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目的用淀粉源介孔碳(SMC)作为载体来提高非诺贝特(FNB)的溶出速率,并结合双层渗透泵技术使药物得到控释释放,从而提高口服生物利用度。方法通过吸附法将药物FNB载入SMC的介孔孔道中制备载药体系(FNB-SMC)。通过差示扫描量热法(DSC)和粉末X射线衍射法(PXDR)对载药前后药物的存在状态进行表征。体外溶出实验考察FNB-SMC的溶出速率,并对双层渗透泵片进行优化。通过体内实验考察自制片的口服生物利用度。结果表征结果表明,FNB以无定型状态存在在SMC的介孔孔道中。体外溶出实验表明,SMC能显著提高FNB的溶出速率,并且双层渗透泵技术使药物达零级释放。体内实验表明,自制片的口服生物利用度得到明显改善。结论淀粉源介孔碳载体和双层渗透泵技术的联合防止了突释效应,明显改善FNB的口服吸收。
OBJECTIVE To improve the oral bioavailability of fenofibrate (FNB) by using starch mesoporous carbon (SMC) as carrier to improve the dissolution rate of fenofibrate (FNB) combined with double osmotic pump technology. Methods FNB-SMC was prepared by loading drug FNB into mesopore of SMC by adsorption method. The presence of drugs before and after drug loading was characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXDR). The dissolution rate of FNB-SMC was investigated in vitro and the bi-layer osmotic pump was optimized. Oral bioavailability of self-made tablets was investigated by in vivo experiments. Results The characterization results show that FNB is present in the mesoporous channel of SMC in an amorphous state. In vitro dissolution experiments showed that SMC can significantly improve the dissolution rate of FNB, and double-layer osmotic pump technology to zero drug release. In vivo experiments show that oral bioavailability of self-made tablets has been significantly improved. Conclusion The combination of starch source mesoporous carbon carrier and double osmotic pump technology prevents the burst effect and significantly improves the oral absorption of FNB.