Development and optimization of guaifenesin sustained release mini-tablets for adult and geriatric patients

<b>Aim:</b> The main aim of this study was to formulate and optimize sustained release mini-tablets of guaifenesin. <b>Materials &amp; methods:</b> Guaifenesin granules were successfully prepared using different blend ratios of carnauba wax to drug by melt granulation method. The properties of granules were further modified by combining them with ethyl cellulose. The obtained granules were then mixed and compressed into mini-tablets using a tablet press machine. The resulting mini-tablets were characterized in terms of weight, thickness, hardness, drug content and <i>in vitro</i> drug release. <b>Results:</b> Mini-tablets with 1:6 carnauba wax to drug ratio showed superior physicochemical characteristics, releasing about 100.03% of guaifenesin over 8 h. Ethyl cellulose offers a great potential to accurately control drug release from mini-tablets. <b>Conclusion:</b> The prepared mini-tablets seem to be a very promising alternative to guaifenesin conventional formulations and can be used in adults and elderly people. Guaifenesin granules were formulated using different blend ratios of carnauba wax to drug by melt granulation method and compressed into mini-tablets. In mini-tablets, EC can be used as a taste masking and modified release agent. Guaifenesin mini-tablets exhibited acceptable hardness, content, weight, thickness and erosion. Mini-tablets comprising EC were particularly suitable to release guaifenesin over 8 h time period. Guaifenesin mini-tablets seem to be a very promising alternative to the guaifenesin conventional formulations and can be used in adult and elderly people.

<b>研究目的：</b>本研究的核心目标为处方开发并优化愈创甘油醚（guaifenesin）的缓释微片。<b>材料与方法：</b>采用熔融制粒法，按照巴西棕榈蜡（carnauba wax）与药物的不同配比，成功制备愈创甘油醚颗粒；通过加入乙基纤维素（ethyl cellulose）对所得颗粒的性质进行进一步调控。随后将制备得到的颗粒混合均匀，利用压片机压制成微片，并对所得微片开展多项表征，包括重量、厚度、硬度、药物含量以及<i>in vitro</i>体外药物释放行为。<b>研究结果：</b>巴西棕榈蜡与药物配比为1:6的微片展现出更优异的理化性质，可在8小时内累计释放约100.03%的愈创甘油醚；乙基纤维素可精准调控微片的药物释放行为，具备良好应用潜力。<b>结论：</b>本研究制备的愈创甘油醚缓释微片相较于传统愈创甘油醚制剂具备极佳的应用前景，可适用于成人及老年人群。本研究通过熔融制粒法，按照不同巴西棕榈蜡与药物配比制备愈创甘油醚颗粒并压制成微片；在微片体系中，EC可同时作为掩味剂与缓释调节剂。愈创甘油醚微片的硬度、含量、重量、厚度及体外侵蚀特性均符合可接受标准。添加EC的微片尤其适用于8小时内的愈创甘油醚持续释放。综上，愈创甘油醚微片相较于传统愈创甘油醚制剂具备极佳的应用前景，可安全用于成人及老年人群。