Abstract

Background: 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.

Objective: The objective was to prepare intestinal targeted delivery for Zolmitriptan which will release the drug by pulsatile effect in small intestine by retarding drug release in upper GI tract.

Method: Targeted delivery was prepared by compression coating technique. 3² factorial design was applied with independent variables polyoxN12K 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 polyoxN12K and methacrylic acid was applied in compression coating.

Results: Optimized batch F8 consist of polyoxN12K (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.

Conclusion: Study indicated F8 can be a potential to achieve the targeted site delivery for zolmitriptan.

Keywords: Chronobiology, drug delivery, lag time, migraine, pulsatile, zolmitriptan.

Graphical Abstract