聚合物膜厚对流化床包衣颗粒药物释放的影响以及预期的工艺和产品控制。

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY
Marcel Langner, Florian Priese, Bertram Wolf
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引用次数: 0

摘要

背景/目的:涂层药物颗粒在硬明胶胶囊中得到广泛应用。在异质颗粒中,药物被分层包覆在核心颗粒上。涂层通常用于产生缓释或肠道涂层:本研究中,药物颗粒上聚合物包衣层的厚度与药物释放动力学相关:结果:需要回答的问题是,当达到与预期药物释放相关的包衣层厚度时,是否有可能停止包衣过程。在配有 Wurster 入口的流化床设备中,惰性颗粒首先被苯甲酸钠包衣,然后被不同量的水不溶性聚丙烯酸酯包衣。通过测量粒度和层厚度,利用过程分析技术对整个过程进行在线控制。研究了体外苯甲酸钠的释放情况,通过不同的标准模型对数据进行了线性化处理,并与聚丙烯酸酯层厚度进行了比较。随着聚丙烯酸酯层厚度的增加,释放率也随之降低。影响释放的几个过程的叠加导致释放曲线近似于一阶动力学。包衣层厚度与确定的药物释放曲线相对应:结论:通过包衣工艺控制和包衣层厚度测量,可以制造出具有预期药物释放效果的包衣药物颗粒。有必要对不同配方进行初步研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Influence of Polymer Film Thickness on Drug Release from Fluidized Bed Coated Pellets and Intended Process and Product Control.

Background/objectives: Coated drug pellets enjoy widespread use in hard gelatine capsules. In heterogeneous pellets, the drug substance is layered onto core pellets. Coatings are often applied to generate a retarded release or an enteric coating.

Methods: In the present study, the thickness of a polymer coating layer on drug pellets was correlated to the drug release kinetics.

Results: The question should be answered whether it is possible to stop the coating process when a layer thickness referring to an intended drug release is achieved. Inert pellets were first coated with sodium benzoate and second with different amounts of water insoluble polyacrylate in a fluidized bed apparatus equipped with a Wurster inlet. The whole process was controlled in-line and at-line with process analytical technology by the measurement of the particle size and the layer thickness. The in-vitro sodium benzoate release was investigated, and the data were linearized by different standard models and compared with the polyacrylate layer thickness. With increasing polyacrylate layer thickness the release rate diminishes. The superposition of several processes influencing the release results in release profiles corresponding approximately to first order kinetics. The coating layer thickness corresponds to a determined drug release profile.

Conclusions: The manufacturing of coated drug pellets with intended drug release is possible by coating process control and layer thickness measurement. Preliminary investigations are necessary for different formulations.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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