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利用自微乳药物传递系统提高非索非那定的溶解度,改善仿生特性。

Solubility enhancement of fexofenadine using self-nano emulsifying drug delivery system for improved biomimetic attributes.

机构信息

AETs St. John Institute of Pharmacy and Research, Palghar, Maharashtra, India.

MES's College of Pharmacy, Sonai, Ahmednagar, Maharashtra, India.

出版信息

Ann Pharm Fr. 2024 May;82(3):433-445. doi: 10.1016/j.pharma.2023.10.003. Epub 2023 Oct 11.

Abstract

BACKGROUND

Fexofenadine is a poorly water-soluble drug, which limit its bioavailability and ultimately therapeutic efficacy. Liquid self-nano emulsifying drug delivery system (L-SNEDDs) is an approach that can enhance the solubility of fexofenadine by increasing its surface area and reducing the particle size, which increases the rate and extent of drug dissolution.

METHOD

In this investigation, L-SNEDDs of fexofenadine was made up using surfactants and co-surfactant. The SNEDDS formulation was optimized using a pseudo-ternary phase diagram and characterized.

RESULTS

The optimized L-SNEDDS incorporated fexofenadine were thermodynamically stable and showed mean droplet size and zeta potential of 155nm and -18mV, respectively unaffected by the media pH. In addition, the viscosity, and refractive index were observed 18.4 and 1.49 cps, respectively for optimized L-SNEDDS fortified fexofenadine. The results of Fourier transform infrared spectroscopy revealed an insignificant interaction between the fexofenadine and excipients. A drug loading efficiency of 94.20% resulted with a complete in vitro drug release in 2h, compared with the pure drug, which demonstrate significant improvement in the efficacy. Moreover, these results signify that on further in vivo assessment L-SNEDDS fortified fexofenadine can indicate improvement in pharmacokinetic and clinical outcome.

CONCLUSION

Thus, the investigation revealed that, the L-SNEDDs incorporated fexofenadine was most effective with a mixture of surfactant and co-surfactant with improved solubility intend to relieve pain associated with inflammation with single-dose oral administration.

摘要

背景

非索非那定是一种水溶性较差的药物,其生物利用度和最终疗效受到限制。液体自微乳给药系统(L-SNEDDS)是一种可以通过增加表面积和减小粒径来提高非索非那定溶解度的方法,从而提高药物的溶解速率和程度。

方法

在这项研究中,使用表面活性剂和助表面活性剂制备了非索非那定的 L-SNEDDS。通过伪三元相图优化 SNEDDS 配方并进行表征。

结果

优化的 L-SNEDDS 包载非索非那定后热力学稳定,表现出平均粒径和 zeta 电位分别为 155nm 和-18mV,不受介质 pH 值的影响。此外,观察到优化的 L-SNEDDS 包载非索非那定的粘度和折射率分别为 18.4 和 1.49cps。傅里叶变换红外光谱的结果表明非索非那定与赋形剂之间没有明显的相互作用。与纯药物相比,优化的 L-SNEDDS 包载非索非那定的药物载药量为 94.20%,完全体外释放 2h,表明疗效显著提高。此外,这些结果表明,进一步的体内评估表明,L-SNEDDS 包载非索非那定可以改善药代动力学和临床结果。

结论

因此,该研究表明,L-SNEDDS 包载非索非那定与表面活性剂和助表面活性剂的混合物最有效,具有改善的溶解度,旨在通过单次口服给药缓解与炎症相关的疼痛。

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