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美洛昔康自微乳给药系统的处方前研究与评价。

Formulation and evaluation of meloxicam as a self-microemulsifying drug delivery system.

机构信息

Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Baghdad Governorate, Iraq.

出版信息

F1000Res. 2023 May 30;12:315. doi: 10.12688/f1000research.130749.2. eCollection 2023.

DOI:10.12688/f1000research.130749.2
PMID:37359788
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10285354/
Abstract

The nonsteroidal anti-inflammatory medication meloxicam (MLX) belongs to the oxicam family and is used to reduce inflammation and pain. The aim of this study was to improve MLX's dispersibility and stability by producing it as a liquid self-microemulsifying drug delivery system since it is practically insoluble in water. Five different formulations were made by adjusting the amounts of propylene glycol, Transcutol P, Tween 80, and oleic acid oil and establishing a pseudo-ternary diagram in ratios of 1:1, 1:2, 1:3, 1:4, and 3:4, respectively. All of the prepared formulations were tested for a variety of properties, including thermodynamic stability, polydispersity index, particle size distributions, dilution resistance, drug contents, dispersibility, solubility of the drug, and emulsification time. F5 was chosen as the optimal MLX liquid self-microemulsion due to its higher drug content (99.8%), greater release (100% at 40 min), smaller droplet size (63 nm), lower polydispersity index (PDI) value (0.3), and higher stability (a zeta potential of -81 mV). According to the data provided here, the self-microemulsifying drug delivery system is the most practical method for improving the dispersibility and stability of MLX.

摘要

非甾体抗炎药美洛昔康(MLX)属于昔康类,用于减轻炎症和疼痛。本研究旨在通过制备 MLX 的液体自微乳给药系统来提高其分散性和稳定性,因为它在水中几乎不溶。通过调整丙二醇、Transcutol P、吐温 80 和油酸油的用量,并分别以 1:1、1:2、1:3、1:4 和 3:4 的比例建立伪三元图,制备了 5 种不同的配方。对所有制备的配方进行了多种性质的测试,包括热力学稳定性、多分散指数、粒径分布、稀释阻力、药物含量、分散性、药物溶解度和乳化时间。由于 F5 具有较高的药物含量(99.8%)、更大的释放度(40 分钟内达到 100%)、较小的粒径(63nm)、较低的多分散指数(PDI)值(0.3)和更高的稳定性(zeta 电位为-81mV),因此被选为最佳 MLX 液体自微乳。根据这里提供的数据,自微乳给药系统是提高 MLX 分散性和稳定性最实用的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/a91d87f60351/f1000research-12-148205-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/699d5092ce86/f1000research-12-148205-g0000.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/7af00b28556b/f1000research-12-148205-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/e8a49a33dc7d/f1000research-12-148205-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/73e9f7d15de0/f1000research-12-148205-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/49c374014989/f1000research-12-148205-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/a91d87f60351/f1000research-12-148205-g0005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/699d5092ce86/f1000research-12-148205-g0000.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/7af00b28556b/f1000research-12-148205-g0001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/e8a49a33dc7d/f1000research-12-148205-g0002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/73e9f7d15de0/f1000research-12-148205-g0003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/49c374014989/f1000research-12-148205-g0004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd6f/10285434/a91d87f60351/f1000research-12-148205-g0005.jpg

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