Process optimisation, characterisation and evaluation of resveratrol-phospholipid complexes using Box-Behnken statistical design.

A. Agarwal, Vandana Kharb, V. Saharan
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引用次数: 29

Abstract

With the advent of 21 st century, researchers worldwide have extensively reviewed herbs and botanicals for their marked clinical efficacy. It has been estimated that most of the newly discovered compounds offer poor bioavailability due to their low aqueous solubility. Phospholipid complexation of the drug often helps to improve its water solubility and enhance the bioavailability. This study includes optimization of resveratrol-phospholipid complexes using a 3-factor, 3-level box-behnken design (15 batches). Three independent variables i.e. phospholipid-resveratrol ratio, refluxing temperature and reflux time were optimized for two dependent variables, i.e. yield and entrapment efficiency (EE). Complexes were prepared by refluxing stoichiometric ratio of Phospholipon 90G and resveratrol in dichloromethane and retrieved by precipitation with n-hexane. Complexation was confirmed by Fourier Transform Infra-Red (FTIR) spectroscopy. The data was suitably used to explore quadratic response surfaces and construct second order polynomial models with Design Expert®. Formulation with highest desirability (D=0.994) was selected as optimum and prepared using 1.5:1 Phospholipon 90G-resveratrol ratio (X1) at 59.4°C temperature (X2) and 4 h time (X3) to give maximum yield and entrapment efficiency. Analysis of variance (ANOVA) was also found to be significant for both the responses. Complexes were optimised for good yield and EE. The partition coefficient was lowered to 2.25 hypothesizing good passive absorption. DOI:  http://dx.doi.org/10.3329/icpj.v3i7.19079 International Current Pharmaceutical Journal, June 2014, 3(7): 301-308
使用Box-Behnken统计设计对白藜芦醇-磷脂复合物进行工艺优化、表征和评价。
随着21世纪的到来,世界各地的研究人员对草药和植物药的临床疗效进行了广泛的研究。据估计,大多数新发现的化合物由于水溶性较低,生物利用度较差。磷脂络合的药物往往有助于改善其水溶性和提高生物利用度。本研究采用3因素、3水平盒本肯设计(15批)对白藜芦醇-磷脂复合物进行优化。对磷脂-白藜芦醇比、回流温度和回流时间三个自变量对产率和包封效率(EE)两个因变量进行优化。用磷脂90G与白藜芦醇的化学计量比在二氯甲烷中回流制备配合物,用正己烷沉淀法回收。傅里叶变换红外光谱(FTIR)证实了络合作用。利用Design Expert®对数据进行二次响应面探索,构建二阶多项式模型。以1.5:1磷脂90g -白藜芦醇比(X1)为最优配方(D=0.994),在59.4℃温度(X2)、4 h时间(X3)条件下制备得率和包封效率最高。方差分析(ANOVA)也被发现对两种反应都是显著的。优化后的配合物产率和EE均较高。分配系数降低到2.25,假设有良好的被动吸收。DOI: http://dx.doi.org/10.3329/icpj.v3i7.19079国际现代医药杂志,2014年6月,3(7):301-308
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