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  • pharmacokinetics  (6)
  • acid site concentration  (2)
  • cloud point  (2)
  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and bioavailability of oral and intramuscular artemether (1997)
    Springer
    European journal of clinical pharmacology 52 (1997), S. 307-310 
    Details
    ISSN: 1432-1041
    Keywords: Key words Artemether ; Thai males; malaria ; dihydroartemisinin ; pharmacokinetics ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Objective: The pharmacokinetics and bioavailability of artemether and dihydroartemisinin were investigated in eight Thai males following the administration of single oral and intramuscular doses of artemether (300 mg) in a randomized two-way cross-over study. Results: Both oral and intramuscular artemether were well-tolerated. In most cases, artemether and dihydroartemisinin were detected in plasma after 30 min and declined to levels below the limit of detection within 18–24 h. Compared with intramuscular administration, oral administration of artemether resulted in a relatively rapid but incomplete absorption [Cmax: 474 vs 540 ng · ml−1; t max: 2.0 vs 3.9 h; AUC: 2.17 vs 5.20 μg · h · ml−1]. Geographic means of lag-time and absorption half-life (t 1/2a) of oral vs intramuscular artemether were 0.28 and 1.1 h vs 0.30 and 2 h, respectively. t 1/2z was significantly shortened after the oral dose [2.8 vs 6.9 h]. Mean oral bioavailability relative to intramuscular administration was 43.2%. The ratio of the AUCs of artemether to dihydroartemisinin was significantly lower after the oral than after the intramuscular dose (geometric mean: 0.29 vs 0.60).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002280050295
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  • 2
    Electronic Resource
    Electronic Resource
    Paracetamol disposition in Thai patients during and after treatment of falciparum malaria (1995)
    Springer
    European journal of clinical pharmacology 48 (1995), S. 65-69 
    Details
    ISSN: 1432-1041
    Keywords: Paracetamol ; Malaria ; pharmacokinetics ; phase II conjugation ; glucuronidation ; sulphation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Investigations in animals have suggested that conjugation of paracetamol may be reduced in malaria. We have measured plasma concentrations and the urinary excretion of paracetamol and its phase II metabolites in eight Thai patients during uncomplicated falciparum malaria and in convalescence, following a 1000 mg single oral dose. The apparent oral clearance (Malaria, 3.6; Convalescence, 3.9; ml·min−1·kg−1), the elimination half-life (Malaria, 3.8; Convalescence, 3.7 h) and apparent volume of distribution (Malaria, 1.2; Convalescence, 1.2; l·kg−1) of paracetamol were similar during malaria and convalescence. In addition, the urinary excretion of paracetamol and its major phase II metabolites and their formation clearances from paracetamol were not significantly different between the two study phases. These data show that clinical malaria infection has no effect on the conjugation of paracetamol in man.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00202175
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  • 3
    Electronic Resource
    Electronic Resource
    Effect of ampicillin on mefloquine pharmacokinetics in thai males (1991)
    Springer
    European journal of clinical pharmacology 40 (1991), S. 631-633 
    Details
    ISSN: 1432-1041
    Keywords: Mefloquine ; ampicillin ; Thai subjects ; pharmacokinetics ; enterohepatic recycling ; drug interaction ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of a single oral dose of mefloquine given either alone or with ampicillin has been studied in 8 healthy Thai male volunteers. There was a significantly higher maximum whole blood mefloquine concentration after coadministration with ampicillin (1648 vs 1228 ng·ml−1), as well as a significantly reduced terminal half life (15.3 vs 17.7 days), mean residence time (20.1 vs 23.4 days) and volume of distribution at steady state (14.1 vs 19.4 l·kg−1). Although there was no significant change in the AUC from zero time to infinity, the AUC from zero time to 5 days was significantly increased by ampicillin (4.86 vs 3.27 μg·ml−1 day). These changes in mefloquine disposition after antibiotic treatment may be due both to an increase in fractional bioavailability and a reduction in the enterohepatic recycling of mefloquine.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00279985
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  • 4
    Electronic Resource
    Electronic Resource
    Effect of tetracycline on mefloquine pharmacokinetics in Thai males (1992)
    Springer
    European journal of clinical pharmacology 43 (1992), S. 567-569 
    Details
