The influence of drug type on the release profiles from Surelease-coated pellets.
The influence of drug type on the release profiles from Surelease-coated pellets.
复制标题
DOI：
10.1016/s0378-5173(03)00003-6
复制
发表时间：
2003-03
影响因子：
5.8
通讯作者：
F. Sadeghi;J. Ford;A. Rajabi-Siahboomi
中科院分区：
文献类型：
--
作者：
F. Sadeghi;J. Ford;A. Rajabi-Siahboomi
研究了盐酸甲氧氯普胺（一种水溶性阳离子药物）和双氯芬酸钠（一种微溶性阴离子药物）在不同包衣负载下从由乙基纤维素水性分散体（Surelease®）制成的乙基纤维素包衣的小丸中的释放。每种药物的释放速率随着Surelease®包衣负载的增加而降低。然而，尽管双氯芬酸钠的水溶性较低，但在等效包衣负荷下，双氯芬酸钠的释放略快于盐酸甲氧氯普胺。盐酸甲氧氯普胺固化后释放速率的变化更明显，双氯芬酸钠固化后的释放速率低于盐酸甲氧氯普胺。两种药物释放行为之间的差异可能是由于Surelease®中存在的阳离子甲氧氯普胺和阴离子油酸铵之间的相互作用。盐酸甲氧氯普胺的缓慢释放可能是由于药物和油酸铵的难溶性复合物的原位形成。这种复合物，由于其大分子尺寸，可以更缓慢地通过膜扩散，导致盐酸甲氧氯普胺的释放速率降低。这种相互作用也可能解释了药物固化后释放特征的差异。在固化过程中，表面活性剂由于其在热中不稳定的性质，可以转化为其组成组分。固化过程中油酸铵残留量减少，药物与表面活性剂的相互作用降低。然而，相对低的空气体积流速，以及因此在改进的侧通风马内斯蒂塔10中较慢的氨去除也可能影响丸粒的涂覆过程。
The release of metoclopramide hydrochloride (a water-soluble cationic drug) and diclofenac sodium (a sparingly soluble anionic drug) from pellets coated with ethylcellulose from an aqueous ethylcellulose dispersion (Surelease®) at different coating loads was investigated. The release rates of each drug decreased as the coating load of Surelease®increased. However, despite its lower water solubility, diclofenac sodium was released slightly faster than metoclopramide hydrochloride at equivalent coating loads. Changes in the release rates after curing were more pronounced for metoclopramide hydrochloride and the release rates of diclofenac sodium were lower than those of metoclopramide hydrochloride after curing. Differences between the release behaviour of the two drugs were probably due to an interaction between the cationic metoclopramide and the anionic ammonium oleate present in the Surelease®. The slower release of metoclopramide hydrochloride may be due to an in situ formation of a poorly soluble complex of the drug and the ammonium oleate. This complex, because of its large molecular size, may diffuse more slowly through the film, causing a reduction in the release rate of metoclopramide hydrochloride. This interaction may also account for the differences in release characteristics of the drugs after curing. During curing the surfactant, due to its unstable nature in heat, may be converted to its constituent components. The interaction of drug with the surfactant was reduced as the residue of the ammonium oleate decreased during curing. However, a relatively low volume flow rate of air, and therefore, slower removal of ammonia in the modified side-vented Manesty Accela-cota 10 may also have affected the coating process of the pellets.