Development and evaluation of artemether parenteral microemulsion

青蒿醚注射用微乳剂的研制与评价

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Abstract

The objective of the present investigation was to develop a parenteral microemulsion delivering artemether, a hydrophobic antimalarial drug and to evaluate antimalarial activity of the microemulsion in comparison to the marketed oily injection of artemether (Larither(®)). The microemulsion was evaluated for various parameters such as globule size, ability to withstand centrifugation and freeze-thaw cycling and effect of sterilization method on the drug content and globule size. The in vivo antimalarial activity of the microemulsion was evaluated in P. berghei infected mice in comparison to the Larither(;). The stability of the microemulsion was evaluated at 5º for 1 month. The microemulsion exhibited globule size of 113 nm and it could successfully withstand centrifugation and freeze-thaw cycling. The method of sterilization did not have any significant effect on the artemether content and globule size of the microemulsion. The microemulsion showed around 1.5-fold higher antimalarial activity and higher survival as compared to that of marketed artemether injection Larither(®) and it showed a good stability at the end of 1 month.

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