Morita Y, Saino H, Tojo K
Kobe Creative Center, Senju Pharmaceutical Co., Ltd., Japan.
Biol Pharm Bull. 1998 Jan;21(1):72-5. doi: 10.1248/bpb.21.72.
Ocular implants containing fluorometholone (FLM) were prepared using blends of poly (DL-lactic acid) (PLA) and polyvinyl pyrrolidone (PVP). The effect of the fraction of PVP content on the release of FLM from the implant was investigated in vitro. The drug was released from the device by approximately following first order kinetics within the period of 40 d. The release rate gradually increased with an increase in the PVP content. The in vivo study after implantation in the anterior chamber of rabbit eyes indicated that the PLA-PVP implant showed a good correlation between the in vitro and in vivo release of FLM. The present polymer blend implant demonstrated a constant level of FLM in the aqueous humor for one month.
使用聚(DL-乳酸)(PLA)和聚乙烯吡咯烷酮(PVP)的混合物制备了含有氟米龙(FLM)的眼内植入物。体外研究了PVP含量分数对FLM从植入物中释放的影响。在40天内,药物从装置中释放大致遵循一级动力学。释放速率随着PVP含量的增加而逐渐增加。在兔眼前房植入后的体内研究表明,PLA-PVP植入物在FLM的体外和体内释放之间显示出良好的相关性。目前的聚合物共混物植入物在房水中的FLM水平持续了一个月。