European Journal of Biomedical and Pharmaceutical Sciences

FORMULATION AND INVIVO EVALUATION OF METHOTREXATE HOT MELT EXTRUDES USING KOLLIDON VA 64 & PEG 1500

Satyajeet A. Narode*, Dr. P. Srinivasa Babu, Dr. M. V. Basaveswara Rao, Dr. G. Kishore Babu.

ABSTRACT

Methotrexate is an effective anticancer agent which acts by competitively inhibiting dihydrofolate reductase (DHFR). The drug belongs to BCS class II due to which the bioavailability of drug is very less. In the present investigation a total of 12 physical mixtures and hot melt extrudes of the drug is prepared using Kollidon VA 64 and PEG 1500 at various ratios. The formulations are evaluated for dissolution studies. From the % drug dissolved formulation M:Kollidon VA 64: PEG 1500 at a ratio of 1:4:0.4 is selected. The formulation is further evaluated using invivo evaluation. The plasma samples are evaluated using HPLC Agilent 1200 with PDA detector. The samples were analyzed for various kinetic parameter such as Ka, Ke, Cmax, Tmax and AUC. From the evaluation studies a significant increase in all kinetic parameters were observed. The AUC of formulation increased 6.2 folds when compared to pure drug and the Ka increased about 8 folds.

Keywords: Hot Melt Extrusion, Cmax, AUC, Invitro and Invivo evaluation.