表界面特性在药物制剂研究中的应用现状
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摘要
表界面作为两相之间的过渡区域,属于物理化学范畴,目前在材料等科学领域广泛应用。同样,在药学研究中该性质也起着重要作用。药物制剂研究过程中所涉及的界面层离不开气-液-固之间二相或三相的相互作用,界面作用会影响制剂最终的成型性以及药物在人体内的溶出、吸收等。笔者通过对比表面积、表界面张力、表面吉布斯自由能等表界面特性的概述以及润湿、增溶、乳化等界面现象在药学研究中应用的分析,从药物制剂的过程控制及制剂产品的有效性等角度阐述表界面特性在药物制剂领域的重要作用。提示表界面特性作为药物的关键物理性质之一加以重视并应用到药学研究中是必要的。
The surface and interface,as the transition region between two phases,belongs to the category of physical chemistry. At present,it is widely used in materials and other scientific fields. Meanwhile,this property also plays an important role in pharmaceutical research. The interface layer involved in the progress of pharmaceutical preparations is connected with the two-phase or three-phase between gas,liquid and solid closely.The interface effect will affect the final shaping of pharmaceutical preparations and the dissolution and absorption of drugs in the human body. In this paper,the surface and interface characteristics( specific surface area,surfacial and interfacial tension and surface Gibbs free energy) were compared,and the application of interface phenomena( wetting,solubilization and emulsification) in pharmaceutical research were introduced. From the points of view of the progress control of pharmaceutical preparations and the effectiveness of their products,the article expounds the important role of properties of surface and interface in the field of pharmaceutical preparations. Therefore,it is necessary to pay attention to the properties of surface and interface,one of the key physical properties of drugs,and to apply them in the pharmaceutical research.
The surface and interface,as the transition region between two phases,belongs to the category of physical chemistry. At present,it is widely used in materials and other scientific fields. Meanwhile,this property also plays an important role in pharmaceutical research. The interface layer involved in the progress of pharmaceutical preparations is connected with the two-phase or three-phase between gas,liquid and solid closely.The interface effect will affect the final shaping of pharmaceutical preparations and the dissolution and absorption of drugs in the human body. In this paper,the surface and interface characteristics( specific surface area,surfacial and interfacial tension and surface Gibbs free energy) were compared,and the application of interface phenomena( wetting,solubilization and emulsification) in pharmaceutical research were introduced. From the points of view of the progress control of pharmaceutical preparations and the effectiveness of their products,the article expounds the important role of properties of surface and interface in the field of pharmaceutical preparations. Therefore,it is necessary to pay attention to the properties of surface and interface,one of the key physical properties of drugs,and to apply them in the pharmaceutical research.
引文
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[2]秦志永.木材与胶表界面润湿特性表征与影响因素研究[D].北京:北京林业大学,2014.
[3]山树民,吕小明,辛宏,等.陇东致密油藏低界面张力及高接触角助排剂的研发及应用[J].科学技术与工程,2017,17(13):15-19.
[4]刘幸平.物理化学[M].北京:中国中医药出版社,2012:198-201.
[5]邓怡平,赵修华,祖元刚,等.布洛芬纳米微粉的制备、表征及体外透皮性研究[J].中国药房,2017,28(1):99-102.
[6]胡琳琳,韦祎,徐玉松,等.两亲性刺突微球的制备及性能表征[J].过程工程学报,2017,17(4):821-826.
[7]蔡璐,梁少瑜,戴开金,等.人参超微粉与细粉的体外溶出度比较[J].南方医科大学学报,2013,33(10):1547-1550.
[8]尹振兴,孔辉,王海川,等.关于表面张力和表面自由能的讨论[J].大学化学,2016,31(9):77-82.
[9]明良山,李哲,吴飞,等.基于表面自由能性质的物料压缩特性研究[J].药学学报,2017,52(7):1170-1177.
[10]明良山,李哲,吴飞,等.基于表面自由能的粒子设计研究进展[J].中国药学杂志,2017,52(14):1201-1207.
[11]Papós K,Kása P,Ili?I,et al. Effect of the surface free energy of materials on the lamination tendency of bilayer tablets[J]. Int J Pharm,2015,496(2):609-613.
[12]邓江莉,王金,曲韵智.滴丸成型力影响因素的研究现状[J].黑龙江医药,2013,26(1):80-82.
[13]Giardino L,Andrade F B,Beltrami R. Antimicrobial effect and surface tension of some chelating solutions with added surfactants[J]. Braz Dent J,2016,27(5):584-588.
[14]HAN K,Woghiren O E,Priefer R. Surface tension examination of various liquid oral,nasal,and ophthalmic dosage forms[J]. Chem Cent J,2016,doi:10. 1186/s13065-016-0176-x.
[15]张青,王斌.表面活性剂促进片剂崩解的研究及展望[J].实用心脑肺血管病杂志,2017,25(S1):229-230.
