Abstract:
:This paper describes a new sensitive gas chromatographic method with electron capture detector to assay estazolam in human plasma, which has been developed and validated for pharmacokinetic purposes. The drug and the internal standard (triazolam) were extracted from plasma buffered at pH 9.0 into toluene and analysed on a widebore DB 17 column. The calibration curve covered the 1.0-200 ng ml-1 range with a mean determination coefficient of 0.9996. The quantification limit was 1.0 ng ml-1. This method was used to investigate the bioequivalence of a new formulation of estazolam in drops (test) and the formulation in tablets (reference, ESILGAN). Both formulations were administered at a single dose of 2 mg in a clinical trial carried out on 24 healthy volunteers consisting of 12 males and 12 females, following a crossover randomised design in two periods with wash-out. The test and the reference formulations proved to be fully bioequivalent according to operating guidelines, namely through 90% confidence intervals in the 0.80-1.25 range.
journal_name
Pharmacol Resjournal_title
Pharmacological researchauthors
Dal Bo L,Verga F,Marzo A,La Commare P,De Vito MLdoi
10.1006/phrs.1997.0144subject
Has Abstractpub_date
1997-04-01 00:00:00pages
329-33issue
4eissn
1043-6618issn
1096-1186pii
S1043-6618(97)90144-4journal_volume
35pub_type
临床试验,杂志文章,随机对照试验abstract::Alcoholic liver disease (ALD) is a major cause of chronic liver disease worldwide that afflicts human health. With the in-depth study of the disease, its pathogenesis has gradually become clear. Although great breakthroughs have been made in the research of ALD, the research and development of drugs related to ALD has...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2019.104501
更新日期:2019-12-01 00:00:00
abstract::Antifertility activity of a triterpenoid glycoside, DSS, isolated from the root of Dalbergia saxatilis was investigated in female Wistar rats of breeding age. When administered by gastric intubation at a dose rate of 200 mg kg(-1)body weight at the premating period, conception was inhibited in 71.4% of the treated ani...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0615
更新日期:2000-05-01 00:00:00
abstract::Perfusion of all mammalian heart muscle except hamster with Ca(2+)-free Tyrode and thereafter reperfusion with normal Tyrode causes irreversible damage, the calcium paradox. Our study aims at deciphering the role of creatine kinase, high energy phosphates and Ca(2+)influx in the genesis of myocardial injury in the rat...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0595
更新日期:2000-03-01 00:00:00
abstract::Prader-Willi syndrome (PWS), the leading genetic cause of obesity, is characterized by a striking hyperphagic behavior that can lead to obesity, type-2 diabetes, cardiovascular disease and death. The molecular mechanism underlying impaired satiety in PWS is unknown. Oleoylethanolamide (OEA) is a lipid mediator involve...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.12.024
更新日期:2017-03-01 00:00:00
abstract::Advanced glycation end products (AGEs) and their receptor (RAGE) axis contributes to diabetic nephropathy. An oral hypoglycemic agent, metformin may have a potential effect on the inhibition of glycation reactions. Further, since a pathophysiological crosstalk between renin-angiotensin system (RAS) and AGEs-RAGE axis ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2011.11.001
更新日期:2012-03-01 00:00:00
abstract::Dyslipidemia and hyperglycemia are associated with an increased risk of ischemic cardiovascular disease. Positive effects of a nutraceutical combination comprising red yeast rice, berberine, policosanol, astaxanthin, coenzyme Q10 and folic acid (NComb) on plasma lipid and glucose levels have been reported in some but ...
