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目的研究大黄酚聚氰基丙烯酸丁酯纳米囊、大黄酚羟丙基-β-环糊精包合物、大黄酚脂质体在小鼠体内组织分布的差异,通过大黄酚制剂的组织分布特性来了解剂型的药效学特性。以期选出对脑部靶向最强,药效最佳的大黄酚制剂。方法小鼠尾静脉注射同等剂量的制剂,按不同时间点取小鼠的心、肝、脾、肺、肾、脑以及血浆,经过打匀浆去蛋白处理,用高效液相色谱法检测各组织的大黄酚分布。结果三种大黄酚制剂与大黄酚单体溶液相比,均能延长在小鼠体内的消除时间,并且有较好的组织器官靶向性。结论三种大黄酚制剂的组织分布相比较,以大黄酚脂质体在各组织的分布较好,脑组织靶向最为显著。大黄酚脂质体有望成为治疗脑血管疾病临床应用的新剂型。
OBJECTIVE To study the differences of tissue distribution of chrysophanol polybutylcyanoacrylate nanocapsules, rhubarb phenols hydroxypropyl-β-cyclodextrin inclusion complex and chrysophanol liposomes in mice. Through the tissue distribution characteristics of chrysophanol preparations To understand the pharmacodynamic properties of the dosage form. In order to select the strongest brain targeting, the best pharmacological effects of chrysophanol preparations. Methods The mice were injected intravenously with the same dose of tail vein at different time points. The hearts, liver, spleen, lung, kidney, brain and plasma of mice were taken out at different time points. After being homogenized and deproteinized, the tissues were examined by high performance liquid chromatography Chrysophanol distribution. Results Compared with chrysophanol solution, all three chrysophanol preparations could prolong the elimination time in mice and had better tissue and organ targeting. Conclusion Compared with the tissue distribution of three kinds of chrysophanol preparations, the distribution of chrysophanol liposomes in each tissue is better and the brain tissue targeting is the most obvious. Chrysophanol liposome is expected to become a new type of clinical application of cerebrovascular disease.