羟丙基甲基纤维素的理化性质对富马酸喹硫平缓释基质片剂释放的影响

IF 4.3 2区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY BMC Chemistry Pub Date : 2024-11-07 DOI:10.1186/s13065-024-01311-2
Takwa E. Ellakwa, Ahmad S. Abu-Khadra, Doha El-Sayed Ellakwa
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引用次数: 0

摘要

富马酸喹硫平是一种典型的抗精神病药物,半衰期短,仅为 6 小时,每天多次给药。本研究将开发一种用于控制富马酸喹硫平给药的共聚物。为了防止副作用并提高患者的依从性,羟丙基甲基纤维素 K15M(HPMC K15M)被添加到富马酸喹硫平口服缓释片的配方中,浓度为 10-30%。采用了一系列分析方法来确定所制备水凝胶的特性,包括傅立叶变换红外光谱法、差示扫描量热法、X射线衍射法和扫描电子显微镜。在两种不同的 pH 值(1.2 和 6.8)下,进行了溶胀和释放研究。研究人员使用了多种释放动力学模型来研究药物释放机制。富马酸喹硫平制备的水凝胶采用非菲克扩散机制释放药物。研究发现,增加 HPMC K15M 的用量可增加溶胀。与其他批次(10-20%)相比,HPMC K15M 含量为 30% 的片剂在溶解 20 小时后具有更好的释放曲线。由于有效基质复合物在水中的溶解度有限,药物以稳定的速度通过凝胶体层扩散,而不是快速溶解。
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Influence of physico-chemical properties of hydroxypropyl methylcellulose on quetiapine fumarate release from sustained release matrix tablets

Quetiapine fumarateis a typical antipsychotic with a short half-life of 6 h and is administered multiple times daily. In this study, a copolymer for controlled delivery of quetiapine fumarate will be developed. In order to prevent side effects and improve patient compliance, hydroxypropyl methylcellulose K15M (HPMC K15M) was included in the formulation of the quetiapine fumarate oral sustained-release tablets at a concentration of 10–30%. A series of analytical methods were used to determine the characteristics of the prepared hydrogels, including Fourier transform-infrared spectroscopy, Differential scanning calorimetry, X-ray diffraction, and Scanning electron microscope. At two different pH values (1.2 and 6.8), swelling and release studies were conducted. A variety of release kinetic models was used to study drug release mechanisms. A non-Fickian diffusion mechanism released hydrogels prepared from quetiapine fumarate. It was found that swelling was increased by increasing the amount of HPMC K15M. Compared to the other batches (10–20%), the produced tablets with 30% HPMC K15M content had a better release profile after 20 h of dissolution. Because of the effective matrix complex’s limited solubility in water, the drug diffuses through the gel layer at a steady rate rather than dissolving quickly.

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来源期刊
BMC Chemistry
BMC Chemistry Chemistry-General Chemistry
CiteScore
5.30
自引率
2.20%
发文量
92
审稿时长
27 weeks
期刊介绍: BMC Chemistry, formerly known as Chemistry Central Journal, is now part of the BMC series journals family. Chemistry Central Journal has served the chemistry community as a trusted open access resource for more than 10 years – and we are delighted to announce the next step on its journey. In January 2019 the journal has been renamed BMC Chemistry and now strengthens the BMC series footprint in the physical sciences by publishing quality articles and by pushing the boundaries of open chemistry.
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