Purpose: A stereoselective high performance liquid chromatographic analytical method withphotodiode array detector was developed and validated as per the International Conferenceon Harmonization (ICH) guidelines for the determination of alogliptin (ALO) enantiomers informulations and rat plasma.Methods: Enantiomeric separation was performed on a Phenomenex Lux Cellulose-2 chiralcolumn. Box-Behnken design was used to identify the optimum conditions of the threeindependent variables for the desired output responses.Results: The HPLC peaks of ALO enantiomers and the internal standard pioglitazone wereachieved before 8 min with a resolution of 0.77 min between R and S enantiomer and resolutionof more than 2.0 between each enantiomer and pioglitazone (internal) with more than 95%recovery. The linearity range and the limit of quantification of both the enantiomers in rat plasmawere 10-70 ng mL-1 and 1.2 ng mL-1 respectively.Conclusion: The developed method after validation was successfully applied for estimation ofALO enantiomers in formulations. Single oral dose of 25 mg of the ALO racemate tablets wereadministered to a group of 6 healthy rats for a comparative pharmacokinetic study of both theenantiomers.
Among the various fused heterocyclic rings, benzothiazole and its analogs have been explored broadly in search of newer therapeutic medicinal agents. The benzothiazole scaffold has been associated with huge biological potential like anticancer, antidiabetic, anti-inflammatory, antitubercular, antiviral, anti-convulsant etc. The occurrence of benzothiazole core in various compounds proves its value in the sphere of pharmaceutical chemistry. The connected research and developments in benzothiazole based chemistry become an active topic for medicinal scientists. A large number of benzothiazole and its heterocyclic derivatives are available in the market and used for the treatment as clinical drugs have been extensively used in practice to treat diverse types of ailments with high therapeutic potential. This review presents the latest therapeutic developments of benzothiazole containing compounds in the medicinal chemistry.
13 May 2025 in Naunyn-Schmiedeberg's Archives of Pharmacology