朱辰奇　顾依　周琴　刘馨 沈惠明 陈志鹏

摘要 目的：利用聚多巴胺（PDA）对丹参注射液中多成分进行负载，构建丹参注射液（SMI）缓释制剂（PDA-SMI）。方法：建立丹参注射液的原儿茶醛、迷迭香酸和丹酚酸B3种成分的分析方法并进行含量测定;制备PDA，在pH值2.5的条件下对SMI进行负载，制备PDA-SMI;对PDA-SMI体外释放行为进行考察。结果：SMI中原儿茶醛、迷迭香酸、丹酚酸B的浓度分别为0.344、0.214、0.262 mg/mL;PDA-SMI对原儿茶醛、迷迭香酸、丹酚酸B的载药量分别为8.59%，15.90%和20.57%;PDA-SMI中原儿茶醛、迷迭香酸、丹酚酸B体外累计释放率分别为84.05%，77.57%和63.12%。结论：PDA可以负载SMI的多种成分，载药量较高，并具有良好的缓释效应。

关键词 丹参注射液;聚多巴胺;缓释制剂;高效液相色谱法

Study on Preparation of Danshen Injection Sustained-release Preparation Using Polydopamine

ZHU Chenqi1，2，GU Yi2，ZHOU Qin1，LIU Xin1，SHEN Huiming1，CHEN Zhipeng2

（1 Department of Pharmacy，Suzhou Hospital Affiliated to Nanjing Medical University，Suzhou 215002，China; 2 School of Pharmacy，Nanjing University of Chinese Medicine，Nanjing 210023，China）

Abstract Objective：To use polydopamine（PDA）to carry out multiple components of Salvia miltiorrhiza injection，and to construct a slow-release preparation of Salvia miltiorrhiza injection（SMI）（PDA-SMI）.Methods：Establish the analysis method of the three components of protocatechuic aldehyde，rosmarinic acid and salvianolic acid B of Salvia miltiorrhiza injection and determine the content; prepare PDA，load SMI under the condition of pH 2.5 to prepare PDA-SMI; The in vitro release behavior of PDA-SMI was investigated.Results：The concentrations of protocatechuic aldehyde，rosmarinic acid and salvianolic acid B in SMI were 0.344，0.214 and 0.262 mg/mL，respectively; the loading of protocatechuic aldehyde，rosmarinic acid and salvianolic acid B by PDA-SMI The doses were 8.59%，15.90% and 20.57% respectively; the cumulative release rates of protocatechuic aldehyde，rosmarinic acid and salvianolic acid B in PDA-SMI were 84.05%，77.57% and 63.12%，respectively.Conclusion：PDA can load multiple components of SMI and has a good sustained-release effect.

Keywords Salvia miltiorrhiza injection; Polydopamine; Sustained-release preparation; High performance liquid chromatography

中圖分类号：R283文献标识码：Adoi：10.3969/j.issn.1673-7202.2020.15.009

随着人口老龄化程度日益加深，人们生活方式和饮食结构的改变，心血管疾病成为了威胁人类健康的头号杀手[1]。Salviae Miltiorrhizae Radix et Rhizoma是唇形科丹参属植物丹参Salvia miltiorrhiza Bge.的干燥根和根茎[2]。研究表明，丹参中的多种成分对心血管可以发挥抗氧化、抗血小板聚集及心肌保护的作用[3-5]。丹参注射液（Salvia Miltiorrhiza Injection，SMI）是丹参水提醇沉后精制而成，是心肌梗死的住院患者使用频率最高的中药制剂，使用频率高达35.5%[6]。但是，SMI存在药物成分在体内代谢较快的问题，导致到达靶部位药量较少[7-8]。有必要设计中药新型制剂对SMI进行改善，能够负载SMI多成分的同时，具有一定缓释效应。

多巴胺可以在碱性环境下聚合形成聚多巴胺（Polydopamine，PDA）纳米粒[9]。PDA具有良好的生物相容性，可以对多种药物同时进行吸附[10-11]。本研究提出利用PDA对SMI中的多成分进行负载，构建中药新制剂PDA-SMI，赋予其缓释性能，有助于延长药物在体内滞留时间。……