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奥硝唑自微乳给药系统的研制及其对提高 BCS Ⅱ类药物溶解度和口服生物利用度的评价。

Development and characterization of a self-nano emulsifying drug delivery system (SNEDDS) for Ornidazole to improve solubility and oral bioavailability of BCS class II drugs.

机构信息

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

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

出版信息

Sci Rep. 2024 Nov 12;14(1):27724. doi: 10.1038/s41598-024-73760-7.

Abstract

This study aimed to investigate the in vitro performance of self-nanoemulsifying drug delivery systems (SNEDDSs) of Ornidazole (ORD), a poorly water-soluble drug. Self-nanoemulsifying drug delivery systems of ORD were prepared using various oils, non-ionic surfactants, and/or water-soluble co-solvents and assessed visually/by droplet size measurement. Equilibrium solubility of ORD in the anhydrous and diluted SNEDDS was conducted to achieve the maximum drug loading. The in vitro dissolution of SNEDDS was studied to compare the solubility of the representative formulations with API. The results from the characterization and solubility studies showed that SNEDDS formulations were stable with lower droplet sizes and showed higher ORD solubility. From the dissolution studies, it was found that the developed A7-SNEDDS formulation provided a significantly higher rate of ORD release (98.94 ± 0.68 in 1.0 h) compared to API. ORD-loaded SNEDDS formulations could be a potential oral pharmaceutical product with high drug-loading capacity, improved drug dissolution, and enhanced oral bioavailability.

摘要

本研究旨在考察奥硝唑(ORNIDAZOLE,一种难溶性药物)自微乳药物传递系统(SNEDDS)的体外性能。使用各种油、非离子表面活性剂和/或水溶性共溶剂制备 ORNIDAZOLE 的自微乳药物传递系统,并通过目视观察/液滴大小测量进行评估。对无水和稀释的 SNEDDS 中的 ORNIDAZOLE 平衡溶解度进行了研究,以实现最大药物载量。对 SNEDDS 的体外溶出度进行了研究,以比较代表性制剂与原料药的溶解度。表征和溶解度研究的结果表明,SNEDDS 制剂具有较低的液滴尺寸且表现出更高的 ORNIDAZOLE 溶解度,稳定性良好。从溶出度研究中发现,与原料药相比,开发的 A7-SNEDDS 制剂能显著提高 ORNIDAZOLE 的释放速率(1.0 小时内 98.94 ± 0.68)。载 ORNIDAZOLE 的 SNEDDS 制剂可能是一种具有高载药量、改善药物溶解和提高口服生物利用度的潜在口服药物产品。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/806c/11557912/90ca2e7d788c/41598_2024_73760_Fig1_HTML.jpg

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