    ISSN: 1432-1041
    Keywords: Mefloquine ; Tetracycline ; Thai subjects ; Thai subjects ; drug interaction ; pharmacokinetics ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of a single oral dose of mefloquine given either alone or with tetracycline has been studied in 20 healthy Thai male volunteers. There was a significantly higher maximum whole blood mefloquine concentration after coadministration with tetracycline (1600 vs 1160 ng · ml−1), as well as a significantly reduced terminal half-life (14.4 vs 19.3 days), mean residence time (11.9 vs 16.0 days) and volume of distribution at steady state (13.3 vs 19.91 · kg−1). Although there was no significant change in the AUC from zero time to infinity, the AUC from zero time to 7 days was significantly increased by tetracycline (6.18 vs 4.76 μg · ml−1 · day). The changes in mefloquine disposition after tetracycline treatment are probably due to a reduction in enterohepatic recycling. The initial increase in mefloquine AUC without an apparent increase in side-effects suggests that this combination may have a place in the treatment of multi-drug resistant falciparum malaria.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02285105
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  • 5
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of quinine in patients with chronic renal failure (1996)
    Springer
    European journal of clinical pharmacology 49 (1996), S. 497-501 
    Details
    ISSN: 1432-1041
    Keywords: Quinine ; Malaria ; pharmacokinetics ; chronic renal failure
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract Methods: We investigated the pharmacokinetics of quinine (Qn) following administration of a single oral dose of 600 mg Qn sulphate in six male Thai patients with a moderate degree of chronic renal failure (CRF), and six male Thai subjects with normal renal function. Results: The drug was well tolerated in both groups of subjects; no major adverse reactions were observed. A marked alteration in the pharmacokinetics of Qn was found in patients with CRF compared to healthy subjects; there were six signifiicant changes in the pharmacokinetic parameters. Absorption was delayed, but increased in CRF (tmax 4.5 vs 1.6 h, Cmax 6.17 vs 3.45 μg·ml−1). Total clearance was significantly reduced 0.94 vs 2.84 ml·min−1·kg−1, whereas Vz/f remained unchanged (1.82 vs 2.78 1·kg−1). This resulted in the increased values of AUC and prolongation of the t1/2z and MRT in the patients (AUC 181.5 vs 61.8 μg·min−1·ml−1, t1/2z 26 vs 9.7 h, MRT 36.4 vs 11.3 h). Median concentrations of plasma unbound fraction of Qn collected at 4 h after drug administration in patients and healthy subjects were 7.3 vs 9.8%, respectively.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00195937
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  • 6
    Electronic Resource
    Electronic Resource
    Pharmacokinetics of mefloquine in the presence of primaquine (1992)
    Springer
    European journal of clinical pharmacology 42 (1992), S. 559-560 
    Details
    ISSN: 1432-1041
    Keywords: Mefloquine ; Thai subjects ; pharmacokinetics ; Primaquine ; drug interaction ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00314870
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  • 7
    Electronic Resource
    Electronic Resource
    Cloud Point of Nonionic Surfactants: Modulation with Pharmaceutical Excipients (1999)
    Springer
    Pharmaceutical research 16 (1999), S. 562-568 
    Details
    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
    URL: http://dx.doi.org/10.1023/A:1018831415131
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  • 8
    Electronic Resource
    Electronic Resource
    Physical Stability of Ethyl Diatrizoate Nanocrystalline Suspension in Steam Sterilization (1999)
    Springer
    Pharmaceutical research 16 (1999), S. 569-574 
    Details
    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
    URL: http://dx.doi.org/10.1023/A:1018883431970
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  • 9
    Electronic Resource
    Electronic Resource
    Skeletal isomerization of 1-butene over mesoporous materials (1999)
    Springer
    Catalysis letters 57 (1999), S. 209-215 
    Details
    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
    URL: http://dx.doi.org/10.1023/A:1019028522765
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  • 10
    Electronic Resource
    Electronic Resource
    Influence of the fluorine loading level on the skeletal isomerization of 1-butene over fluorine-modified alumina (1998)
    Springer
    Catalysis letters 51 (1998), S. 101-107 
    Details
    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
    URL: http://dx.doi.org/10.1023/A:1019037017971
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