SATURABLE TRANSPORT SYSTEM FOR VILDAGLIPTIN AT THE LEVEL OF INTESTINAL MEMBRANE IN RABBITS
Ahmed M. Elmeniar1, Mohamed A. Osman2, Sanaa A. El-Gizawy2, Yusuf A. Haggag2
1Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science& Technology, Egypt.
2Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt.
Vildagliptin is approved for the treatment of type II diabetes in adults. The study utilized in situ rabbit intestinal perfusion technique to investigate the existence of saturable transport system for vildagliptin across rabbit intestinal membrane from duodenum and ascending colon. The results reflected significant changes in the membrane transport parameters of vildagliptin when increasing dose by tenfold compared with perfusion of the drug as normal daily dose. This change depended on the site of absorption as the absorptive clearance decreasing significantly in case of the colon without a significant change in case of duodenum. This is indicating for existence of saturable transport system for vildagliptin across intestinal membrane. The amino acid transporters in the intestine may be responsible for the somewhat diminished and delayed absorption of vildagliptin.
June 2022