Purpose

Liqui-Tablet is a dosage form derived from Liqui-Mass technology. It has proven to be a promising approach to improve drug dissolution rate of poorly water-soluble drugs. So far, Liqui-Tablet is feasible for low-dose drugs. In this study, an attempt was made to produce high-dose Liqui-Tablet, whilst maintaining ideal physicochemical properties for ease of manufacturing.

Methods

Liqui-Tablets containing 100 mg of ketoprofen were produced using various liquid vehicles including PEG 200, Span 80, Kolliphor EL, PG, and Tween 85. Investigations that were carried out included saturation solubility test, dissolution test, tomographic study, and typical quality control tests for assessing flowability, particle size distribution, friability, and tablet hardness.

Results

The weight of these Liqui-Tablets was acceptable for swallowing (483.8 mg), and the saturation solubility test showed PEG 200 to be the most suitable liquid vehicle (493 mg/mL). Tests investigating physicochemical properties such as flowability, particle size distribution, friability, and tablet hardness have shown no issue concerning quality control and manufacturability. The drug release test of the best formulation has shown extremely rapid drug release at pH 7.4 (100% after 5 min). At pH 1.2 the drug release was reasonable considering the formulation was yet to be optimized.

Conclusion

Despite the high amount of API and liquid vehicle, it is possible to produce a high-dose dosage form with acceptable size and weight for swallowing using the novel Liqui-Mass technology. This has the potential to diversify the technology by removing the restriction of high dose drug that has been seen in liquisolid technology.

中文翻译：

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使用新型Liqui-Mass技术生产大剂量的Liqui-tablet（酮洛芬100毫克），以增强药物释放

目的

Liqui-Tablet是源自Liqui-Mass技术的剂型。它已被证明是改善水溶性差的药物的药物溶解率的一种有前途的方法。到目前为止，Liqui-Tablet对于低剂量药物是可行的。在这项研究中，试图生产高剂量的液体片剂，同时保持理想的理化性质以易于制造。

方法

使用各种液体媒介物（包括PEG 200，Span 80，Kolliphor EL，PG和Tween 85）生产了包含100 mg酮洛芬的液体片剂。所进行的研究包括饱和溶解度测试，溶出度测试，层析成像研究和典型的质量控制用于评估流动性，粒度分布，脆性和片剂硬度的测试。

结果

这些液体片剂的重量可以吞咽（483.8 mg），并且饱和溶解度测试表明PEG 200是最合适的液体载体（493 mg / mL）。研究诸如流动性，粒度分布，脆性和片剂硬度之类的理化特性的测试没有发现与质量控制和可制造性有关的问题。最佳配方的药物释放测试显示，在pH 7.4下（5分钟后100％），药物释放极快。考虑到尚未优化配方，在pH 1.2时药物释放是合理的。

结论

尽管有大量的API和液体载体，但仍可以使用新颖的Liqui-Mass技术生产具有可接受大小和重量的可吞咽的高剂量剂型。通过消除液体固体技术中出现的高剂量药物的限制，这具有使技术多样化的潜力。