Optimization of Site Targeted Zolmitriptan Delivery Using Polyox N12K and Methacrylic Acid

Zolmitriptan is the drug of choice for the treatment of migraine with or without aura. Oral bioavailability of drug is 40% due to high first pass metabolism. Elimination half life is 3 hrs and drug degradation occurs in acidic environment of GIT. To overcome these problems present research was aimed to prepare intestinal targeted delivery. This was prepared by compression coating technique as maximum absorption of drug occurs in small intestine. 32 factorial design was applied with independent variables polyox N12K and methacrylic acid. Core tablet consists of croscarmellose sodium as superdisintegrant, avicel as binder, dicalcium phosphate as diluent and zolmitriptan as drug. Outer coating of polyox N12K and methacrylic acid was applied in compression coating. Optimized batch F8 consist of polyox N12K (60%) & methacrylic acid (3%). In-vitro release study in simulated media indicated presence of the tablet in small intestine giving burst release. In-vivo placebo X- ray radiographic technique for F8 showed that tablet was not adhered throughout GIT and bypass stomach. This indicated F8 can be a potential to achieve the targeted site delivery.