ABSTRACT:
Pellets have long been employed to improve the bioavailability of drugs undergoing significant first pass hepatic metabolism. Drug is an antidepressant drug. It has very strong side effect of vomiting in the dosage form, so it is necessary to developed its Sustain Release dosage form to avoiding this side effect. Chances of dose dumping were very negligible in the multiunit particulate system drug delivery system. It was under goes extensive first pass metabolism resulting in an oral bioavailability of 45 % and it shows variable absorption from GIT. Multiunit particulate oral drug delivery system offers several advantages such as rapid absorption, reducing peak plasma fluctuation and ease of administration and termination of therapy. Hence in the present work pellets of drug were prepared with the objective of avoiding first pass metabolism and controlling the release of drug for prolog period of time. Extended released pellets containing drug was prepared using an extrusion-spheronization technique. Amount of Microcrystalline cellulose (Avicel pH101), HPMC 15 cps and Eudragit NE 30D were taken as the formulation variables for optimizing to keep round shape of pellets and percentage release of drug. The pellets were evaluated for Physical characterization, Assay, Sizing, SEM, In-vitro drug release and Binder’s concentration tends to very effective pellets shape and size. Percentage release of drug tended to very non-linear with polymer type and percentage of coating on the pellets. The formulation with 0.45% HPMC, 65.94% MCC and 13% Eudragit NE 30D coating was consider as a best product with respect to perfect size and shaped pellets and In-vitro drug release study. Multiunit particulate drug delivery system gives unique release pattern, which was seen in F9I formula. This product was further subjected to stability study, the results of which indicated no significant change with respect to Shape, color, surface and in vitro drug release.