ABSTRACT
A sensitive, simple, and economic spectrophotometric method was developed and validated for the determination ofgabapentin in pure form and pharmaceutical preparations. The method is based on Schiff base condensation reaction ofthe primary amino group of gabapentin with salicylaldehyde reagent in the presence of acetate solution at 45°C for 20minutes. The obtained yellow-colored derivative in methanolic medium showed absorption maxima at 403 nm. Underthe optimum conditions, Beer’s law was obeyed in the concentration range of 6 to 100 μg/ml with correlation coefficientvalue of 0.9961. Limit of detection and limit of quantification were found to be 1.16 and 3.48 μg/ml, respectively. Thevalidity of the described method was assessed according to the International Conference on Harmonization guidelines.The mean percentage recoveries ± SD were 100.57 ± 1.5 by applying the standard addition technique. The method wasrepeatable and precise (RSD ≤ 0.61% and ≤ 1.34%, respectively) and was successfully applied for the determinationof the investigated drug in its pharmaceutical dosage form without detectable interference from the additives, hence,can be suggested for routine analysis of the gabapentin.
ABSTRACT
A sensitive, simple, and economic spectrophotometric method was developed and validated for the determination ofgabapentin in pure form and pharmaceutical preparations. The method is based on Schiff base condensation reaction ofthe primary amino group of gabapentin with salicylaldehyde reagent in the presence of acetate solution at 45°C for 20minutes. The obtained yellow-colored derivative in methanolic medium showed absorption maxima at 403 nm. Underthe optimum conditions, Beer’s law was obeyed in the concentration range of 6 to 100 μg/ml with correlation coefficientvalue of 0.9961. Limit of detection and limit of quantification were found to be 1.16 and 3.48 μg/ml, respectively. Thevalidity of the described method was assessed according to the International Conference on Harmonization guidelines.The mean percentage recoveries ± SD were 100.57 ± 1.5 by applying the standard addition technique. The method wasrepeatable and precise (RSD ≤ 0.61% and ≤ 1.34%, respectively) and was successfully applied for the determinationof the investigated drug in its pharmaceutical dosage form without detectable interference from the additives, hence,can be suggested for routine analysis of the gabapentin.
ABSTRACT
Dipeptidyl peptidase IV (DPP IV) is relatively new anti-diabetic target. DPP IV inhibitors lower fasting andpostprandial glucose concentrations by preventing the degradation of the natural hypoglycemic incretin hormones:glucose-dependent insulinotropic peptide and glucagon-like peptide-1. In this work, the high throughput dockingsoftware FRED was used as a virtual screening tool against in house built drug database to discover new DPP IVinhibitors. One of the highest ranking hits, the antihistamine drug fexofenadine, was found to inhibit recombinanthuman DPP IV in vitro with IC50 = 4.6 (±1.0) µM. The anti-diabetic effect of fexofenadine was validated in vivo byoral glucose tolerance test. These results could be helpful in the development of novel DPP IV inhibitors based onfexofenadine scaffold for the treatment of type 2 diabetes.