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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 of fenofibrate (FNB) and to improve its oral bioavailability by using starch-derived mesoporous carbon material (SMC). Methods: SMC was prepared by using mesoporous silica (FDU) as a template. FNB-SMC was prepared by loading drug FNB into SMC mesopore via adsorption method. The structure of SMC was observed by transmission electron microscopy (TEM). Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were used to characterize the drug’s existence in mesopores. The dissolution rate of FNB-SMC was investigated by dissolution test. In vivo experiments to examine self-made tablets and commercially available tablets in rabbits in vivo plasma concentration changes. Results: SMC can inhibit the crystallinity of FNB and make the drug exist in amorphous form. Dissolution tests showed that SMC significantly increased the dissolution rate of FNB. In vivo tests showed that oral bioavailability of self-made tablets was significantly improved. Conclusion: The solid dispersions improve the water solubility of poorly soluble drugs and improve the oral bioavailability.