Abstract:
BACKGROUND:Meclofenoxate hydrochloride is a psychostimulant in the nootropic agent group available in capsule and tablet formulations approved for traumatic cataphora, alcoholic poisoning, anoxia neonatorum, and children's enuresis in China. Although these 2 generic formulations are marketed in China, information regarding their pharmacokinetics and bioequivalence in humans has not been published. OBJECTIVE:The aim of this study was to compare the pharmacokinetic properties and bioequivalence of the capsule (test) and tablet (reference) formulations of meclofenoxate hydrochloride 200 mg in healthy Chinese volunteers. METHODS:This single-dose, randomized-sequence, open-label, 2-period crossover study was performed at the Nanjing First Hospital of Nanjing Medical University, Nanjing, China. Eligible subjects were healthy male volunteers who were randomly assigned at a 1:1 ratio to receive a single 200-mg dose of the test or reference formulation, followed by a 1-week washout period and administration of the alternate formulation. The study drugs were administered after a 12-hour overnight fast. As a prodrug, meclofenoxate is hydrolyzed into 4-chlorophenoxyacetic acid and is not detected in plasma. The active metabolite of meclofenoxate, chlorophenoxyacetic acid, was assayed using a high-performance liquid chromatography method. For analysis of pharmacokinetic properties, including Cmax, AUC0-24, and AUC0-infinity, blood samples were obtained at 0.33, 0.67, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 14, and 24 hours after administration. The formulations were considered bioequivalent if the log-transformed ratios of Cmax and AUC were within the predetermined equivalence range (80%-125%) as established by the US Food and Drug Administration (FDA). Subjects were interviewed concerning the occurrence of adverse events including excitement, insomnia, lassitude, and headache. Tolerability was assessed at baseline (before administration) and at 1, 2, 6, and 12 hours after administration by monitoring vital signs and laboratory tests (hematology, blood biochemistry, hepatic function, and urinalysis). RESULTS:Twenty-four Chinese male subjects (mean [range]age,23.5[22-30]years;weight,63.3[56-68]kg; height, 171 [165-184] cm) were enrolled; all completed the study. No period or sequence effect was observed. The 90% CIs for the log-transformed ratios of chlorophenoxyacetic acid Cmax, AUC0-24, and AUC0-infinity were 95.7 to 122.9, 97.6 to 111.9, and 97.8 to 111.7, respectively (all, P>0.05). Similar results were found for the data without log-transformation. No adverse events were reported or observed during this single-dose study. CONCLUSIONS:In this small study in healthy Chinese adult male volunteers, a single 200-mg dose of the capsule formulation was found to be bioequivalent to a single 200-mg dose of the tablet formulation based on the US FDA's regulatory definition (rate and extent of absorption). Both formulations were well tolerated.
journal_name
Clin Therjournal_title
Clinical therapeuticsauthors
Zou JJ,Ji HJ,Wu DW,Yao J,Hu Q,Xiao DW,Wang GJdoi
10.1016/j.clinthera.2008.09.013subject
Has Abstractpub_date
2008-09-01 00:00:00pages
1651-7issue
9eissn
0149-2918issn
1879-114Xpii
S0149-2918(08)00306-8journal_volume
30pub_type
杂志文章,随机对照试验abstract::This study was designed to determine changes in the number of beta-adrenergic receptors of circulating lymphocytes in patients with varying degrees of congestive heart failure. Thirty-seven patients with congestive heart failure were classified into four groups according to the functional classifications of the New Yo...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
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abstract:PURPOSE:Interruptions in opioid use have the potential to cause pain relapse and withdrawal symptoms. The objectives of this study were to observe patterns of opioid interruption during acute illness in nursing home residents and examine associations between interruptions and pain and withdrawal symptoms. METHODS:Pati...
journal_title:Clinical therapeutics
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journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2013.06.011
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abstract:PURPOSE:Coadministration of morphine with oral gabapentin has been shown to increase plasma gabapentin concentrations. This study evaluated whether there was any interaction between gabapentin enacarbil (GEn), which is a prodrug of gabapentin, and morphine in terms of pharmacokinetics, pharmacodynamics, safety, and tol...
journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2014.10.015
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abstract::Oral rehydration therapy (ORT) has had a dramatic global impact. The worldwide consequences of this therapy are discussed in four categories: (1) adoption of ORT as the primary therapy for acute dehydrating diarrhea; (2) establishment of national ORT programs; (3) scientific knowledge gained from studies into intestin...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:
更新日期:1990-01-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验,收录出版
doi:10.1016/s0149-2918(04)90177-4
更新日期:2004-07-01 00:00:00
abstract::Flumazenil is a new drug indicated for the reversal of the sedative effects of benzodiazepines mediated at the benzodiazepine-receptor site. Worldwide sources to date have disclosed 43 cases of seizures related, at least temporally, to the intravenous administration of flumazenil. There was no apparent relationship be...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:
更新日期:1992-03-01 00:00:00
abstract:PURPOSE:The effect of peripheral arterial disease (PAD) among young and middle-aged adults can be significant, but no previous study has examined the prognosis and the associated health care cost of the disease in this population. We evaluated the clinical and economic burden of PAD in patients from a large claims data...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2014.06.013
更新日期:2014-08-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:10.1016/s0149-2918(03)80320-x
更新日期:2003-10-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,meta分析
doi:10.1016/S0149-2918(00)88479-9
更新日期:2000-02-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2017.12.001
更新日期:2018-01-01 00:00:00
abstract::Hyaluronic acid is the most abundant mucopolysaccharide in connective tissue. Because of its high viscous elasticity, it lubricates joints and can hold cells together in the intercellular spaces in connective tissue. The administration of exogenous hyaluronic acid can increase the repair potential of damaged tissue. A...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:
更新日期:1989-11-01 00:00:00
abstract::To determine the cost relative to efficacy and tolerability of two antimicrobial regimens, a prospective, multicenter study compared imipenem-cilastatin (I-C) monotherapy with clindamycin+aminoglycoside (C+A) in the treatment of serious lower respiratory, intra-abdominal, gynecologic, and urinary tract infections. The...
journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,多中心研究,随机对照试验
doi:
更新日期:1992-01-01 00:00:00
abstract:PURPOSE:The effect of posaconazole, a strong cytochrome P450 3A (CYP3A) inhibitor and commonly used antifungal agent, on the pharmacokinetic properties of venetoclax, a CYP3A substrate, was evaluated in patients with acute myeloid leukemia to determine the dose adjustments needed to manage this potential interaction. ...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2017.01.003
更新日期:2017-02-01 00:00:00
abstract:BACKGROUND:In this era of evidence-based medicine, clinicians require a comprehensive range of well-designed studies to support prescribing decisions and patient management. In recent years, data from observational studies have become an increasingly important source of evidence because of improvements in observational...
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pub_type: 杂志文章,评审
doi:10.1016/j.clinthera.2007.07.004
更新日期:2007-06-01 00:00:00
abstract:OBJECTIVE:The goal of this health economic analysis was to asses the cost-effectiveness of a fixed combination of aspirin plus extended-release dipyridamole (ASA/ER-DP) or clopidogrel compared with ASA monotherapy for prevention of recurrent ischemic stroke. BACKGROUND:The second European Stroke Prevention Study (ASA/...
journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/S0149-2918(00)80041-7
更新日期:2000-03-01 00:00:00
abstract::Ketoprofen is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid family with demonstrated efficacy in the treatment of rheumatoid arthritis and osteoarthritis; a distinguished safety profile; and good tolerability. This report describes a new extended-release formulation that maintains therapeutic pla...
journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
doi:
更新日期:1994-03-01 00:00:00
abstract:BACKGROUND:Vitamin B12 (cobalamin) deficiency may be caused by inadequate dietary intake of B12 or by conditions that result in malabsorption of the vitamin. Crystalline vitamin B12, usually in the form of cyanocobalamin, is administered parenterally (ie, intramuscularly) or orally for treating deficiency states. Intra...
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pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2011.05.088
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journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章
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pub_type: 杂志文章
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2009.07.020
更新日期:2009-07-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
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更新日期:2020-03-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1997-09-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章
doi:10.1016/j.clinthera.2005.05.007
更新日期:2005-05-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:2004-05-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
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更新日期:2013-08-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
doi:10.1016/j.clinthera.2007.04.013
更新日期:2007-04-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,评审
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更新日期:1999-10-01 00:00:00
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journal_title:Clinical therapeutics
pub_type: 杂志文章,随机对照试验
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更新日期:2009-09-01 00:00:00