基于粉体表面改性的青黛干混悬剂制备与评价  

Preparation and evaluation of Indigo Naturalis dry suspension based on powder surface modification

作　　者：黄胜杰 苏娟[1] 葛春丽 谢锦 郭治平 杨明 伍振峰 张定堃[1] 韩丽[1] HUANG Sheng-jie;SU Juan;GE Chun-li;XIE Jin;GUO Zhi-ping;YANG Ming;WU Zhen-feng;ZHANG Ding-kun;HAN Li(Pharmacy School,State Key Laboratory of Southwestern Chinese Medicine Resources,Chengdu University of Traditional Chinese Medicine,Chengdu 611137,China;Sichuan Houde Pharmaceutical Technology Co.,Ltd.,Chengdu 610041,China;State Key Laboratory of Innovation Drug and Efficient Energy-Saving Pharmaceutical Equipment,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China)

机构地区：[1]成都中医药大学药学院,西南特色中药资源国家重点实验室,四川成都611137 [2]四川厚德医药科技有限公司,四川成都610041 [3]江西中医药大学,现代中药制剂教育部重点实验室,江西南昌330004

出　　处：《药学学报》2023年第5期1347-1353,共7页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金面上项目(82173976,81773918);江西中医药大学创新药物与高效节能降耗制药设备国家重点实验室开放基金课题项目(GZSYS202003)。

摘　　要：采用粉体改性技术,设计了一种基于乳糖-青黛复合粒子的青黛干混悬剂,实现润湿性与沉降性的平衡,满足青黛饮片临床用药需求。以接触角为评价指标,考察改性剂乳糖研磨时间、乳糖用量以及乳糖青黛共研时间对亲水改性效果的影响,并通过粒径、扫描电镜、红外光谱、表面自由能、多重光散射技术等对比改性前后青黛的差异。结果表明乳糖-青黛复合粒子最优工艺为:乳糖单独研磨2 min后,以1∶1的比例与青黛共研6 min。青黛改性后粒径d0.9由112.75μm降至87.30μm。BET和Langmuir比表面积分别下降8.661和12.512 m^(2)·g^(-1)。SEM显示改性青黛表面附着有乳糖;表面元素分析显示改性青黛的Si、Ca、Mg元素小于普通青黛,O元素大于普通青黛;红外光谱显示改性青黛同时拥有青黛和乳糖的特征峰。亲水性考察结果显示改性青黛接触角和非极性分量较未改性青黛分别降低35.1°和9.975 mJ·m^(-2),极性分量和表面自由能分别增加36.956和26.950 mJ·m^(-2)。多重光散射结果显示改性青黛透光度较未改性青黛降低35%,背散射光强增加约25%。本研究仅使用一种辅料成功制备了润湿性与混悬性良好的青黛干混悬剂,为青黛饮片的临床应用提供了便利。A dry suspension of Indigo Naturalis(IN)based on lactose-IN composite particles was designed by powder modification technology to meet the clinical needs of IN.The contact angle was used as an evaluation index to investigate the effects of the type of modifier lactose,the amount of lactose,and the co-grinding time of lactose and IN on the hydrophilicity of IN.The difference between IN before and after modification was compared through physical properties such as particle size and scanning electron microscope,as well as hydrophilic properties such as surface free energy and multiple light scattering.The optimal process of lactose-IN composite particles is as follows:after lactose is ground alone for 2 minutes,it is co-ground with IN at a ratio of 1∶1 for 6 minutes.The results of the investigation of powder properties show that the particle size d0.9 of IN is reduced from 112.75μm to 87.30μm after modification.The BET and Langmuir specific surface areas decreased by 8.661 m^(2)·g^(-1)and 12.512 m^(2)·g^(-1),respectively.SEM shows that lactose is attached to the surface of modified IN(MIN);surface element analysis shows that Si,Ca,and Mg elements of MIN are smaller than IN,and O elements are larger.The infrared spectrum shows that the MIN possesses the characteristic peaks of both IN and lactose.Compared MIN with IN,the contact angle and the non-polar surface free energy decreased by 35.1°and 9.975 mJ·m^(-2),respectively;the polar surface free energy and the surface free energy increased by 36.956 and 26.950 mJ·m^(-2),respectively.The results of multiple light scattering showed that the light transmittance of MIN was 35%lower than that of IN,and the backscattered light intensity was increased by about 25%.Only one excipient was used to successfully prepare IN dry suspension with good wettability and suspending property,which provided a basis for the development of new preparations of IN.

关 键 词：干混悬剂 难溶性 青黛 超微粉碎 粉体表面改性 

分 类 号：R943[医药卫生—药剂学]