In vitro accelerated release of triptorelin acetate microspheres and the in vivo/in vitro correlation / 国际药学研究杂志

ABSTRACT

Objective To establish an in vitro accelerated release method of triptorelin acetate microspheres with good in vi-tro/in vivo correlation(IVIVC). Methods The in vivo release of triptorelin acetate from microspheres was obtained by residual method in rats. Influences of pH value,concentration of ethanol,temperature,rotation speed and concentration of antiseptic on the in vitro accel-erated release were studied,then the correlation between in vitro accelerated release and in vivo release of the microspheres was estab-lished by adjusting the release conditions. Results The in vitro accelerated release medium of triptorelin acetate microspheres composed of 15%ethanol solution(containing 0.06%Tween 80 and 0.1%benzalkonium chloride)at 55℃with rotating rate of 200 r/min. The cumulative release of triptorelin acetate from microspheres was 87.35%at 30 h under accelerated release condition,equivalent to in vivo release for 30 days. The established in vitro accelerated release had a good correlation with that of in vivo(y=0.8845x+12.4510, R2=0.9938). Conclusion The in vitro accelerated release of triptorelin acetate microspheres could correlate well with in vivo release and has a potential application in rapid and effective evaluation of triptorelin acetate microspheres.