| 李勇,赵婧铎,唐国涛.噻吗洛尔微乳凝胶的构建及其药学研究[J].南华大学学报(自然科学版),2018,32(4):84~89, 96.[LI Yong,ZHAO Jingduo,TANG Guotao.The Construction and Pharmaceutical Research of Timolol Microemulsion Gel[J].Journal of University of South China(Science and Technology),2018,32(4):84~89, 96.] |
| 噻吗洛尔微乳凝胶的构建及其药学研究 |
| The Construction and Pharmaceutical Research of Timolol Microemulsion Gel |
| 投稿时间：2018-04-24 |
| DOI： |
| 中文关键词: 星点设计-效应面法 W/O型微乳 微乳凝胶 局部经皮给药 |
| 英文关键词:Central Composite Design/Response Surface Method W/O microemulsion microemulsion gel local transdermal delivery |
| 基金项目:湖南省科技厅一般项目(2014SK3027) |
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| 中文摘要: |
| 运用伪三元相图法和星点设计效应面法筛选最佳载药微乳处方,将其制备噻吗洛尔微乳凝胶,方便血管瘤患儿的经皮给药.采用手工滴加法制备各处方微乳,根据伪三元相图各微乳区面积大小初步筛选处方.然后根据处方各相形成微乳时的用量范围设计星点实验,以油相、表面活性剂、Km为自变量,载药量为响应值,拟合非线性回归方程并建立效应面模型,经过数据分析得到最佳载药处方.随后将凝胶基质加入噻吗洛尔微乳中充分溶胀,即得噻吗洛尔微乳凝胶.最佳处方(质量百分数)为30%油酸,24% Span80/Tween80,无水乙醇:30%,水:15.5%,噻吗洛尔:0.5%,所需凝胶基质卡波姆940的最佳用量为8.3%.最优处方制得的噻吗洛尔微乳凝胶呈淡黄色透明半固体状,质地均匀细腻,黏度适中,便于婴幼儿血管瘤的局部给药. |
| 英文摘要: |
| The optimal drug-loaded microemulsion formulation was screened by pseudo-ternary phase diagram method and Central Composite Design/Response Surface Method,and timolol microemulsion gel was prepared to facilitate the percutaneous administration of infantile hemangiomas in children.The prescription microemulsions were prepared by manual dropping addition,and the prescriptions were preliminarily screened according to the size of each microemulsion area of the pseudo-ternary phase diagram.Then the central composite was designed according to the range of the amount of microemulsion formed in each phase of the formulation.The oil phase,surfactant,and Km were independent variables and the drug loading was the response value.The nonlinear regression equation was fitted and an effect surface model was established.The best drug prescription was obtained by data analysis.Subsequently,the gel matrix was added to timolol microemulsion to sufficiently swell to obtain timolol microemulsion gel.The best prescription is 30% oleic acid,24% Span 80/Tween 80,30% absolute ethanol,15.5% water,0.5% timolol,and the optimal amount of gel matrix needed for Carbomer 940 is 8.3%.The 0.5% timolol microemulsion gel prepared by the optimal prescription is pale yellow transparent semi-solid,uniform in texture,moderate in viscosity,and convenient for local administration of infantile hemangiomas. |
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