伊维菌素释药行为与介质中溶解度相关性研究
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摘要
为阐明伊维菌素固体分散体(Ivermectin Solid Dispersion,IVM SD)释药行为与介质中溶解度的相关性,先测定伊维菌素在不同比例复合介质中的溶解度,然后研究释药行为。结果表明,随着乙醇浓度的增大,IVM溶解度越大,IVM SD中IVM的释药现象越明显,初始释放速度越大;在不同溶解度介质中,初始释放速度和溶解度之间具有指数相关性,S=0. 2471e1. 4372v,R2=0. 8629,证实IVM SD中IVM的释放速率和溶解度之间具有正相关性。这为IVM SD长效混悬注射剂的介质和辅料的筛选提供理论依据。
In order to clarify correlation between drug release behavior of Ivermectin Solid Dispersion(IVM SD) and solubility of medium. Firstly,this paper determine the solubility of ivermectin in a series of different proportion compound medium. Then,we study drug release behavior of IVM SD in ethanol-PBS compound medium. The results showed that the increase of ethanol concentration,solubility is greater,drug release phenomenon is more obvious,initial release rate is greater,drug release kinetics and drug release mechanism are both different. In particular,there are exponential correlation between initial rate and solubility,S = 0. 2471 e1. 4372 v,R2= 0.8629,this confirmed that release rate and solubility have a positive correlation. Therefore,this provides theoretical basis for screening supplementary material of IVM SD long-term suspension injection,and provides new method and thought for other suspension agent.
In order to clarify correlation between drug release behavior of Ivermectin Solid Dispersion(IVM SD) and solubility of medium. Firstly,this paper determine the solubility of ivermectin in a series of different proportion compound medium. Then,we study drug release behavior of IVM SD in ethanol-PBS compound medium. The results showed that the increase of ethanol concentration,solubility is greater,drug release phenomenon is more obvious,initial release rate is greater,drug release kinetics and drug release mechanism are both different. In particular,there are exponential correlation between initial rate and solubility,S = 0. 2471 e1. 4372 v,R2= 0.8629,this confirmed that release rate and solubility have a positive correlation. Therefore,this provides theoretical basis for screening supplementary material of IVM SD long-term suspension injection,and provides new method and thought for other suspension agent.
引文
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[2]张志荣.药剂学[M].北京:高等教育出版社,2014:311-315.
[3]Fritz M L,Walker E D,Miller J R.Lethal andsublethal effects of avermectin/milbemycin parasiticides on the African malaria vector,Anopheles arabiensis[J].Journal of Medical Entomology,2012,49(02):326-331.
[4]张粉丽.芬苯达唑混悬剂的制备及其质量控制[D].杨凌:西北农林科技大学,2014.
[5]Tapscott A,Hakim L.1224 Bupivacaine extended-release liposome injectable suspension for postoperative pain management in penoscrotal urologic surgery[J].Journal of Urology,2013,189(4):501.
[6]党丽梅.阿苯达唑混悬剂的制备及其质量控制[D].杨凌:西北农林科技大学,2015.
[7]Agarwal S,Murthy R S R.Effect of Different Polymer Concentration on Drug Release Rate and Physicochemical Properties of Mucoadhesive Gastroretentive Tablets[J].Indian Journal of Pharmaceutical Science,2015,77(06):705-714.
[8]Yong Z,Melrong H,Jianping Z,et al.DDSolver:An Add-In Program for Modeling and Comparison of Drug Dissolution Profiles[J].The AAPS Journal,2010,3(12):263-271.
[9]王月然.抗病毒药物盐酸替洛隆缓释片的研究[D].天津:南开大学,2012.
[10]Horoszok L,Raymond V,Sattelle D B.GLC-3:a novel frpronil and BIDN-sensitive,but picrotoxinin-insensitive,L-glutamate-gated chloride channel subunit from Caenorhabditis elegans[J].British Journal of Pharmacology,2001,6:1 247-1 254.
[11]崔福德.药剂学[M].北京:人民卫生出版社,2011:347-351.
[12]夏晓静,周建平,王翔,等.伊维菌素聚乳酸微球的制备[J].中国药科大学学报,2004,35(5):43-46.