摘要
目的:制备小檗碱-厚朴酚共无定形系统以调控小檗碱的释放行为,并提高其抗菌性能。方法:选择厚朴酚为配体,通过溶剂挥发法制备小檗碱-厚朴酚的共旋蒸产物。采用粉末X-射线衍射、差示扫描量热分析、扫描电镜及傅里叶变换红外光谱法对小檗碱-厚朴酚的共旋蒸产物进行表征,同时对制剂的物理稳定性、体外溶出行为以及抗菌性能进行了考察。结果:表征结果证明成功制备了小檗碱-厚朴酚共无定形系统。物理稳定性结果表明小檗碱-厚朴酚共无定形系统在一个月内稳定性良好。溶解24 h后,共无定形系统中小檗碱的溶解度最高为211.30μg·mL^(-1),释放度约80%,其溶解度降低,并表现出缓释行为。在小檗碱-厚朴酚共无定形系统中,达到抑菌作用时小檗碱的药物质量浓度仅为32μg·mL^(-1),优于小檗碱单独抗菌性能。结论:小檗碱-厚朴酚共无定形系统降可调控小檗碱的释放行为,使其缓慢释放,并提高小檗碱的抗菌性能。
OBJECTIVE To prepare berberine magnolol(BBR-MAG)co-amorphous system to regulate the release behav-ior of BBR and improve its antibacterial performance.METHODS Selected as a co-former and a co-evaporation product of BBR,MAG was prepared by solvent evaporation.Then it was characterized by powder X-ray diffraction(PXRD),differential scanning calorimetry,scanning electron microscope and Fourier transform infrared spectroscopy.Next,physical stability,invitro dissolution behavior and antibacterial properties of the formulation were evaluated.RESULTS The characterization results indi-cated that the co-amorphous system of BBR-MAG was successfully prepared.The physical stability results indicated that the BBR-MAG co-amorphous system remained stable for 1 month.After 24 h dissolution,the highest solubility of BBR in the co-amorphous system was 211.30μg·mL^(-1) releasing approximately 80%of BBR,reducing its solubility and exhibiting sustained release behavior.When the co-amorphous system of BBR-MAG displayed antibacterial effect,drug concentration of BBR was only 32μg·mL^(-1) with better antibacterial activity than BBR alone.CONCLUSION The co-amorphous system of BBR-MAG can regulate the release behavior of BBR,slow its release and improve its antibacterial properties.
作者
王杰
张成
王欣宇
卢昊
郭瑜婕
洪怡
卢山
贺建华
许汉林
WANG Jie;ZHANG Cheng;WANG Xinyu;LU hao;GUO Yujie;HONG Yi;LU Shan;HE Jianhua;XU Hanlin(School of Pharmacy,Hubei University of Traditional Chinese Medicine,Hubei Wuhan 430065,China)
出处
《中国医院药学杂志》
CAS
北大核心
2024年第22期2620-2627,共8页
Chinese Journal of Hospital Pharmacy
关键词
小檗碱
厚朴酚
共无定形
溶出度
抗菌性能
berberine
magnolol
co-amorphous
dissolution
antibacterial property
作者简介
王杰,男,硕士研究生,研究方向:中药新制剂与新剂型型;通信作者:贺建华,男,博士,副教授,研究方向:中药新制剂与新剂型;通信作者:许汉林,男,博士,教授,研究方向:中药新制剂与新剂型。
