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目的比较大黄酚羟丙基-β-环糊精包合物(Chry-HP-β-CD)、聚氰基丙烯酸丁酯纳米囊(Chry-PBCA-NC)、脂质体(Chry liposomes)3种制剂的稳定性和体外溶出度,从中优选适于临床应用的最佳制剂。方法将同等剂量的3种大黄酚制剂,在热、湿和光稳定性试验中分别于0,2,5,8,10 d提取样品,观测各制剂的外观和包封率及降解率的强弱。体外溶出度试验中,采用动态透析技术在0.5,1,2,4,6,8,12,24,36,48,60,72 h不同时间点,于0.5%SDS缓冲介质中取样,以累计释放百分数为考察指标,进行比较。结果观测外观和包封率,Chry-PBCA-NC长时间放置后易挂壁,尤以Chry脂质体包封率最好。3种大黄酚制剂在热、湿稳定性条件下,其含量均无明显变化,但相对光稳定性,降解率较大,以Chry-PBCA-NC稳定性最差。体外溶出试验中,以Chry-PBCA-NC在0.5%的SDS缓冲介质中溶出最缓慢。结论综合考虑,3种大黄酚制剂中选用Chry脂质体为最佳制剂以供临床应用研究。
OBJECTIVE: To compare Chry-HP-β-CD, Chry-PBCA-NC, Chry liposomes 3 The stability of the formulation and the dissolution in vitro are optimized from which the best formulation is suitable for clinical use. Methods Three chrysophanol preparations of the same dose were extracted at 0, 2, 5, 8 and 10 d respectively in heat, humidity and light stability tests. The appearance and encapsulation efficiency and degradation rate of each preparation were observed . In in vitro dissolution test, dynamic dialysis was used to sample in 0.5% SDS buffer medium at different time points of 0.5,1,2,4,6,8,12,24,36,48,60,72 h to accumulate The percentage released is the index of investigation and compared. Results Observed the appearance and encapsulation efficiency, Chry-PBCA-NC easy to wall after being placed for a long time, especially Chry liposome encapsulation efficiency is the best. The three kinds of chrysophanol preparations under heat and humidity stability conditions, no significant changes in its content, but the relative light stability, degradation rate, the worst Chry-PBCA-NC stability. In in vitro dissolution tests, Chry-PBCA-NC was the most slowly eluted in 0.5% SDS buffer medium. Conclusion Considering the three Chrysophanol preparations, chry liposomes are the best preparation for clinical application.