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目的将积雪草苷制成修饰脂质体,考察该制剂在体内的药动学过程及组织分布情况。方法 SD大鼠尾iv积雪草苷溶液及经过D-甘露糖或十八胺修饰和未经修饰的脂质体制剂,不同时间点采集大鼠血浆及组织,样品处理后采用HPLC法检测血浆与组织中的药物浓度,绘制药-时曲线,计算药动学参数,比较积雪草苷剂型间在体内药动学参数和组织分布的差异。结果积雪草苷、积雪草苷脂质体、D-甘露糖-积雪草苷脂质体、十八胺-积雪草苷脂质体4种制剂的药-时曲线均符合权重为1/C2的单室模型。积雪草苷溶液及各脂质体的消除半衰期(t1/2)分别为(14.52±0.56)、(101.35±12.47)、(149.82±20.00)、(159.58±16.46)min,药时曲线下面积(AUC)分别为(1 929.70±159.00)、(57 004.35±8 710.89)、(93 736.52±12 710.76)、(64 737.48±6 365.28)min·μg/m L。同时制成脂质体后,积雪草苷在各器官中的质量分数显著上升,在肺部的质量分数由(4.94±0.94)μg/g升至(39.12±12.04)μg/g。结论将积雪草苷制成修饰脂质体制剂后,缓释明显,并能增强靶向作用。
OBJECTIVE: The asiaticoside was made into modified liposomes and its pharmacokinetics and tissue distribution in vivo were investigated. Methods SD rat tail iv asiaticoside solution and after D-mannose or octadecylamine modified and unmodified liposome preparations were collected at different time points of rat plasma and tissue samples were processed by HPLC after plasma And the drug concentration in the tissue, the drug-time curve was drawn, the pharmacokinetic parameters were calculated, and the differences of in vivo pharmacokinetic parameters and tissue distribution between Asiaticoside formulations were compared. Results Asiaticoside, asiaticoside liposomes, D-mannose-asiaticoside liposomes, octadecylamine-asiaticoside liposomes four kinds of preparations of drug-time curve are in line with the weight of 1 / C2 single-chamber model. The half-lives (t1 / 2) of asiaticoside solution and liposomes were (14.52 ± 0.56), (101.35 ± 12.47), (149.82 ± 20.00) and (159.58 ± 16.46) min, respectively. The area under the curve (AUC) were (1 929.70 ± 159.00), (57 004.35 ± 8 710.89), (93 736.52 ± 12 710.76), (64 737.48 ± 6 365.28) min · μg / m L, respectively. At the same time, the mass fraction of asiaticoside in various organs increased significantly from 4.94 ± 0.94 μg / g to 39.12 ± 12.04 μg / g after liposome was made. Conclusion Asiaticoside modified liposome preparation made after sustained release significantly, and can enhance the targeting effect.