journal_title:Pharmacological research
pub_type: 杂志文章,meta分析,评审
doi:10.1016/j.phrs.2016.04.021
更新日期:2016-08-01 00:00:00
abstract::Cosmetics are largely diffused substances topically applied to wash, to perfume or to improve the look, nevertheless the number of reported adverse reactions is very low, probably because of underreporting. This could be due to self-diagnosis and self-medication that is common in the presence of not severe reactions. ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.08.003
更新日期:2006-01-01 00:00:00
abstract::Flibanserin has been reported to be an agonist at 5-HT1A-receptors and an antagonist at 5-HT2A receptors, with higher affinity for 5-HT1A receptors. Despite the fact that less receptor occupation is required by full agonists than by antagonists to exert their effects, flibanserin was shown to exert 5-HT2A antagonism a...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0762
更新日期:2001-02-01 00:00:00
abstract::Quiescent hepatic stellate cell (HSC) activation and subsequent conversion into myofibroblasts is the central event in hepatic fibrosis pathogenesis. Epithelial-mesenchymal transition (EMT), another vital participant in liver fibrosis, has the potential to initiate HSC activation, which promotes abundant myofibroblast...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2017.10.013
更新日期:2018-02-01 00:00:00
abstract::Several factors such as proteinuria and renal fibrosis may be important in the progression of many forms of chronic renal diseases. The purposes of the current study were to investigate the progressive renal failure of the rats with surgical renal mass reduction (RMR) and the effect of the angiotensin-converting enzym...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00321-3
更新日期:2003-03-01 00:00:00
abstract::Cetyl myristoleate (CM) was reported by Diehl and May [J Pharm Sci 83 (1994) 296] to block inflammation and prevent adjuvant-induced arthritis in rats. To verify this earlier work, we have synthesized pure CM and tested its anti-arthritic properties in a collagen-induced arthritis model in DBA/1LacJ mice. Multiple int...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(02)00239-6
更新日期:2003-01-01 00:00:00
abstract::Iron is an essential element for virtually all organisms. It facilitates cell proliferation and growth but also contributes to major hallmarks of cancer such as tumor initiation, growth, and metastasis. Often, iron handling of tumor cells is disturbed, with altered iron acquisition, efflux, and storage. Targeting pert...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.03.018
更新日期:2017-06-01 00:00:00
abstract::Cicletanine [(+/-)-C] is a racemic furopyridine derivative used as an antihypertensive agent. Pharmacokinetic and metabolic studies have shown that cicletanine is rapidly and almost fully metabolized into sulfo- and glucuro-conjugated metabolites. However, the stereoselective metabolism of cicletanine is not well-know...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.2000.0660
更新日期:2000-07-01 00:00:00
abstract::Endothelial dysfunction (ED), an established response to cardiovascular risk factors, is characterized by increased levels of soluble molecules secreted by endothelial cells (EC). Evidence suggest that ED is an independent predictor of cardiac events and that it is associated with a deficiency in production or bioavai...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.01.022
更新日期:2017-05-01 00:00:00
abstract::Outbreak and pandemic of coronavirus SARS-CoV-2 in 2019/2020 will challenge global health for the future. Because a vaccine against the virus will not be available in the near future, we herein try to offer a pharmacological strategy to combat the virus. There exists a number of candidate drugs that may inhibit infect...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104859
更新日期:2020-07-01 00:00:00
abstract::The effect of flumazenil (FLU) on plasma protein binding of diazepam (DZ), nordiazepam (ND) and oxazepam (OX) was determined in plasma from drug-naive dogs to which graded concentrations of tested drugs alone and in combination were added. The results revealed that as the concentration of FLU added to plasma alone was...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80018-0
更新日期:1995-11-01 00:00:00
abstract::Curcumin, a bioactive polyphenol, is a yellow pigment of the Curcuma longa (turmeric) plant. Curcumin has many pharmacologic effects including antioxidant, anti-carcinogenic, anti-obesity, anti-angiogenic and anti-inflammatory properties. Recently, it has been found that curcumin affects lipid metabolism, and subseque...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2017.02.008
更新日期:2017-05-01 00:00:00
abstract::As a function of the structural modification of the steroid nucleus, the inhibitory interaction of 11 progesterone derivatives with human Na/K-ATPase (Na+/K(+)-transporting ATPase, EC 3.6.1.37), through C3-O-rhamnosylation, is either much decreased or weakly up to strongly increased, so that the rhamnosyl residue cont...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/s1043-6618(05)80102-1
