Amide prodrugs of NSAIDs: Synthesis and biological evaluation with a hydrolysis study
Journal Title: Scholars Academic Journal of Pharmacy - Year 2015, Vol 4, Issue 3
Abstract
The aim of the present study was to synthesize prodrugs of commonly used NSAIDs to overcome the gastrointestinal toxicity (irritation and bleeding) associated with their use. A total of six amide-based prodrugs (Ia-f) of aceclofenac, diclofenac, fenbufen, indomethacin, mefenamic acid and 4-biphenyl acetic acid were synthesized through one-pot method (single step synthesis). The structures of the synthesized prodrugs were confirmed by modern analytical techniques. The release pattern of parent drug from prodrug Ia was also studied by reverse phase HPLC method in acidic buffer (pH 1.2), phosphate buffer (pH 7.4), 80% plasma, 10% rat intestinal homogenate and 10% rat liver homogenate (pH 7.4). The prodrugs were also evaluated for their anti-inflammatory and ulcerogenic actions and compared to their corresponding parent drugs. Keywords: NSAID, Prodrug, Anti-inflammatory, Hydrolysis, Ulcerogenic.
Authors and Affiliations
Asif Husain, Priyanka Ahuja, Aftab Ahmad, Shah Alam Khan
Changes in Function and Expression Level of Multidrug Resistance-Associated Protein during Intestinal Ischemia/Reperfusion
Abstract: Ischemic bowel disease is induced by poor circulation of blood, and thus oxygen and nutrition necessary for the small intestine are not supplied enough. As a result, such condition causes inflammation and ulcer...
Development of Bio-Fertilizers and its Future Perspective
Global warming and climate change have resulted in unexpected drought, stormy rainfalls, extremely high temperature, cold damage and hurricanes in many places around the world where such disastrous tragedy had never occu...
Development and Evaluation of Polyherbal Tablet from Some Hepatoprotective Herbs
The objective of the present study was to develop and evaluate hepatoprotective polyherbal tablet because designing of oral herbal formulation is still a challenge in modern pharmaceutics and the tablet formulation prese...
Mathematical Models of Drug Dissolution: A Review
When a new solid dosage form is developed, it is very important to study drug release or dissolution. The quantitative analysis of values obtained in dissolution or release rates is easier when mathematical formulae are...
Green Chemistry Drift: A Review
Abstract: The green chemistry mutiny is furnishing an enormous number of challenges to those who practice chemistry in industry, education and research. The genesis of green chemistry recognised as a retort to the need t...