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左甲状腺素钠在固体二元体系中的稳定性和相容性研究——仪器筛选

Stability and Compatibility Studies of Levothyroxine Sodium in Solid Binary Systems-Instrumental Screening.

作者信息

Ledeți Ionuț, Romanescu Mirabela, Cîrcioban Denisa, Ledeți Adriana, Vlase Gabriela, Vlase Titus, Suciu Oana, Murariu Marius, Olariu Sorin, Matusz Petru, Buda Valentina, Piciu Doina

机构信息

Department of Pharmacy I, Faculty of Pharmacy, Victor Babes University of Medicine and Pharmacy, 300011 Timișoara, Romania.

Research Centre for Thermal Analysis in Environmental Problems, West University of Timișoara, 300115 Timișoara, Romania.

出版信息

Pharmaceutics. 2020 Jan 10;12(1):58. doi: 10.3390/pharmaceutics12010058.

DOI:10.3390/pharmaceutics12010058
PMID:31936742
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7022666/
Abstract

The influence of excipients on the stability of sodium levothyroxine pentahydrate (LTSS) under ambient conditions and thermal stress was evaluated. Since LTSS is a synthetic hormone with a narrow therapeutic index, the interactions of LTSS with excipients can lead to a drastic diminution of therapeutic activity. Ten commonly used pharmaceutical excipients with different roles in solid formulations were chosen as components for binary mixtures containing LTSS, namely, starch, anhydrous lactose, D-mannitol, D-sorbitol, gelatin, calcium lactate pentahydrate, magnesium stearate, methyl 2-hydroxyethyl cellulose (Tylose), colloidal SiO (Aerosil) and talc. As investigational tools, universal attenuated total reflectance- Fourier transform infrared spectroscopy UATR-FTIR spectroscopy and thermal analysis were chosen and used as follows: UATR-FTIR spectra were drawn up for samples kept under ambient conditions, while thermoanalytical tools (TG/DTG/HF data) were chosen to evaluate the inducing of interactions during thermal stress. The corroboration of instrumental results led to the conclusion that LTSS is incompatible with lactose, mannitol and sorbitol, and these excipients should not be considered in the development of new generic solid formulations.

摘要

评估了辅料在环境条件和热应力下对五水合左甲状腺素钠（LTSS）稳定性的影响。由于LTSS是一种治疗指数狭窄的合成激素，LTSS与辅料的相互作用可导致治疗活性急剧降低。选择了在固体剂型中具有不同作用的十种常用药用辅料作为含LTSS二元混合物的成分，即淀粉、无水乳糖、D - 甘露醇、D - 山梨醇、明胶、五水合乳酸钙、硬脂酸镁、甲基2 - 羟乙基纤维素（泰勒多糖）、胶体二氧化硅（气相二氧化硅）和滑石粉。作为研究工具，选用了通用衰减全反射傅里叶变换红外光谱法（UATR - FTIR光谱法）和热分析，并按如下方式使用：绘制在环境条件下保存的样品的UATR - FTIR光谱，同时选择热分析工具（TG/DTG/HF数据）来评估热应力期间相互作用的诱导情况。仪器结果的证实得出结论，LTSS与乳糖、甘露醇和山梨醇不相容，在开发新的通用固体剂型时不应考虑这些辅料。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/cd7c6ad5b8e1/pharmaceutics-12-00058-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/edb99f2cac59/pharmaceutics-12-00058-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/824cb93c4ea5/pharmaceutics-12-00058-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/5dcf3331ece9/pharmaceutics-12-00058-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/cd7c6ad5b8e1/pharmaceutics-12-00058-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/edb99f2cac59/pharmaceutics-12-00058-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/824cb93c4ea5/pharmaceutics-12-00058-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/5dcf3331ece9/pharmaceutics-12-00058-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f3a3/7022666/cd7c6ad5b8e1/pharmaceutics-12-00058-g004.jpg

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