Purpose

Acceptable content uniformity is one of the major challenges in industrial pharmacy especially in low-dose drugs with narrow therapeutic index. Several methods have been proposed for solving this problem. Liquisolid technique is a new promising method that mainly has been used for enhancing solubility rate of drugs. It seems that this method could be able to obtain better distribution of drug and then content uniformity. The purpose of this investigation was to improve content uniformity of fingolimod hydrochloride, which is a low-dose drug with narrow therapeutic index, using liquisolid technique.

Methods

In this study, liquisolid formulations were prepared using PG as nonvolatile solvent and also absolute ethanol as a volatile solvent. The analysis carried out using HPLC method and content uniformity test was done according to the USP guideline.

Results

The results showed that content uniformity was improved in liquisolid method in comparison with classic method. Better distribution was obtained using combination of nonvolatile and volatile solvents.

Conclusion

It seemed that liquisolid method could be used as a promising technique for obtaining acceptable content uniformity in low-dose drugs with narrow therapeutic index such as fingolimod hydrochloride.

中文翻译：

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使用液固技术增强芬戈莫德含量低的窄治疗指数药物的药物含量

目的

可接受的含量均匀性是工业制药业的主要挑战之一，特别是在治疗指数狭窄的低剂量药物中。已经提出了几种解决该问题的方法。液体固体技术是一种新的有前途的方法，主要用于提高药物的溶解度。看来这种方法可以更好地分配药物，然后含量均匀。这项研究的目的是使用液固技术改善盐酸芬戈莫德（一种低剂量，治疗指数狭窄的药物）的含量均匀性。

方法

在这项研究中，使用PG作为非挥发性溶剂以及无水乙醇作为挥发性溶剂制备液状固体制剂。使用HPLC方法进行分析，并根据USP指南进行含量均一性测试。

结果

结果表明，与传统方法相比，液固法提高了含量均匀度。使用非挥发性和挥发性溶剂的组合可获得更好的分布。

结论

似乎可以将液固法用作在治疗指数较窄的低剂量药物（如芬戈莫德盐酸盐）中获得可接受的含量均匀性的有前途的技术。