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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
    ISSN: 1573-904X
    Keywords: nonionic surfactants ; cloud point ; cloud point boosters ; poloxamers ; poloxamines ; liquid formulation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To determine the cloud point of a variety of nonionic surfactants and to search for means to raise the surfactant cloud point in liquid formulations. Methods. Cloud points of nonionic surfactants were determined visually in a water bath. Organic compounds, many of which have been used as pharmaceutical excipients, were tested initially for effect on the cloud point of poloxamine 908. Four effective cloud point boosters (CPBs) from different structural classes were further tested on additional surfactants. Results. A number of compounds can raise the cloud point of nonionic surfactants. These cloud point boosters are classified into two categories: nonionic and ionic. The nonionic CPBs include poly(ethylene glycols), propylene glycol, methanol, ethanol, isopropanol, and 2-hydroxypropyl-β-cyclodextrin. They are effective at molar concentrations. The ionic CPBs include anionic and cationic surfactants, charged phospholipids, long chain fatty acids, and bile salts. They are effective at millimolar concentrations. Conclusions. The cloud point of nonionic surfactants used in liquid formulations can be modulated through the proper choice of excipient.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1573-904X
    Keywords: nanocrystals ; submicron crystals ; suspensions ; steam sterilization ; physical stability ; surfactants ; cloud point ; ethyl diatrizoate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To study the effects of formulation variables on the physical stability of a submicron crystal (nanocrystal) suspension under steam sterilization conditions. Methods. Suspensions of ethyl diatrizoate nanocrystals were prepared by wet milling in the presence of the surfactant poloxamine 908. Particle size distribution and zeta potential were measured by photon correlation spectroscopy. Results. On heating, the mean particle size of the nanocrystal suspension remained essentially unchanged up to 110°C, the cloud point of the stabilizing surfactant, but increased significantly above that temperature. The increase in particle size was a result of particle aggregation rather than crystal growth. Adding a cloud point booster to the suspension significantly minimized the particle aggregation at high temperatures. The purity of poloxamine 908 and the tonicity agent and buffer salt used also affected the heat stability of the suspension, the latter agents apparently through altering the surfactant cloud point. Conclusions. The aggregation of the ethyl diatrizoate nanocrystalline suspension under steam sterilization conditions was a result of phase separation of the stabilizing surfactant at its cloud point. When formulated with a cloud point booster to prevent the phase-separation, the suspension maintained its physical stability under steam sterilization without any significant change in particle size distribution.
    Type of Medium: Electronic Resource
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