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Comparative Study
. 2008;9(3):966-71.
doi: 10.1208/s12249-008-9131-z. Epub 2008 Aug 22.

Development and evaluation of lorazepam microemulsions for parenteral delivery

Amit A Kale  1 , Vandana B Patravale
Affiliations
Comparative Study

Development and evaluation of lorazepam microemulsions for parenteral delivery

Amit A Kale et al. AAPS PharmSciTech. 2008.

Abstract

The objective of this investigation was to develop lorazepam (LZM) microemulsions as an alternative to the conventional cosolvent based formulation. Solubility of LZM in various oils and Tween 80 was determined. The ternary diagram was plotted to identify area of microemulsion existence and a suitable composition was identified to achieve desired LZM concentration. The LZM microemulsions were evaluated for compatibility with parenteral fluids, globule size, in vitro hemolysis and stability of LZM. Capmul MCM demonstrated highest solubilizing potential for LZM and was used as an oily phase. LZM microemulsions were compatible with parenteral dilution fluids and exhibited mean globule size less than 200 nm. The in vitro hemolysis studies indicated that microemulsions were well tolerated by erythrocytes. The LZM microemulsions containing amino acids exhibited good physical and chemical stability when subjected to refrigeration for 6 months.

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Figures

Fig. 1
Fig. 1
Solubility of LZM in various oils and Tween 80 (n = 3)
Fig. 2
Fig. 2
Ternary diagram of Tween 80-Capmul MCM–Water system
Fig. 3
Fig. 3
Effect of various dilution fluids on globule size and pH of LZM microemulsion
Fig. 4
Fig. 4
Results of hemolytic studies
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