|本期目录/Table of Contents|

[1]邢正英,李继彬,李 晗,等.星点设计-效应面法优化枸橼酸西地那非分散片处方[J].天津医科大学学报,2017,23(01):74-78.
 XING Zheng-ying,LI Ji-bin,LI Han,et al.Optimizing the formation of sildenafil citrate dispersible tablets by central composite design-response surface methodology[J].Journal of Tianjin Medical University,2017,23(01):74-78.
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《天津医科大学学报》[ISSN:1006-8147/CN:12-1259/R]

卷:
23卷
期数:
2017年01期
页码:
74-78
栏目:
技术与方法
出版日期:
2017-01-16

文章信息/Info

Title:
Optimizing the formation of sildenafil citrate dispersible tablets by central composite design-response surface methodology
文章编号:
1006-8147(2017)01-0074-05
作者:

邢正英李继彬李 晗杨金荣房志仲

?

(天津医科大学药学院,天津市临床药物关键技术重点实验室,天津300070)
Author(s):
XING Zheng-ying LI Ji-bin LI Han YANG Jin-rong FANG Zhi-zhong
(College of Pharmacy, Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development of Clinical Therapeutics and Diagnostics(Theranostics), Tianjin 300070, China)
关键词:

line-height: 125%" align="left">枸橼酸西地那非分散片星点设计-效应面法处方筛选分散均匀性累积溶出百分率

Keywords:
sildenafil citrate dispersible tablets central composite design-response surface methodology prescription screening dispersible uniformity cumulative dissolution
分类号:
R9
DOI:
-
文献标志码:
A
摘要:

目的:以枸橼酸西地那非为模型药物,采用星点设计-效应面法优化分散片的处方。方法: 在筛选优化分散片处方时采用星点设计-效应面优化法结合单因素考察的方法。在预试验的基础上,以处方中內加交联羧甲基纤维素钠(CCNa)、外加交联羧甲基纤维素钠(CCNa)以及羟丙甲基纤维素(HPMC)的含量为考察因素,以分散均匀性和15 min累积溶出百分率为评价指标,根据星点设计的原理进行试验,并采用多元线性回归和多元非线性回归拟合两个评价指标与影响因素之间的数学模型,经效应面法预测得到最佳处方。鉴于本分散片在15 min的累积溶出百分率大于85%,可不与原研制剂进行f(2)因子的比较。结果:数据表明,多元非线性拟合的相关系数高于线性拟合,具有较高的可信度。综合效应面优化和评估结果,最佳处方确定为内加CCNa为30 mg,外加CCNa为40 mg,HPMC为0 mg。结论:通过星点设计-效应面优化法所建立的模型可以用于枸橼酸西地那非分散片处方的优化。

Abstract:
Objective: To optimize the formulation of dispersible tablets using silde-nafil citrate as a model drug by central composite design-response surface methodolo-gy. Methods: In this study, the central composite design- response surface methodology with single factor method was applied to screen and optimize prescription .On the basis of preliminary experiments, the proportion of CCNa(inside and outside the particles) and HPMC were set up as study factors, and dispersible uniformity and 15 min cumulative dissolution were set up as evaluation indexes. According to the theory of central composite design, the correlation between evaluation indexes and formulation was simulated using multi-linear equation and multi-nonlinear equation. The possible optimal formulation was predicted by response surface method. Due to the fact that the 15 min cumulative dissolution of the dispersible tablets was higher than 85%, there was no need to compare the f(2) factors with original development agents. Results: The data shown that multi-nonlinear equation models were superior to multi-linear equation models with better regression coefficients and higher reliability. It was determined that the dosage of CCNa (inside and out-side the particles) and HPMC were 30 mg, 40 mg and 0 mg in the optimized formulation, respectively. Conclusion: The established model based on the central composite design-response surface methodology may be suitable for the optimization of sildenafil citrate dispersible tablets.

参考文献/References:

[1] 朱锋. 肺动脉高压研究进展[J]. 心血管病学进展, 2011,32(2):167

[2] 苏威,李江. 肺动脉高压药物靶向治疗的展望[J].中华临床医师杂志, 2014,8(16):3016

[3] 罗鹏.动脉型肺动脉高压靶向药物治疗的中国证据[J].中国循环杂志, 2014,29(7):552

[4] 李宏军.勃起功能障碍的诊治进展与共识[J].中国性科学, 2011,20(1):5

[5] 张兴源,潘连军.西地那非和酚妥拉明治疗勃起功能障碍的临床疗效比较[J]. 现代药物与临床, 2014,29(12):1386

[6] 赵良运,耿瑞明,张志兴,等. 长期小剂量西地那非治疗勃起功能障碍58例[J].湖北民族学院学报, 2011,28(2):4

[7] Galie N, Ghofrant HA, Torbicki A, et al. Sildenafil citrate therapy for pulmonary arterial hype-

rtension[J]. N Engl J Med, 2005,253:2148

[8] 闫芳,夏宇,李威,等. 西地那非治疗肺动脉高压的疗效及安全性研究[J].中国临床药理学杂志, 2014,30(10):877

[9] 孔翠萍,时文祥.美洛昔康分散片处方筛选研究[J].江苏科技信息,2015,2:46

[10] 国家药典委员会.中国药典[S].二部.北京:中国医药科技出版社,2015:附录IA

[11] 国家药典委员会.中国药典[S].二部.北京:中国医药科技出版社,2015:附录XC

[12] 刘逊,陈俭清,李明雁,等. 星点设计-效应面法优化连翘颗粒剂的制备工艺研究[J].东北农业大学学报, 2012,43(6):130

[13] 隋洪飞,王姿婧,刘青,等.星点设计-效应面法优化硝苯地平分散片处方[J]. 天津医科大学学报, 2014,20(4):323

[14] 陈飞,邢雪飞,白雪,等.星点设计-效应面法优选欣宁泡腾片提取工艺[J].中草药, 2014,45

(11):1566

[15] 施昶,沈诗偲,黄海飞,等.星点设计-效应面优化法在处方筛选和优化中的应用[J].中国制药装备, 2014, 32:41

[16] 刘艳杰,项荣武.星点设计效应面法在药学试验设计中的应用[J].中国现代应用药学杂志,

2007,24(6):455

[17] 胡昌勤,潘瑞雪.溶出度试验评价/预测固体口服制剂生物等效性的研究进展[J].中国新药杂志, 2014,23(1):45

[18] 靖博宇,王志远,李 燕,等.非洛地平固体分散体的制备和体外溶出度考察[J].沈阳药科大学学报, 2010, 27(3):186

[19] 姚永新,林婉婷,廖华卫,等.中美6个布洛芬软胶囊的体外溶出度与生物利用度比较研究[J].广东药学院学报, 2015,31(2):146

[20] 郝海军,张红芹,贾幼智,等.采用制剂新技术提高中药磷脂复合物的溶出度和生物利用度研究进展[J].中草药, 2013,44(17):2476

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备注/Memo

备注/Memo:
作者简介 邢正英(1994-),女,硕士在读,研究方向:药物制剂与质量控制;通信作者:房志仲,E-mail:fangzhizhong@tijmu.edu.cn
更新日期/Last Update: 2017-01-16