丹参酮Ⅱ_A脂化乳的制备及其稳定性研究

Preparation and stability of Tanshinone ⅡA Lipo-emul

目的制备丹参酮ⅡA脂化乳,并考察丹参酮ⅡA脂化乳在人工胃肠液中的稳定性,为脂化乳作为口服制剂的合理性和可行性研究提供依据。方法制备丹参酮ⅡA混悬液、脂化乳、脂化乳粒。以原型药物为对照,采用紫外分光光度法测定不同制剂中丹参酮ⅡA的质量浓度。比较丹参酮ⅡA混悬液、脂化乳、脂化乳粒在人工胃液和人工肠液中的变化。结果不同制剂中丹参酮ⅡA在人工胃液中的质量浓度均有所降低,但脂化乳、脂化乳粒均较混悬液中丹参酮ⅡA质量浓度高。在人工胃液中,3 h后混悬液中丹参酮ⅡA质量浓度比脂化乳粒少11.8%、比脂化乳少33.3%。脂化乳粒、脂化乳在人工肠液中丹参酮ⅡA质量浓度几乎没有变化,混悬液中丹参酮ⅡA质量浓度有所降低,但较胃液中降低幅度有所缓和。在人工肠液中,6 h后混悬液中丹参酮ⅡA质量浓度比脂化乳粒少20.3%、比脂化乳少25.8%。结论丹参酮ⅡA脂化乳、脂化乳粒均能提高人工胃、肠液中所包载丹参酮ⅡA的稳定性,且脂化乳效果优于脂化乳粒,提示稳定体系有助于进一步提高人工胃、肠液中制剂稳定性。

Objective To prepare Tanshinone ⅡA Lipo-emul, and study stability oftanshinone ⅡA in artificial gastrointestinal fluid, so as to provide the basis for study of rationality and feasibility for lipo-emul n as oral preparation. Methods Tanshinone ⅡA Suspension, Lipo-emul, and Lipo-emul Particles were prepared. Tanshinone ⅡA was used as model drugs, and UV spectrophotometry was used to determine concentration of tanshinone ⅡA in different preparations. Concentration changes of tanshinone ⅡA in different preparations in artificial gastrointestinal fluid were compared. Results Concentrations of tanshinone ⅡA in different preparations in artificial gastric juice were decreased, but concentration of tanshinone ⅡA in Tanshinone ⅡA Lipo-emul and Lipo-emul Particles were higher than those in Tanshinone ⅡA Suspension. In the artificial gastric juice treated for 3 h, the concentration of tanshinone ⅡA in Tanshinone ⅡA Suspension was 11.8% and 33.3%, which was less than that of Tanshinone ⅡA Lipo-emul Particles and Lipo-emul. The concentration of tanshinone ⅡA in Tanshinone ⅡA Lipo-emul and Lipo-emul Particles had almost no change in artificial intestinal juice, but that in Tanshinone ⅡA Suspension was decreased, however, the extent of decrease was shorter than those in gastric juice. In artificial intestinal juice treated for 6 h, the concentrations of tanshinone ⅡA in Tanshinone ⅡA Suspension were 20.3% and 25.8% less than those of Tanshinone ⅡA Lipo-emul Particles and Lipo-emul. Conclusion Tanshinone ⅡA Lipo-emul Particles and Lipo-emul both can improve the stability of loaded-drugs in the artificial gastrointestinal fluid, and the stability of Lipo-Emul is better than that of Lipo-Emul particles, which suggests that stability of the system is helpful to further enhance the stability of preparation in artificial gastrointestinal fluid.