丹参酮固体分散体滴丸的工艺方法研究

Study on the technology of tanshinone solid dispersion dripping pills

目的建立测定丹参酮纯化物中丹参酮IIA和隐丹参酮含量的高效液相色谱法;设计丹参酮固体分散体滴丸制备工艺。方法采用色谱柱Agilent TC-C18柱[5μm,4.6×150 mm,流动相甲醇-水(75∶25)],流速1 mL/min,柱温25℃,检测波长270 nm,进行含量测定;以水溶性高分子材料聚乙二醇4000、PEG 6000为载体,采用溶剂-熔融法制备丹参酮固体分散体滴丸,采用正交设计优化处方,测定其体外溶出度。结果最佳制备工艺为载药比为5∶1,温度为70℃,PEG4000∶PEG 6000为1∶1,增溶剂为泊洛沙姆。结论建立了测定丹参酮的高效液相色谱方法,并应用于溶出度的测定,该方法专属性好、灵敏度高;采用溶剂-熔融法制作丹参酮固体分散体滴丸,显著提高了丹参酮的溶解度和溶出速度,该方法简便、快捷。

Objective To establish a high performance liquid chromatography determination for tanshinone IIA and cryptotanshinone content of tanshinone purification. To design the method of tanshinone solid dispersion pill preparation technology. Methods Using Agilent column TC-C18 column [5 m, 4.6×150 mm, mobile phase of methanol water （75：25）], flow rate of 1 mL/min, column temperature of 25 %, the detection wavelength of 270 nm to determinate content. The water soluble polymer materials PEG 4000 and PEG 6000 was as carrier, solvent melting method was use to prepare tanshinone solid dispersion pills, orthogonal design method was used to optimize prescription and to determinate its dissolution in vitro. Results The drug loading ratio was 5：1, the temperature was 70 ℃, PEG4000：PEG6000 was 1：1, solubilizer is poloxamer. Conclusion The establishment of high performance liquid chromatography method for the determination of tanshinone is applied to determinate dissolution, which has good specificity and high sensitivity, and conform to method of inspectiorL Solvent melting method for tanshinone solid dispersion pills can significantly improve the solubility and dissolution of tanshinone speed, which is simple and quick.