目的 制備丹參酮II_A脂化乳，并考察丹參酮II_A脂化乳在人工胃腸液中的穩(wěn)定性，為脂化乳作為口服制劑的合理性和可行性研究提供依據(jù)。方法 制備丹參酮II_A混懸液、脂化乳、脂化乳粒。以原型藥物為對照，采用紫外分光光度法測定不同制劑中丹參酮II_A的質(zhì)量濃度。比較丹參酮II_A混懸液、脂化乳、脂化乳粒在人工胃液和人工腸液中的變化。結(jié)果 不同制劑中丹參酮II_A在人工胃液中的質(zhì)量濃度均有所降低，但脂化乳、脂化乳粒均較混懸液中丹參酮II_A質(zhì)量濃度高。在人工胃液中，3 h后混懸液中丹參酮II_A質(zhì)量濃度比脂化乳粒少11.8%、比脂化乳少33.3%。脂化乳粒、脂化乳在人工腸液中丹參酮II_A質(zhì)量濃度幾乎沒有變化，混懸液中丹參酮II_A質(zhì)量濃度有所降低，但較胃液中降低幅度有所緩和。在人工腸液中，6 h后混懸液中丹參酮II_A質(zhì)量濃度比脂化乳粒少20.3%、比脂化乳少25.8%。結(jié)論 丹參酮II_A脂化乳、脂化乳粒均能提高人工胃、腸液中所包載丹參酮II_A的穩(wěn)定性，且脂化乳效果優(yōu)于脂化乳粒，提示穩(wěn)定體系有助于進一步提高人工胃、腸液中制劑穩(wěn)定性。

Objective To prepare Tanshinone II_A Lipo-emul, and study stability of tanshinone II_A 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 II_A Suspension, Lipo-emul, and Lipo-emul Particles were prepared. Tanshinone II_A was used as model drugs, and UV spectrophotometry was used to determine concentration of tanshinone II_A in different preparations. Concentration changes of tanshinone II_A in different preparations in artificial gastrointestinal fluid were compared. Results Concentrations of tanshinone II_A in different preparations in artificial gastric juice were decreased, but concentration of tanshinone II_A in Tanshinone II_A Lipo-emul and Lipo-emul Particles were higher than those in Tanshinone II_A Suspension. In the artificial gastric juice treated for 3 h, the concentration of tanshinone II_A in Tanshinone II_A Suspension was 11.8% and 33.3%, which was less than that of Tanshinone II_A Lipo-emul Particles and Lipo-emul. The concentration of tanshinone II_A in Tanshinone II_A Lipo-emul and Lipo-emul Particles had almost no change in artificial intestinal juice, but that in Tanshinone II_A 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 II_A in Tanshinone II_A Suspension were 20.3% and 25.8% less than those of Tanshinone II_A Lipo-emul Particles and Lipo-emul. Conclusion Tanshinone II_A 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.

北京市自然科學(xué)基金項目（7132118）