纤维素类药物辅料对药物释放的影响  

Effects of cellulose drug excipients on drug release

作　　者：王爽 许潇文 黄璐瑶 尹宗宁[1] WANG Shuang;XU Xiaowen;HUANG Luyao;YIN Zongning(Key Laboratory of Drug Targeting and Drug Delivery Systems,West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China)

机构地区：[1]四川大学华西药学院靶向药物与释药系统教育部重点实验室,四川成都610041

出　　处：《华西药学杂志》2021年第2期159-162,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81673363)。

摘　　要：目的研究纤维类药用辅料的膳食纤维特性以及在消化道的过程。方法通过测定纤维的吸水性、持水性、持油性,并以简单的颗粒剂赋性,考察颗粒的溶出;用细胞膜红色荧光探针荧光示踪考察纤维在消化道内的变化过程。结果水溶性纤维辅料无膨胀性,持水性能差;溶胶性纤维辅料溶胀性能、持水性能在3种类型的纤维辅料中最好;3种纤维的持油性能无差异。不同纤维制成的颗粒在相同介质中的差异表现在溶出的速度和纤维素辅料的溶解速度有关,溶胀系数越强溶出速度越慢。在荧光示踪实验中,用细胞膜红色荧光探针为荧光染料,在小鼠体内荧光强度的持续时间与纤维材料的持油性能有关,持油性能越强在体内的荧光强度越强且荧光持续时间长。结论纤维类药用辅料的持水性可能会影响水溶性药物的溶出,持油性能可能会影响脂溶性药物在体内的滞留时间。OBJECTIVE To study the characteristics of dietary fiber and its process in digestive tract.METHODS The water absorption,water holding and oil holding of fiber were determined,and the granules were used to investigate the dissolution of the fiber.DID fluorescence tracing was used to investigate the changes of fibers in the digestive tract.RESULTS Water-soluble fiber excipients had no expansibility and poor water-holding performance.The swelling and water holding properties of sol fiber excipients were the best among the three types of fiber excipients.There was no difference in oil holding performance among the three fibers.The difference of particles made of different fibers in the same medium was related to the dissolution rate of cellulose excipients.The stronger the swelling coefficient was,the slower the dissolution rate would be.In the fluorescence tracer experiment,DID was used as the fluorescent dye,and the duration of fluorescence intensity in mice was related to the oil-holding performance of the fiber material.The stronger the oil-holding performance was,the stronger the fluorescence intensity was in vivo and the longer the fluorescence duration was.CONCLUSION The water-holding properties of fibrous pharmaceutical excipients may affect the dissolution of water-soluble drugs,and the oil-holding properties may affect the retention time of fat-soluble drugs in vivo.

关 键 词：纤维素 药用辅料 膳食纤维 吸水性 持水性 持油性 荧光示踪 体外释放 

分 类 号：R94[医药卫生—药剂学]