[16]Affandi M M R M M,Tripathy M,Majeed A. Solubility enhancement of simvastatin and atorvastatin by arginine:contact angle determination, wettability and surfaceenergy characteristics[J]. J Mol Liq,2017,doi:10. 1016/j. molliq. 2017. 05. 068.
[17]罗丹,李小芳,余琳,等.基于液固压缩技术葛根总黄酮片速释机理探究[J].中药与临床,2015,6(2):51-54.
[18]王鑫,刘剑云,张定堃,等.青黛饮片亲水性改性工艺的优选研究[J].中草药,2016,47(3):401-406.
[19]冯易,张力中,凌保东,等.化合物接触角与溶解度、溶出速度的相互关系[J].暨南大学学报:自然科学与医学版,2017,38(3):214-222.
[20]华东东,李鹤然,杨白雪,等.药用辅料接触角的测定及表面活性剂对辅料润湿性的调节作用[J].药学学报,2015,50(10):1342-1345.
[21]杨鑫,杜宇坤,田文军,等.表面活性剂对辅料接触角的影响[J].中国药师,2017,20(11):2090-2092.
[22]洪春雪,束怡,曹宇,等.双氯芬酸钠缓释液体栓制备与体内外相关性研究[J].武汉大学学报:理学版,2012,58(4):281-285.
[23]Al-Hanbali O A,Hamed R,Arafat M,et al. Formulation and evaluation of diclofenac controlled release matrix tablets made of HPMC and Poloxamer 188 polymer:An assessment on mechanism of drug release[J]. Pak J Pharm Sci,2018,31(Suppl1):345-351.
[24]赵美荣.表面活性剂在增加药物溶解性方面的应用及发展趋势[J].企业科技与发展,2013(14):28-29.
[25]金云峰,刘瑞新,李宇辉,等. 3种非离子型表面活性剂对清开灵注射液中难溶性成分的增溶效果比较[J].中国现代中药,2016,18(2):213-218.
[26]陈诚,童青平,唐达.不同表面活性剂对盐酸沙拉沙星溶解度影响[J].中国动物保健,2016,18(12):81-84.
[27]徐洁,单爽,黄静,等.四种表面活性剂对姜黄素和黄芩苷的增溶作用[J].中国药剂学杂志,2016,14(3):78-88.
[28]丛英,张明令,苏柘僮,等.中药注射剂用辅料“吐温80”的增溶适宜性研究[J].中成药,2011,33(3):439-442.
[29]张崴,周雅文,赵莉,等.表面活性剂的性能与应用(Ⅷ)—表面活性剂的乳化作用及其应用[J].日用化学工业,2015,45(1):7-10.
[30]Bahloul B,Lassoued M A,Sfar S. A novel approach for the development and optimization of self emulsifying drug delivery system using HLB and response surface methodology:application to fenofibrate encapsulation[J]. Int J Pharm,2014,466(1/2):341-348.
[31]Ishak K A,Annuar M S M. Temperature-induced threephase equilibrium of medium-chain-length poly-3-hydroxyalkanoates-incorporated emulsion system for production of polymeric nanoparticle[J]. J Disper Sci Technol,2018,39(3):375-383.
[32]Mercado R A,Salager J L,Sadtler V,et al. Breaking of a cationic amine oil-in-water emulsion by p H increasing:Rheological monitoring to modelize asphalt emulsion rupture[J]. Colloid Surface A,2014,458:63-68.
[33]Driscoll D F. Lipid injectable emulsions:pharmacopeial and safety issues[J]. Pharm Res,2006,23(9):1959-1969.
[34]Memvanga P B,Préat V. Formulation design and in vivo antimalarial evaluation of lipid-based drug delivery systems for oral delivery ofβ-arteether[J]. Eur J Pharm Biopharm,2012,82(1):112-119.
[35]苏瑾,胡艳秋,田鸣.满山红油自乳化释药微乳的制备研究[J].黑龙江医药科学,2016,39(5):10-12.
[36]杨亚宁,董敬,张春荣,等.表(界)面张力等温曲线法评价乳化剂的乳化能力[J].中国药剂学杂志:网络版,2005,3(4):215-219.
[37]李荣苗,管咏梅,王森,等.烷基糖苷类乳化剂及其复配对乳膏微观结构与物理稳定性的影响[J].中成药,2016,38(1):62-67.
[38]Arancibia C,Riquelme N,Zú1iga R,et al. Comparing the effectiveness of natural and synthetic emulsifiers onoxidative and physical stability of avocado oil-based nanoemulsions[J]. Innov Food Sci Emerg,2017,44:159-166.
[39]Pandey V, Kohli S. SMEDDS of pioglitazone:formulation,in-vitro evaluation and stability studies[J].Future J Pharm Sci,2017,3(1):53-59.
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