复方丹参片剂与黏附微丸体外释放对比研究

Studies on differences between Fufang Danshen tablets and Fufang Danshen adhesion pellets release in vitro

关键词:  复方丹参黏附微丸  复方丹参片  体外溶出

Key words:  Fufang Danshen adhesion pellets  Fufang Danshen tablets  release in vitro

摘要:

[目的] 建立复方丹参黏附微丸中三七皂苷R1、人参皂苷Rg1、人参皂苷Rb1、人参皂苷Rd及丹酚酸B、丹参酮ⅡA 6种成分的含量测定方法并以6种成分为指标比较复方丹参片和复方丹参黏附微丸体外溶出度差异。[方法] 采用挤出滚圆法制成复方丹参黏附微丸。溶出介质为pH6.8的磷酸盐缓冲液，转篮法测定6种成分的体外溶出度，比较复方丹参片与黏附微丸体外溶出速率及累积溶出量。[结果] 三七皂苷R1（丸剂4.02%，片剂2.19%）；人参皂苷Rg1（丸剂22.31%，片剂8.73%）；人参皂苷Rb1（丸剂14.33%，片剂7.69%）；人参皂苷Rd（丸剂3.29%，片剂1.56%）；丹酚酸B（丸剂17.41%，片剂21.70%）；丹参酮ⅡA（丸剂0.34%，片剂1.17%）。溶出结果显示120 min内复方丹参片中6种成分累计溶出度基本能达到90%，相比之下黏附微丸各成分释放缓慢持久，720 min在人工肠液中仍有释放。[结论] 从体外溶出实验结果分析，较复方丹参片，复方丹参黏附微丸在体内停留时间长，释放速度缓慢持久，延长药物作用时间，可实现药物在体内达到缓释的效果。

Abstract:

[Objective] Establish an HPLC method to determinate salviaacidB,tanshinoneⅡA and four panaxsapoins:Notoginsenoside R1, ginsenoside Rg1,ginsenoside Rd,ginsenoside Rb1in FufangDanshen adhesion pellets. Meanwhile, compare release difference of the two dosage form in vitro.[Methods] The pellets of compound salvia miltiorrhiza were prepared by extrusion-spheronization method. The dissolution rate of the six components in vitro and the dissolution rate and cumulative dissolution rate of compound Danshen Tablets and adhesive pellets were compared by using the phosphate buffer solution with pH6.8.[Results] Content of notoginsenoside R1 in Fufang Danshen adhesion pellets and Fufang Danshen tablets was 4.02% and 2.19%, ginsenoside Rg1 was 22.31% and 8.73%; ginsenoside Rb1 was 14.33% and 7.69%; ginsenoside Rd was 3.29% and 1.56%; salviaacid B was 17.41% and 21.70%; tanshinone ⅡA was 0.34% and 1.17%. The dissolution results showed that the total dissolution rate of the six components in the compound Danshen tablets can reach 90% within 120min, compared with the sustained release of the components of the pellets, and release in the release medium.[Conclusion] Compared with compound Danshen tablets and Compound Danshen Adhesive Pellets, the retention time in vivo is long, the release rate is slow and prolonged, and the drug action time can be prolonged, which indicated pellets can be sustained release in vivo.