降胆固醇药物与氧化镁复合单一混悬液的化学稳定性研究。

IF 1.2 Q4 PHARMACOLOGY & PHARMACY
Ginjiro Kato, Hidemichi Mitome, Yusura Miyauchi, Syu Takeda, Yoshito Toyota, Noriaki Hidaka, Mamoru Tanaka, Kazuki Akira
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引用次数: 0

摘要

背景:吞咽固体药物困难是一个常见的问题,尤其是老年人,因为吞咽功能下降,也被称为吞咽困难。针对这种功能障碍的患者,一种简单的悬浮法已经被开发出来,并在日本临床广泛应用。这种方法是用温水将固体药物分解并悬浮。然而,关于多种配方的简单共混悬液的药物稳定性的信息很少,特别是包括酸性或碱性配方。在本研究中,研究了典型降胆固醇药物与碱性氧化镁(MgO)在简单共悬液中的化学稳定性。碱性氧化镁在日本常被用作泻药或抗酸药。方法:将降胆固醇药物(1片)加入或不加入氧化镁(MgO)于55℃温水中浸泡,室温静置10 min或5 h,用高效液相色谱法分析制备的混悬液。利用核磁共振谱和质谱对降解产物进行了结构分析。结果:在与MgO共悬的情况下,阿托伐他汀和普伐他汀没有明显的降解,而瑞舒伐他汀的共悬5 h后回收率明显下降。而与MgO共悬的辛伐他汀和依泽替米贝则分别部分降解为辛伐他汀酸和吡喃化合物。结论:阿托伐他汀、普伐他汀、瑞舒伐他汀与MgO简单共混剂是可行的,但瑞舒伐他汀片不宜长时间浸泡。此外,不建议将辛伐他汀或依折替贝与MgO一起停用,因为它们会部分降解。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

A study on the chemical stability of cholesterol-lowering drugs in concomitant simple suspensions with magnesium oxide.

A study on the chemical stability of cholesterol-lowering drugs in concomitant simple suspensions with magnesium oxide.

A study on the chemical stability of cholesterol-lowering drugs in concomitant simple suspensions with magnesium oxide.

A study on the chemical stability of cholesterol-lowering drugs in concomitant simple suspensions with magnesium oxide.

Background: Difficulty in taking solid medicines is a common issue particularly for the elderly because of a decline in swallowing function, also known as dysphagia. For patients with such a dysfunction, a simple suspension method, in which solid medicines are disintegrated and suspended using warm water, has been developed and widely used in Japanese clinical settings. However, there is little information on drug stability in the simple co-suspension of multiple formulations especially including acidic or alkaline ones. In this study, the chemical stability of typical cholesterol-lowering drugs was investigated in a simple co-suspension with alkaline magnesium oxide (MgO) which is frequently used as a laxative or antacid in Japan.

Methods: A cholesterol-lowering drug (one tablet) was soaked with or without MgO in warm water (55°C), and the vessel was left at room temperature for 10 min or 5 h. The suspensions prepared were then analyzed by high-performance liquid chromatography. Degradation products were analyzed by nuclear magnetic resonance spectroscopy and mass spectrometry for the structural elucidation.

Results: In the simple co-suspension with MgO, no significant degradation was observed for atorvastatin or pravastatin, while a significant decrease of the recovery from the co-suspension was observed for rosuvastatin after 5 h. On the other hand, simvastatin and ezetimibe co-suspended with MgO were partially degraded to simvastatin acid and a pyran compound, respectively.

Conclusions: A simple co-suspension with MgO is feasible for atorvastatin, pravastatin, and rosuvastatin, although the rosuvastatin tablet should not be left soaking for a long time. Further it is inadvisable to suspend simvastatin or ezetimibe together with MgO because of their partial degradation.

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来源期刊
CiteScore
1.80
自引率
0.00%
发文量
29
审稿时长
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