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表面活性剂链长对难溶性药物自乳化制剂乳化动力学的影响。

Effect of Surfactant Chain Length on Emulsification Dynamics of Self Emulsifying Formulation of Poorly Soluble Drug.

机构信息

Department of Pharmaceutical Sciences, Mohanlal Sukhadia University, Udaipur, Rajasthan, India.

出版信息

Curr Drug Deliv. 2022;19(8):874-888. doi: 10.2174/1567201818666210727092639.

Abstract

AIM

In this work, the aim was to study the effect of the chain length of surfactant on the self emulsifying system of a poorly soluble drug, aceclofenac. The selection of almond oil as a lipid vehicle was done on the basis of solubility and compatibility of the vehicle with the drug.

METHODS

The effect of varying chain length of different surfactants of Tween series, namely Tween 20, Tween 40, Tween 60 and Tween 80, was evaluated on self emulsifying efficiency by constructing the pseudoternary diagrams. PEG-400 was used as a co-surfactant in a definite ratio with all the surfactants to minimize their concentration. The best self emulsifying ability was exhibited by Tween 80: PEG-400 combination followed by Tween 60: PEG-400, Tween 40: PEG-400, Tween 20: PEG-400. This observation indicates that as the chain length of Tweens increases, their ability to form a good microemulsion increases if the same co-surfactant is used.

RESULTS

However, it has also been found that the presence of unsaturated bond in Tween 80 provides it an elasticity which supports good intermixing of oil and water, leading to formation of a fine microemulsion. Six different formulations were prepared using a combination of almond oil, Tween 80, PEG-400 and the drug aceclofenac.

CONCLUSION

The formulations were subjected to various evaluation parameters, such as dispersibility, transmittance, pH, globule size, polydispersibility, zeta potential, viscosity, refractive index and in vitro dissolution. The best formulation was found to have globule size of less than 100 nm and zeta potential of -3.35 ± 0.60 mV, indicating the formation of a microemulsion of aceclofenac with good stability.

摘要

目的

在这项工作中,目的是研究表面活性剂的链长对难溶性药物醋氯芬酸自乳化系统的影响。选择杏仁油作为脂质载体是基于载体与药物的溶解度和相容性。

方法

通过构建伪三元相图,评价了吐温系列中不同表面活性剂(即吐温 20、吐温 40、吐温 60 和吐温 80)的链长变化对自乳化效率的影响。聚乙二醇 400(PEG-400)与所有表面活性剂以一定比例用作助表面活性剂,以最小化其浓度。Tween 80:PEG-400 组合表现出最佳的自乳化能力,其次是 Tween 60:PEG-400、Tween 40:PEG-400、Tween 20:PEG-400。这表明,使用相同的助表面活性剂时,随着吐温的链长增加,其形成良好微乳液的能力增加。

结果

然而,也发现 Tween 80 中不饱和键的存在为其提供了弹性,支持油和水的良好混合,从而形成精细的微乳液。使用杏仁油、Tween 80、PEG-400 和药物醋氯芬酸组合制备了六种不同的配方。

结论

对配方进行了各种评价参数的测试,如分散性、透光率、pH 值、液滴大小、多分散性、zeta 电位、粘度、折射率和体外溶解。发现最佳配方的液滴大小小于 100nm,zeta 电位为-3.35±0.60mV,表明形成了具有良好稳定性的醋氯芬酸微乳液。

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