DEVELOPMENT, EVALUATION AND STABILITY OF ZOLEDRONIC ACID I.V INJECTION BY LYOPHILIZATION TECHNIQUE

The objective of the study is to develop a stable lyophilized formulation of Zoledronic acid for injection for better stability and for long term storage. The lyophilized product of all the formulations (F1- F6) prepared were an appearance of white to white Lyophilized cake. mannitol was used with water for injection . The filled vials were loaded into lyophilizer and lyophilized them as per cycle. Different composition of additives was used and the different pH concentrations of 5.7 to 6.7 were adjusted with sodium citrate were tried to formulate the formulation. The pH of all the formulations is in the range of 5.4-6.5. The related substances in formulations not exceeded the limit of 0.5%. The assay values of formulations (F1-F6) were in the range of 92% – 104 %. The formulations (F1- F6) show a water content range of 0.93% to 1.6 %. The results concluded that the formulation F4 is the optimized and the best formulation. Zoledronic acid was developed as lyophilised formulation for better stability. The obtained results suggested that a stable formulation for drug Zoledronic acid was developed which was comparable to reference listed product. Keywords: Lyophilisation, mannitol, Zoledronic acid.