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目的制备缬沙坦口服定时释药片,研究体内药物动力学。方法采用溶剂挥发法制备缬沙坦/硅胶的固体分散体。采用薄膜包衣法制备定时释药片。通过释放试验考察片芯、包衣材料等主要因素对定时释药片释药时滞和释药速率的影响。以HPLC法进行定量分析。采用家犬口服定时释药片,考察体内药物动力学。结果制备的固体分散体30 min释放药物90%以上。崩解剂加入方法明显影响片芯药物释放速率,包衣液中致孔剂及含量、包衣增重为影响释药时滞和释药速率的主要因素。口服定时释药片与市售胶囊相比,AUC和C_(max)明显提高(P<0.05)。市售胶囊的t_(max)为1.89 h,口服定时释药片的t_(max)为5.67 h。结论缬沙坦口服定时释药片在体外和体内均具有定时释药特性,并能提高生物利用度。
Objective To prepare oral sustained-release tablets of valsartan and study pharmacokinetics in vivo. Methods The solid dispersion of valsartan / silica gel was prepared by solvent evaporation method. Preparation of time-release tablets by film coating method. Through the release test to examine the core, coating materials and other major factors on the release of time-lapse tablets release and delay the release rate. Quantitative analysis by HPLC method. Domestic dog oral time-release tablets, in vivo pharmacokinetics. Results The prepared solid dispersion released more than 90% of the drug for 30 min. The addition of disintegrant significantly affects the release rate of core drug, the porogen and content of coating solution, and the weight gain of coating are the main factors affecting the drug release delay and drug release rate. Compared with the commercially available capsules, the oral sustained-release tablets showed significantly higher AUC and C max (P <0.05). The t_ (max) of commercially available capsules was 1.89 h, and the t_ (max) of oral sustained-release tablets was 5.67 h. Conclusion Valsartan oral time-release tablets have the characteristics of time release in vitro and in vivo, and can improve the bioavailability.