更新日期:1991-01-01 00:00:00
abstract::A global transcriptional regulator, MgrA, was previously identified as a key determinant of virulence in Staphylococcus aureus. An 80% EtOH extract of Uncaria gambier was found to attenuate the virulence of S. aureus via its effects on MgrA. Using bioassay-guided fractionation, a polyphenolic polymer, uncariitannin, w...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.104328
更新日期:2019-09-01 00:00:00
abstract::Paradoxical sleep deprivation in rats is considered as an experimental animal model of mania endowed with face, construct, and pharmacological validity. We induced paradoxical sleep deprivation by placing rats onto a small platform surrounded by water. This procedure caused the animal to fall in the water at the onset...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.11.029
更新日期:2017-03-01 00:00:00
abstract::The effect of chloroquine and other antimalarial drugs on glutamate dehydrogenase activity was studied in liver and renal mitochondria as well as in kidney-cortex tubules of rabbit. In permeabilized mitochondria, with free access of substrates and drugs to glutamate dehydrogenase, 100 microns chloroquine decreased bot...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1996.0108
更新日期:1997-01-01 00:00:00
abstract::Antioxidants have a great potential as adjuvant therapeutics in patients with Duchenne muscular dystrophy, although systematic comparisons at pre-clinical level are limited. The present study is a head-to-head assessment, in the exercised mdx mouse model of DMD, of natural compounds, resveratrol and apocynin, and of t...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2016.02.016
更新日期:2016-04-01 00:00:00
abstract::The ataxin-2 binding protein 1 (A2BP1) gene is reported to be one of the susceptibility genes in schizophrenia, autism, and obesity. The aim of this study was to explore the association of A2BP1 gene polymorphisms with antipsychotic induced weight gain (AIWG) in Chinese Han population. Three hundred and twenty-eight p...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2015.06.003
更新日期:2015-09-01 00:00:00
abstract::The modification in the composition of bile acids in hamster by the administration of high dose of ursodeoxycholic acid (UDCA) was investigated. Male Golden Syrian hamsters were divided into five groups: a control group, two groups that received 0.5 g of UDCA per 100 g of standard diet during 30 and 60 days and anothe...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/1043-6618(90)90727-u
更新日期:1990-05-01 00:00:00
abstract::Diabetic erectile dysfunction (DED) hugely affected the patients' sexual life quality. However, there are no satisfactory therapeutic methods and intervention targets for this subtype of erectile dysfunction (ED). Inspired by the clinical practice of traditional Chinese medicine (TCM), we found that hirudin, the main ...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2020.105244
更新日期:2021-01-01 00:00:00
abstract::Pharmacokinetic of methyldopa (50 mg kg(-1)i.p.) was studied in anesthetized sham operated and sinoaortic denervated (SAD) rats by using the microdialysis technique. Vascular shunt probe was inserted into the carotid artery and concentric probe was placed in the striatum. Levels of methyldopa were measured by HPLC-EC....
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1006/phrs.1999.0610
更新日期:2000-04-01 00:00:00
abstract::Herpesviruses encode transmembrane G protein-coupled receptors (GPCRs), which share structural homology to human chemokine receptors. These viral GPCRs include KSHV-encoded ORF74, EBV-encoded BILF1, and HCMV-encoded US28, UL33, UL78 and US27. Viral GPCRs hijack various signaling pathways and cellular networks, includi...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1016/j.phrs.2020.104804
更新日期:2020-06-01 00:00:00
abstract::Sumatriptan is a 5-HT1B/D receptor agonist of documented efficacy in relieving migraine and associated symptoms such as nausea and vomiting. In the past decade, several studies reported an important delay of gastric emptying induced by sumatriptan in healthy humans. The impact of this gastric motor effect of sumatript...
journal_title:Pharmacological research
pub_type: 杂志文章,评审
doi:10.1006/phrs.2000.0766
更新日期:2001-03-01 00:00:00
abstract::A traditional Chinese medicine (TCM) formula (SL) comprising Sophorae Flos and Lonicerae Japonicae Flos was used for treating melanoma in ancient China. We have previously shown that an ethanolic extract of SL (SLE) possesses anti-melanoma effects and suppresses STAT3 signaling in vitro and in vivo. STAT3 has been lin...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2019.02.020
更新日期:2019-04-01 00:00:00
abstract::We investigated the anti-platelet effect of a newly synthesized guanidine derivative KR-32560, a sodium/hydrogen exchanger-1 (NHE-1) inhibitor, together with the elucidation of the possible mode of action. KR-32560 concentration dependently inhibited the aggregation of washed rabbit platelets induced by collagen (10 m...
journal_title:Pharmacological research
pub_type: 杂志文章
doi:10.1016/j.phrs.2005.12.003
更新日期:2006-03-01 00:00:00