Studies On Breviscapine Intragastric Floating Sustained Release Tablet

Breviscapine is a flavone glucuronide extracted from a Chinese herb Erigeronbreviscapinus (Vant.) Hand-Mazz. Pharmacological studies showed that breviscapinecan improve the blood flow, promote microcirculation, protect cells from oxidativedamages and so on. Clinically, it has been widely used for cardio-cerebrovasculardisease such as cerebral thrombosis, coronary heart disease and angina pectoris. Inthis research breviscapine is developed to intragastric floating sustained release tablet,which would delay the gastrointestinal residence time to improve its stability, promoteits absorption in the main absorption site, increase bioavailability of breviscapine.The analystical approach of breviscapine intragastric floating sustained releasetablet in vitro was established by HPLC to study its release rate and floating property.This methodology consideration result showed that: the specificity, precision, stability,repeatability and recovery all could meet the requirement. It was suitable for analysisof breviscapine intragastric floating sustained release tablet in vitro.The prescription of breviscapine intragastric floating sustained release tablet wasoptimized by central composite design-response surface methodology: breviscapine20mg, HPMC K4M20mg, lactose10mg, NaHCO315mg, octadecanol10mg,0.7%magnesium stearate, MCC24.3mg. The result of release rate in vitro showed that thetablets could float within5s and maintain for10h.The plasma concentration of breviscapine intragastric floating sustained releasetablet and breviscapine nomal tablet in rabbits was determined by HPLC, and thepharmacokininetics were processed by DAS2.0. The results showed that Tmaxwaslater and Cmaxwas higher than breviscapine nomal tablet, and relative bioavailabilityof breviscapine intragastric floating sustained release tablet was (152.38±12.796)%,compared with breviscapine nomal tablet. Breviscapine intragastric floating sustainedrelease tablet had a good correlation between absorption of percentage in vivo andrelease percentage in vitro(r=0.9768).