非诺贝特胶囊剂及家犬体内生物利用度

Fenofibrate capsules and its bioavailability on dogs

目的采用纳米分散技术制备非诺贝特胶囊剂,以提高其溶出度及生物利用度。方法用反溶剂沉淀法和高压匀质法制备非诺贝特纳米混悬剂,并通过喷雾干燥将其固化以制备胶囊剂,用差示扫描量热法(differential scanning calorimetry,DSC)和X-射线粉末衍射分析表征药物在胶囊剂中的存在状态,并测定药物的溶出度及家犬体内的生物利用度。结果非诺贝特以纳米晶体状态分散于胶囊剂中,自制胶囊溶出度为国产胶囊的3倍,相对生物利用度为国产胶囊的(274.5±15.6)%。结论自制非诺贝特胶囊剂可以通过增加非诺贝特的分散度来提高药物的溶出度与生物利用度。

Objective To prepare fenofibrate capsules using the nanosuspension technique for dissolution improvement and the bioavailability enhancement. Methods The fenofibrate nanosuspension was prepared using the method of anti-solvent precipitation technology and high pressure homogenization, then the dispersion was solidified by the method of spray drying to obtain fenofibrate capsules. The state of fenofibrate in nanosuspension was determined by using DSC and X-ray diffraction. The dissolution in vitro and bioavailability on dogs were also measured. Results Fenofibrate of preparation was existed in the forms of crystal. The dissolution of fenofibrate nanosuspension was three times higher than that of common commercial preparation. The bioavailability of self-made fenofibrate capsules was （274. 5 ± 15.6）% of common capsules. Conclusions Fenofibrate nanosuspension can improve dissolution and bioavailability with dispersibility increment.