摘要
本研究旨在考察不同类型稳定剂对两种不同性质药物纳米混悬剂的影响。采用介质研磨法,以3种不同类型稳定剂制备多奈哌齐和美洛昔康药物纳米混悬剂,并以粒径、电位、形态、晶型、体外释放及稳定性等为指标进行评价。结果显示,非离子型表面活性剂稳定作用与药物疏水程度相关,疏水性强的多奈哌齐更适合于低HLB值的非离子表面活性剂,而疏水性性较弱的美洛昔康与非离子型表面活性剂HLB值的高低无相关性。单一的离子型稳定剂不能使混悬剂保持长时间的稳定效果,对pH敏感的离子表面活性剂受到药物酸碱性的影响。亲水性聚合物PVP直接吸附到药物表面稳定颗粒,HPMC则更适合具有极性基团的美洛昔康。研究表明药物及稳定剂的理化性质对形成稳定的纳米混悬剂有着关键作用,为纳米混悬剂中稳定剂的选择提供了参考。
The purpose of this study is to investigate the effects of different types of stabilizers on two kinds of drug nanosuspensions. Donepezil and meloxicam nanosuspensions are prepared by medium grinding method with three different types of stabilizers, and the particle size, potential, morphology, crystal form, in vitro release and stability are evaluated. The results show that the stabilization of nonionic surfactants is related to the hydrophobicity of drugs. Donepezil with strong hydrophobicity is more suitable for nonionic surfactants with low HLB value, while meloxicam with weaker hydrophobicity is not related to HLB value of Nonionic surfactants. A single ionic stabilizer can not keep the suspension stable for a long time, and the pH-sensitive ionic surfactants are affected by the acid-base property of the drug. The hydrophilic polymer PVP is directly adsorbed on the drug surface to stabilize the particles, and HPMC is more suitable for meloxicam with polar groups. The research shows that the physicochemical properties of drugs and stabilizers play a key role in the formation of stable nanosuspensions, which provides a reference for the selection of stabilizers in nano-suspensions.
作者
吕亚男
王琳琳
綦玉洁
王爱萍
LYU Ya-nan;WANG Lin-lin;QI Yu-jie;WANG Ai-ping(School of Pharmacy,Key Laboratory of Molecular Pharmacology and Drug Evaluation(Yantai University),Ministry of Education,Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong.Yantai University,Yantai 264005,China;State Key Laboratory of Long-acting and Targeting Drug Delivery System,Shandong Luye Pharmaceutical Co Ltd,Yantai 264003,China)
出处
《烟台大学学报（自然科学与工程版）》
CAS
2022年第4期421-427,442,共8页
Journal of Yantai University(Natural Science and Engineering Edition)
基金
山东省自然科学基金重大基础研究项目(ZR2018ZC1055)。
