“Background: Efforts to ease administration and enhance ac

“Background: Efforts to ease administration and enhance acceptability of the oral anti-malarial artemether-lumefantrine (A-L) crushed tablet to infants and children triggered the development of a novel dispersible tablet of A-L. During early development of this new formulation, two studies were performed in healthy subjects, one to evaluate the palatability of three flavours

of A-L, and a second one to compare the bioavailability of active 4SC-202 cell line principles between the dispersible tablet and the tablet (administered crushed and intact).

Methods: Study 1 was performed in 48 healthy schoolchildren in Tanzania. Within 1 day, all subjects tasted a strawberry-, orange-and cherry-flavoured oral A-L suspension

for 10 seconds (without swallowing) in a randomized, single-blind, crossover fashion. The palatability of each formulation was rated using a visual analogue scale (VAS). Study 2 was an open, randomized crossover trial in 48 healthy adults given single doses of A-L (80 mg artemether + 480 mg lumefantrine) with food. VX-689 manufacturer The objectives were to compare the bioavailability of artemether, dihydroartemisinin (DHA) and lumefantrine between the dispersible tablet and the tablet administered crushed (primary objective) and intact (secondary objective).

Results: Study 1 showed no statistically significant difference in VAS scores between the three flavours but cherry had the highest score in several ratings (particularly for overall liking). Study 2 demonstrated that the dispersible and crushed tablets delivered bioequivalent artemether, DHA and lumefantrine systemic exposure (area under the curve [AUC]); mean +/- SD AUC(0-tlast) were 208 +/- 113 vs 195 +/- 93 h.ng/ml for artemether, 206 +/- 81 vs 199 +/- 84 h.ng/ml for DHA and 262 +/- 107 vs 291 +/- 106 h.mu g/ml for lumefantrine. Bioequivalence was selleckchem also shown for peak plasma concentrations (C(max)) of DHA and lumefantrine. Compared with the intact tablet, the dispersible tablet resulted in bioequivalent lumefantrine exposure, but AUC and C(max) values of artemether and DHA were 20-35% lower.


Considering that cherry was the preferred flavour, and that the novel A-L dispersible tablet demonstrated similar pharmacokinetic performances to the tablet administered crushed, a cherry-flavoured A-L dispersible tablet formulation was selected for further development and testing in a large efficacy and safety study in African children with malaria.”
“This work investigates the influence of some ammonium quaternary compounds as coupling agent in polyethylene/clay nanocomposites to improve the performance of polyethylene used as packaging barrier material. The 3 wt % of vermiculite used as a nanofiller was added to linear low-density polyethylene (LLDPE) and to linear low-density polyethylene grafted with maleic anhydride (LLDPE-g-MA).

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