Jim Joseph*, Jyoti Harindran
Department of Pharmaceutical Sciences, Centre for Professional and Advanced Studies, Cheruvandoor Campus, Ettumanoor- 686631, Kottayam, Kerala, India.
*Address for Corresponding author
Department of Pharmaceutical Sciences,
Centre of Professional and Advanced Studies, Cheruvandoor Campus, Ettumanoor- 686631, Kottayam, Kerala, India
Objective: The study investigated the comparative bioavailability of Nabumetone (NBT) from binary (BSD) and ternary (TSD) solid dispersions prepared by melt method with that of the commercially available marketed tablet formulation in wistar albino rats. Materials and methods: Female Wistar albino rats (three groups with four animals in each) were selected for bioavailability (BA) study. Same sex was desired to maintain similar metabolic pattern throughout the study. Test (T1 and T2) and standard (S1) samples were suitably diluted and administered to the animals after acclimatization. Plasma samples were collected periodically from the tail vein and tested using HPLC for quantification of the active metabolite 6-methoxy-2-naphthyl acetic acid (6-MNA) upto a period of 48h. Results: Cmax , and AUC of 6-MNA were significantly increased by administration of BSD (T1), while the distribution and clearance were decreased when compared to that of marketed sample (S1). T1 was able to increase the 6-MNA bioavailability in 1.79-fold compared to 6-MNA from TSD (T2). T1 increased the 6-MNA bioavailability by 1.26-fold while comparing with S1. Conclusion: Administration of BSD (T1) increased the systemic exposure level of 6-MNA in vivo with elevated AUC, whereas, TSD (T2) decreased both. The Tmax, Vd and Cl of 6-MNA was found to be higher for T2 compared to T1 and S1, suggesting a possible distribution of 6-MNA to the high affinity synovial fluid which is the site of action in case of OA or RA. However, this has to be confirmed with further studies.
Key words: Binary and ternary solid dispersions, Nabumetone, 6-MNA, bioavailability