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Trends in Applied Sciences Research
Year: 2007  |  Volume: 2  |  Issue: 2  |  Page No.: 165 - 169

Synthesis and Physicochemical Characterization of Mutual Prodrug of Indomethacin

Surya Prakash B.N. Gupta and N.S. Hari Narayana Moorthy    

Abstract: Indomethacin, which causes gasterointestional side effect and that, may be minimized by design and development of mutual prodrugs. It involves combining two different pharmacophores with similar pharmacological activities to give synergistic action. The drug (indomethacin) was esterified with paracetamol to prepare mutual prodrug. The structure of the prodrug was confirmed on the basis of IR, 1[H] NMR, mass spectroscopy and elemental analysis. Various physicochemical properties such as solubility in water and organic solvents like chloroform, ether, acetone, methanol and ethanol and partition coefficient in octanol-water, octanol-hydrochloric acid buffer (pH 1.2) and in octanol phosphate buffer (pH 7.4) were determined. In acid pH, the mutual prodrug cannot undergo dissociation and only can undergo in intestinal pH. The mutual prodrug may have devoid of gastric irritation in GIT due to its unionized form in stomach and ionized form in intestine and may have synergic action due to two drugs are combined together. The results indicate that the prodrug dissociate in the intestinal pH because of less partition coefficient in octanol phosphate buffer.

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