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Pandey P, Pandey S, Dubey S. Mutual Amide Prodrug of Etodolac-glucosamine: Synthesis, Characterization and Pharmacological Screening. Indian J Pharm Sci. 2013;75(4):406-12doi: 10.4103/0250-474X.119813.
Pandey, P., Pandey, S., & Dubey, S. (2013). Mutual Amide Prodrug of Etodolac-glucosamine: Synthesis, Characterization and Pharmacological Screening. Indian journal of pharmaceutical sciences, 75(4), 406-12. https://doi.org/10.4103/0250-474X.119813
Pandey, Preeti, et al. "Mutual Amide Prodrug of Etodolac-glucosamine: Synthesis, Characterization and Pharmacological Screening." Indian journal of pharmaceutical sciences vol. 75,4 (2013): 406-12. doi: https://doi.org/10.4103/0250-474X.119813
Pandey P, Pandey S, Dubey S. Mutual Amide Prodrug of Etodolac-glucosamine: Synthesis, Characterization and Pharmacological Screening. Indian J Pharm Sci. 2013 Jul;75(4):406-12. doi: 10.4103/0250-474X.119813. PMID: 24302794; PMCID: PMC3831721.
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Indian J Pharm Sci. 2013 Jul;75(4):406-12. doi: 10.4103/0250-474X.119813.

Mutual Amide Prodrug of Etodolac-glucosamine: Synthesis, Characterization and Pharmacological Screening.

Indian journal of pharmaceutical sciences

Preeti Pandey, S Pandey, Shaifali Dubey

Affiliations

  1. Institute of Pharmacy, Pranveer Singh Institute of Technology, Bhauti, NH-2, Kanpur-209 305, India.

PMID: 24302794 PMCID: PMC3831721 DOI: 10.4103/0250-474X.119813

Abstract

Etodolac, a nonsteroidal antiinflammatory drug, widely used in arthritis is associated with gastric ulceration and irritation due to presence of free carboxylic group. The current investigation reports synthesis of mutual amide prodrug of etodolac by masking free carboxylic group with glucosamine, a nutritional supplement for treatment of arthritis. Confirmation and characterization of the structure of the synthesized prodrug done by elemental and spectroscopy analysis, melting point, determination of migration parameters (Rf, RM, and Rt) by using thin layer chromatography and high performance liquid chromatography, respectively. Partition coefficient and solubility study confirms its lipophilic character so can be suitable candidate for controlled release delivery. In vitro hydrolytic studies of prodrug confirms good rate of hydrolysis in blood plasma, fecal matter, and simulated intestinal fluid while stable in gastric simulated fluid. In vivo pharmacological screening performed on animals. Prodrug with respect to etodolac shows good analgesic, antiinflammatory, and antiarthritic activity. The prodrug was assessed for their probable damaging effects by ulcerogeniticity and histopathological analysis. The histopathological studies showed less ulceration in the gastric region when treated with prodrug, thereby proving the prodrug to be better in action as compared to etodolac and are advantageous in having less gastrointestinal side effects.

Keywords: Mutual amide prodrug; chemical and pharmacological characterization; etodolac; glucosamine

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