Objective

One of the main problems with NSAIDs is the dosing frequency, which leads to patients’ noncompliance. To overcome this, fabrication of sustained release formulation of the drug is considered a well-reputed technique. The present study aimed to develop sustained release formulation of a model drug aceclofenac through the new liquisolid technique.

Methods

Liquisolid powder prepared using glycerin as the liquid vehicle was subjected to pre-compression evaluation, including bulk and tapped densities, Carr’s compressibility index, Hausner’s ratio, angle of slide, FTIR, and atomic force microscopy (AFM). Differential scanning calorimetry (DSC) and X-ray crystallography studies were investigated for any complex formation between drug and excipients, as well as crystal form alterations during the manufacturing process. Powders were compressed into tablets and quality control tests; in vitro dissolution test and storage stability studies were carried out.

Results

The release of aceclofenac was at a predetermined rate and followed zero-order kinetic models. AFM confirmed the surface morphology and particles were well adsorbed by the carrier material. FTIR and DSC studies suggested no drug–excipients interaction and the drugs were found in an amorphous form, which was confirmed through XRD. Upon storage at the given conditions of humidity and temperature, the formulation was found stable.

Conclusion

The study proved that liquisolid technique can be used successfully to develop a sustained release formulation.

Graphical Abstract

中文翻译：

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Liquisolid技术：开发载有醋氯芬酸的Eudragit L-100和基于RS-100的缓释片剂的新型工具

目的

非甾体抗炎药的主要问题之一是给药频率，这导致患者不依从。为了克服这个问题，制造药物的缓释制剂被认为是一种声誉卓著的技术。本研究旨在通过新的液固技术开发模型药物醋氯芬酸的缓释制剂。

方法

使用甘油作为液体载体制备的液态固体粉末经过预压缩评估，包括堆积密度和振实密度，Carr可压缩指数，Hausner比，滑动角，FTIR和原子力显微镜（AFM）。进行了差示扫描量热法（DSC）和X射线晶体学研究，研究了药物与赋形剂之间的任何复杂形成以及制造过程中的晶型变化。将粉末压制成片剂并进行质量控制测试；进行了体外溶出试验和储存稳定性研究。

结果

醋氯芬酸的释放以预定速率且遵循零级动力学模型。AFM证实了表面形态，并且颗粒被载体材料很好地吸附。FTIR和DSC研究表明没有药物与赋形剂的相互作用，并且发现药物为无定形形式，这通过XRD得以证实。在给定的湿度和温度条件下储存后，发现该制剂是稳定的。

结论

研究证明，液固技术可成功用于开发缓释制剂。

图形概要