摘要
目的:用淀粉源介孔碳材料(SMC)改善非诺贝特(FNB)的溶出速率,并提高其口服生物利用度。方法:以介孔二氧化硅FDU作为模板制备SMC,通过吸附法将药物FNB载入SMC介孔孔道中制备固体分散体(FNB-SMC)。采用透射电镜(TEM)观察SMC的结构。采用差示扫描量热法(DSC)和X射线衍射法(XRD)对药物在介孔孔道中的存在状态进行表征。利用溶出试验考察FNB-SMC的溶出速率。通过体内实验考察自制片和市售片在家兔体内的血药浓度变化。结果:SMC能抑制FNB的结晶度,使药物以无定型形式存在。溶出试验表明SMC显著提高了FNB的溶出速率。体内试验表明自制片的口服生物利用度明显提高。结论:固体分散体改善难溶性药物的水溶性的同时,提高了口服生物利用度。
Objective: To improve the dissolution rate and the oral bioavailability of fenofibrate (FNB) by using starch-derived mesoporous carbon materials ( SMC). Methods : FDU of mesoporous silica material was used as template for preparing SMC, and FNB was loaded into the mesopores of SMC by adsorption method to prepare solid dispersion (FNB-SMC). The structure of SMC was observed by transmission electron microscopy (TEM). The existing state of FNB in mesoporous pores was characterized by differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The dissolution rate of FNB-SMC was investigated by dissolution test. The plasma concentrations of FNB in self-made and commercial tablets were investigated by in vivo experiment in rabbits. Results: SMC could inhibit the crystallinity of FNB, and the drug existed in amorphous form. The dissolution test showed that SMC significantly increased the dissolution rate of FNB. The oral bioavailability of self-made tablets was significantly increased compared to commercial tablets. Conclusion: Solid dispersion technology can improve the water solubility of the insoluble drug. fenofibrate, and increase its oral bioavailahilitv
出处
《中国新药杂志》
CAS
CSCD
北大核心
2016年第17期2014-2020,共7页
Chinese Journal of New Drugs
关键词
非诺贝特
淀粉源介孔碳材料
固体分散体
溶出速率
生物利用度
fenofibrate
starch derived mesoporous carbon material
solid dispersion
dissolution rate
bioavailability