Preparation Of Vildagliptin Tablets

Diabetes is caused by insulin secretion and/or functional defect of chronic metabolic disease characterized by elevating blood glucose. The current treatment is difficult to cure diabetes fundamentally. Dipeptidyl peptidase 4 inhibitor may increase the activity of endogenous glucagon-like peptide-1, increase the secretion of postprandial blood glucose,and improve the overall blood glucose of diabetic patients. Vildagliptin is the second dipeptidyl peptidase 4 inhibitor listed in China, developed by Novartis, for the treatment of type 2 diabetes.The key of the study is that whether the related substance and the dissolution behavior of vildagliptin tablets we prepared are similar to original product, and whether the tablets can be producted industrially. The quality research and quality control of vildagliptin was studied in this topic, which laid the foundation of providing the qualified API for the vildagliptin tablets. The high performance liquid chromatography methods for the dissolution test, the content uniformity and content determination to control the quality of vildagliptin tablets were established. The formulation and process were screened and compared with the original product, and the final prescription was determined. This study found that the moisture of excipients had significant influence on the stability of the vildagliptin tablets. The moisture of related excipients was controlled strictly to ensure the quality of vildagliptin tablets. According to the prescription and process parameters of the pilot production, three batches of products were produced. Results of the stability test such as the affected factor test, accelerated test, long-term test showed that the detection results of dissolution, related substances, content and enantiomers were similar to original product, indicating that the pharmaceutics had good stability and the process was easy to operate and suitable for industrial production.