Bioavailability Study of Ondansetron Gel in Rabbits and Human Volunteers Appling Uplc as Analytical Tool and Evaluation of the Antiemetic Effect of Ondansetron Gel in Cisplatin-Induced Emesis in Rats

Abstract

Objective: This study was undertaken to determine the bioavailability of ondansetron gel in experimental animals and humans applying UPLC as an analytical tool and evaluation of the antiemetic effect of ondansetron gel in cisplatin-induced emesis in rats.
 Methods: Ondansetron gel (F13: sodium alginate 7% w/w) was used, marketed I. V. ondansetron (Zofran) ® was chosen as reference. The bioavailability study in rabbits was selected as a parallel design using nine healthy rabbits divided into three groups whereas, bioavailability study in humans was an open-label, wherein 6 healthy subjects administered ondansetron gel. The potential effect of ondansetron gel was evaluated for the prevention of different phases of emesis motivated by exposure to antineoplastic drugs (cisplatin) by determination of body weight loss, water and food intake applying kaolin-pica model in rats using seventy-two rats divided into six groups.
 Results: Ondansetron gel (0.5%) showed detectable plasma concentration 22.833±2.17 ng/m1 after ¼ h and 419.55±2.17 ng/ml after 1-h post-treatment in rabbits and human respectively and concentration was maintained above-reported minimum effective concentration for more than 2.5 h for rabbits and 7 h for humans compared to 1.75 h after I. V. administration.
 The ondansetron gel significantly reduces all phases of cisplatin-induced emesis and a decrease in body weight, water, and food consumption was significantly attenuated.
 Conclusion: Based on the high efficacy of gel on emesis induced by cisplatin, and its high bioavailability, transdermal ondansetron gel could be a promising convenient system to prevent nausea and vomiting following administration of antineoplastic drugs.

AN ELECTROMETRIC METHOD FOR THE DETERMINATION OF IMPACT OF DMSO-WATER MIXTURES ON pKa VALUES OF SALICYLIC ACID DERIVATIVES

“…The half-integral values of both ligands confirm that they have three dissociable protons, 5-SSA has three dissociable protons and exists as LH2 -, LH 2and L 3and 5-HSA has three dissociable protons and they exist as LH3, LH2and LH 2 . The kurtosis values says that the system possess platykurtic.…”

“…The poor solubility of the drug may result in limited absorption, further leading to the decrease in bioavailability [1]. Measurement of drug concentration in biological fluids, such as blood or urine, following drug administration, is considered a direct and efficient method for the determination of systemic drug bioavailability [2]. Drug disposition means the change in the position of drug molecules after administration into the system.…”