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用于布地奈德释放的尤特奇（®）微粒：一项对比研究。

Eudragit(®) microparticles for the release of budesonide: a comparative study.

作者信息

Cortesi Rita, Ravani Laura, Menegatti Enea, Esposito Elisabetta, Ronconi F

机构信息

Department of Life Sciences and Biotechnology, University of Ferrara, 44121-Ferrara, Italy.

出版信息

Indian J Pharm Sci. 2012 Sep;74(5):415-21. doi: 10.4103/0250-474X.108416.

DOI:10.4103/0250-474X.108416
PMID:23716869
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3660867/
Abstract

This study compares the behaviour of budesonide-containing microparticles made of Eudragit(®)RS or Eudragit(®)RS/Eudragit(®)RL 70:30 (w/w) prepared either by solvent evaporation or spray-drying technique. The loading efficiency of budesonide within microparticles was about 72% for microparticles prepared by solvent evaporation and around 78% for spray-dried microparticles. Thermal analyses were assessed to collect information about the structural stability of budesonide within the polymeric microspheres. The in vitro release was performed using simulating gastric (fasted state simulated gastric fluid) and intestinal (fasted state simulated intestinal fluid) fluids as the receiving solutions. After 3 h the drug release from Eudragit(®)RS/Eudragit(®)RL microparticles was about 6-fold higher than that obtained in the case of monopolymer microparticles. Using fasted state simulated intestinal fluid the drug was released between 4 and 30% in both types of preparations. Eudragit(®)RS microparticles showed a better protection of the drug from gastric acidity than those of Eudragit(®)RS/Eudragit(®)RL allowing us to propose Eudragit(®)RS microparticles as a hypothetical system of colon specific controlled delivery.

摘要

本研究比较了采用溶剂蒸发法或喷雾干燥法制备的、由尤特奇（®）RS或尤特奇（®）RS/尤特奇（®）RL 70:30（重量比）制成的含布地奈德微粒的行为。对于通过溶剂蒸发法制备的微粒，布地奈德在微粒中的负载效率约为72%，而对于喷雾干燥微粒，该效率约为78%。进行热分析以收集有关布地奈德在聚合物微球中的结构稳定性的信息。体外释放实验使用模拟胃液（禁食状态模拟胃液）和肠液（禁食状态模拟肠液）作为接收溶液。3小时后，尤特奇（®）RS/尤特奇（®）RL微粒的药物释放量比单一聚合物微粒的情况高出约6倍。在两种制剂中，使用禁食状态模拟肠液时，药物释放量在4%至30%之间。与尤特奇（®）RS/尤特奇（®）RL微粒相比，尤特奇（®）RS微粒对药物具有更好的胃酸保护作用，这使我们能够提出将尤特奇（®）RS微粒作为一种结肠特异性控释的假设体系。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/3061b4f4883d/IJPhS-74-415-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/004b031027ac/IJPhS-74-415-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/ada264c642c1/IJPhS-74-415-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/42cecb427056/IJPhS-74-415-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/3061b4f4883d/IJPhS-74-415-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/004b031027ac/IJPhS-74-415-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/ada264c642c1/IJPhS-74-415-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/42cecb427056/IJPhS-74-415-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4ef6/3660867/3061b4f4883d/IJPhS-74-415-g007.jpg

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