双嘧达莫片剂的制备及家犬体内的生物利用

Preparation and bioavailability of dipyridamole tablets

目的制备双嘧达莫片剂并研究该片剂生物利用度。方法采用超声沉淀法结合高压均质技术制备粒径为300 nm双嘧达莫纳米混悬剂,以喷雾干燥法对其进行固化,用扫描电镜(scanning e-lectron microscope,SEM)观察粒子形态,差示扫描热分析法(differential scanning calorimetry,DSC),X射线衍射(X-ray diffraction analysis,XRD)和红外光谱法分析喷干粉末中药物的存在状态和与稳定剂之间相互作用。通过粉末直接压片法制备双嘧达莫片剂,并与市售普通片相比较,测定双嘧达莫片剂相对生物利用度。结果药物以晶体形式存在于片剂中,且溶出度显著提高,相对生物利用度为185%。结论采用纳米技术分散双嘧达莫后,所制备的片剂能够提高药物在家犬体内的生物利用度。

Objective To prepare dipyridamole tablets in nanotechnology and study its bioavailability. Methods The nanosuspensions were prepared using precipitation-ultrasonication method and high pressure homogenization. The liquid nanosuspensions were solidified by spray drier. SEM （ scanning electron microscope） was used to observe its morphology character, DSC（ differential scanning calorimetry） and XRD （X-ray diffraction analysis） were applied to study its crystalline form, and IR was carried out to analyze the interaction between drugs and its stabilizer. Moreover, the tablets were prepared by direct compression technology, and its bioavailability was study by pharmacokinetic experiments on 3 dogs. Results The preparation remained to be the same crystal form as the raw material but with low crystallinity, and the dissolution rate of dipyridamole tablets was obviously improved. The relative bioavailability of test tablets was 185%. Conclusions The bioavailabilities of dipyridamole tablets in dogs are improved by using nanotechnology.