:00
abstract：PURPOSE:To explore whether miR-19 is involved in the regulation of multidrug resistance (MDR), one of the main causes of breast cancer mortality, and modulates sensitivity of tumor cells to chemotherapeutic agents. METHODS:We analyzed miRNA expression levels in three MDR cell lines in comparison with their parent cell...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0570-y
更新日期：2011-12-01 00:00:00
abstract：PURPOSE:To explore the application of scanning ion occlusion sensing (SIOS) as a novel technology for characterization of nanoparticles. METHODS:Liposomes were employed as model nanoparticles. The size distribution of the liposomes was measured by both SIOS and dynamic light scattering (DLS). Particle number concentra...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-012-0788-3
更新日期：2012-09-01 00:00:00
abstract：PURPOSE:Myricetin (MYR) flavonoid is well-recognized for its antioxidant, anti-inflammatory and anti-tumor potential. Introducing nanomedicine was the ultimate resort to solve the imperfections of this nutraceutical, namely solubility, stability and delivery issues. The study, thus, aims at developing inhalable micropa...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-020-02794-z
更新日期：2020-04-14 00:00:00
abstract：:The delivery of therapeutic nucleic acids to neurons has the potential to treat neurological disease and spinal cord injury. While select viral vectors have shown promise as gene carriers to neurons, their potential as therapeutic agents is limited by their toxicity and immunogenicity, their broad tropism, and the cos...
journal_title：Pharmaceutical research
pub_type： 杂志文章,评审
doi：10.1007/s11095-007-9439-5
更新日期：2008-05-01 00:00:00
abstract：:Knowledge of comparative solubility profiles of a base and its hydrochloride salt is important in selecting one form over the other for dosage form design. The studies with two model bases, namely, tiaramide and papaverine, showed that, except during phase transition from a base to a salt or vice versa, the pH-solubil...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1023/A:1016382426347
更新日期：1985-03-01 00:00:00
abstract：PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respi...
journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-011-0553-z
更新日期：2012-01-01 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
