Objective: In this study; we aimed to increase water solubility and formula dissolution
through synthesizing more soluble chemical derivative of rutin.
Significance: The synthesized rutin derivative is novel and shows an improvement in solubility and
hence possibly a better oral bioavailability. The steps followed in this study are of major benefit
which can be utilized by herbal and pharmaceutical industries to improve their products.
Method: In this study, a selective partial acetylation was performed to produce a hexaacetylated ester
of rutin. Water solubility of the synthesized hexaacetylated ester of rutin and its dissolution were
tested and compared to the original rutin. A simple UV/Vis spectrophotometric method was
developed and validated.
Results: Water solubility and dissolution profile of hexaacetylated ester derivative of rutin were
increased by approximately two folds compared to that of the original rutin. The antioxidant activity
of the synthesized derivative was comparable to original rutin. The developed analytical method was
found to be linear, accurate, precise, robust and capable of quantifying the active ingredient at low
concentration (0.0259 mg/ml).
Conclusion: An improvement in the solubility of rutin was achieved. The tablet formulation of the
partially acetylated ester derivative of rutin gives a better dissolution over the marketed rutin tablets.