杨梅素微乳的制备及质量评价Preparation and quality evaluation of myricetin microemulsion
张颖慧,王淑君,徐琨,杨瑞,吴书昱,刘俏
ZHANG Ying-hui1,WANG Shu-jun1,XU Kun1,YANG Rui2,WU Shu-yu3,LIU Qiao3(1.School of Pharmacy
摘要(Abstract)：
目的制备杨梅素微乳,并评价其质量。方法选择适宜的油相、表面活性剂和助表面活性剂,利用伪三元相图筛选微乳处方,研制出适合经口给药的微乳制剂;采用HPLC法测定杨梅素的含量,并对微乳的类型、载药量、体外释放等进行考察。结果优选处方为聚山梨酯80-聚山梨酯20-乙醇-油酸-pH 6.5磷酸缓冲液的质量比20∶10∶15∶5∶50,杨梅素质量分数为2%。所制微乳外观透明,平均粒径为(56.3±8.7)nm,zeta电位为-2.73 mV,电导率为13.27 mS.m-1。载药微乳在不同pH值环境下对药物有良好的释放效果。结论通过优化处方制备的杨梅素微乳具有较稳定的理化性质,HPLC法可以有效、准确的测定杨梅素微乳的含量,并且微乳载药系统有良好的释药效果。
Objective To prepare myricetin microemulsion and estimate its quality.Methods The formulation was investigated by pseudo-ternary phase diagrams obtained by titration method.Myricetin was determined by HPLC.The type of the microemulsion,in vitro release and carrying dosage were investigated.Results The optimized formulation was composed of Tween 80-Tween 20-ethanol-oleic acid-pH 6.5 phosphate buffer(m∶m∶m ∶m ∶m=20∶10∶15∶5∶50)and the drug loading amount was 2%.The average diameter was(56.3±8.7)nm;the zeta potential was-2.73 mV;the electrical conductivity was 13.27 mS·m-1.Dosages in microemulsion were slow-released in 24 h at different pH conditions.Conclusions By optimized microemulsion formulation,the prepared myricetin microemulsion possess stable physical and chemical properties,the content of myricetin microemulsion can be determined by HPLC method,and microemulsion system shows a good drug release effect.
关键词(KeyWords)：
杨梅素;微乳;伪三元相图;高效液相色谱法;体外释放
myricetin;microemulsion;pseudo-ternary phase diagram;HPLC;releasing in vitro
基金项目(Foundation):
作者(Author):
张颖慧,王淑君,徐琨,杨瑞,吴书昱,刘俏
ZHANG Ying-hui1,WANG Shu-jun1,XU Kun1,YANG Rui2,WU Shu-yu3,LIU Qiao3(1.School of Pharmacy
DOI: 10.14066/j.cnki.cn21-1349/r.2010.10.017
参考文献(References)：
- [1]俞瑜,曾耀英,刘良,等.杨梅素对淋巴细胞活化及增殖的影响[J].中国药理学通报,2006,22(1):63-66.
- [2]SCHECHTER R S.Microemulsions and related system[M].New York:Marcewl Dekker,1998:2.
- [3]PHILIPL L,ROBERT L.Novel micromulsion enhancerfor mulation for simultaneous transdermal delivery ofhydrophilic and hydrophobic drugs[J].Pharm Res,2003,120(2):124-127.
- [4]LEE J M,PARK K M,LIM S J,et al.Microemulsionformulation of clonixic acid:solubility enhancement andpain reduction[J].Pharm Pharmacol,2002,54(1):43-49.
- [5]GASCO M R.Microemulsions in the pharmaceuticalfield:perspec-tives and applications//Industrial appli-cations of microemulsions[M].New York:Marcel Dek-ker,Inc,1997:97-122.
- [6]陆彬,张正全.用三角相图法研究药用微乳的形成条件[J].药学学报,2001,36(1):58-62.
- [7]陈寒梅,姚二东,邱国福,等.盐酸阿比朵尔微乳的制备及其质量评价[J].中国医院药学杂志,2006,26(4):397-400.
- [8]谭建宁,覃结萍,张炜,等.杨梅素原料药质量标准研究[J].中药材,2008,31(12):1908-1911.
- [9]IVANCHEVA S,PETROVA A.A chemosystematicstudy of elevenGeraniumspecies[J].Biochemical Sys-tematics and Ecology,2000,28:255-260.
- [10]张蜀,谭载友,陈济民,等.盐酸多西环素注入用缓释凝胶的体外释放度研究[J].中国新药杂志,2003,12(9):731-734.
- [11]薛昌刚,童春义,肖苏尧,等.诺氟沙星一壳聚糖微球的制备及释药性能[J].中南大学学报:自然科学版,2008,39(3):480-485.
- [12]孙红武,欧阳五庆.黄连素口服纳米乳的研制、质量及安全性评价[J].上海交通大学学报:农业科学版,2007,25(1):60-65.
- [13]LI Lian-li,RANASAL N I,KIN K H.Development ofanethyl laurate-baaed microemulsion for rapid-onset in-tranasal delivery of diazepam[J].Int J Pharm,2002,237:77-85.
- [14]王长虹,孙殿甲.乳剂的缓释和控释作用研究进展[J].国外医学:药学分册,1997,24(5):300.
- [15]汤韦,吕竹芬,陈燕忠,等.克拉霉素纳米乳的制备及体外释放度研究[J].广东药学院学报,2006,22(6):579-582.