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  • 1
    ISSN: 1432-1041
    Keywords: Key words Pharmacokinetics ; Bioequivalence ; Mefloquine ; Uncomplicated falciparum malaria ; Dihydroartemisinin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Objective: To assess the pharmacokinetics and relative bioavailability/bioequivalence of three commercial tablet formulations of mefloquine, i.e. Lariam (reference formulation), Mephaquin 100 Lactab and Eloquin-250, when given sequentially after dihydroartemisinin in Thai patients with acute uncomplicated falciparum malaria. Methods: Twenty-nine Thai patients with acute uncomplicated falciparum malaria were randomised to receive an initial dose of 300 mg dihydroartemisinin, followed by 1250 mg mefloquine (at 24 h and 30 h after dihydroartemisinin) given as either Lariam (n=10 cases), Mephaquin (n=9 cases) or Eloquin-250 (n=10 cases). Serial blood samples were obtained up to day 42 after treatment with mefloquine. Mefloquine concentrations were determined in whole blood by means of ultraviolet high-performance liquid chromatography. The pharmacokinetic parameters of mefloquine were estimated using non-compartmental and compartmental analysis. Results: The three combination regimens were well tolerated. Patients in all treatment groups had a rapid initial response. However, nine patients (four and five cases in regimen containing Mephaquin 100 Lactab and Eloquin-250, respectively) had reappearance of parasitaemia during the follow-up period. Mefloquine from the three formulations showed significantly different pharmacokinetic and bioavailability metrics. Significantly lower peak plasma concentrations (Cmax) and areas under the plasma concentration–time curve (AUC; AUC0–48h, AUC0–7days, and total AUC) were observed with Mephaquin 100 Lactab than with the other two formulations. Mean values for relative bioavailability of the test to standard products were 49.1% (Mephaquin 100 Lactab) and 72.4% (Eloquine-250). Based on the criteria set, the bioavailability of the two test products (Mephaquin 100 Lactab and Eloquine-250) was considered non-equivalent to the reference product with respect to the rate (tmax, Cmax) and extent (AUC0–48h, AUC0–7days, total AUC) of mefloquine absorption.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 53 (1998), S. 375-376 
    ISSN: 1432-1041
    Keywords: Key words Artesunate ; Dihydroartemisinin ; Pharmacokinetics ; Bioequivalence
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Catalysis letters 57 (1999), S. 209-215 
    ISSN: 1572-879X
    Keywords: 1-butene ; skeletal isomerization ; mesoporous material ; acid site concentration ; monomolecular reaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract On the skeletal isomerization of 1-butene, mesoporous materials with mesopores too large to expect any shape selectivity have been used in order to investigate the effects of the concentration of acid sites on the conversion of 1-butene and the selectivity for isobutene. The concentrations of acid sites can be varied through the control of the Si/Al ratio. The conversion of 1-butene increases with increasing the aluminium content of mesoporous materials, while the selectivity for isobutene decreases. The results of ammonia TPD, IR measurement of 1-butene adsorption, and TG analysis of used catalysts indicate that distant location of activated 1-butene molecules induces the monomolecular reaction over the mesoporous materials with low aluminium content, resulting in high selectivity for skeletal isomerization. On the mesoporous material with high aluminium content, however, the high concentration of activated 1-butene molecules accelerates the multimolecular oligomerization and, thus, reduces the selectivity.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1572-879X
    Keywords: 1-butene ; skeletal isomerization ; fluorine-modified alumina ; acid site concentration ; monomolecular reaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract γ-alumina catalysts modified with different weight loadings of fluorine have been used for skeletal isomerization of 1-butene in order to investigate the effects of the fluorine loading level on the conversion of 1-butene and the selectivity to isobutene formation. Increasing the actual loading of fluorine up to 0.012 wt% led to an increase in conversion of 1-butene over fluorine-modified γ-alumina catalysts, while the high selectivity to isobutene remains almost unchanged. On the other hand, a clear trend of increasing 1-butene conversion with a decreasing selectivity to isobutene is observed for the γ-alumina catalysts with higher loadings of fluorine. An analysis of the results from the thermal analysis, NH3 temperature-programmed desorption, infrared and the 1-butene sorption measurments clearly indicates that the number of strong acid sites in the modified γ-alumina catalysts is greatly enhanced at fluorine loadings higher than 0.012 wt%, leading to the acceleration of 1-butene oligomerization followed by cracking to light hydrocarbons. Therefore, the 1-butene isomerization selectivity from fluorine-modified γ-alumina catalysts can be understood in terms of a competition between the monomolecular and bimolecular reaction pathways, which highly depend on the concentration of strong acid sites.
    Type of Medium: Electronic Resource
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