Development of New Floating Pulsatile System for Chronotherapeutic Release

Abstract

Pulsatile drug delivery systems (PDDS) are gaining importance nowadays that delivers the drug at specific time as per the pathophysiological need of the disease resulting in improved patient therapeutic efficacy and compliance. These systems are designed according to the circadian rhythm of the body. The principle rationale for the use of pulsatile release of the drugs is where a constant drug release is not desired. A pulse has to be designed in such a way that a complete and rapid drug release is achieved after the lag time. In this PDDS, floating pulsatile concept is specifically applied to increase the gastric resistance of the dosage form having lag phase in stomach followed by a burst release in the distal small intestine which minimize the inter and intra-subject variability due to difference in gastric emptying rates with predictable gastro intestinal transit time and maximum drug absorption at maximum absorption site and ensure greater product safety. The concept of floating pulsatile beads can also be utilized to minimize the irritant effect of weakly acidic drugs on the stomach by avoiding direct contact with the mucosa and providing a mean of getting to release the drug at desired time as per the pathophysiological need of disease with low dosage. Also these floating pulsatile beads have an advantage over single unit ones as they spread out in a uniform manner over a larger surface area in the GIT and also ensure more uniform drug absorption. Indomethacin is a widely used non-steroidal anti-inflammatory drug (NSAID) most commonly for the treatment of inflammation and pain resulting from osteo and rheumatoid arthritis. It was concluded from the above reports that the objective of this work was achieved by formulation of new dual cross linked floating pulsatile beads using combined polymers (LMP and SA) has shown typical two phase release profile with 8 hours lag time followed by a rapid pulse release in distal region of small intestine and upper part of colon within 3 hours. newline