Synthesis, Formulation and Analytical Method Validation of Rutin Derivative

(E-pub Ahead of Print)

Author(s): Murad Abualhasan*, Mohyeddin Assali, Nidal Jaradat, Tala Sarhan.

Journal Name: Letters in Drug Design & Discovery

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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.

Keywords: Hexaacetylated Rutin, solubility, dissolution, validation, UV/Vis spectrophotometry, antioxidant activity.

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Article Details

(E-pub Ahead of Print)
DOI: 10.2174/1570180816666181108114706
Price: $95