Vraníková Barbora, Gajdziok Jan, Doležel Petr
a Department of Pharmaceutics, Faculty of Pharmacy , University of Veterinary and Pharmaceutical Sciences , Palackeho Trida 1/3 , Brno , Czech Republic.
Pharm Dev Technol. 2017 Mar;22(2):138-147. doi: 10.3109/10837450.2015.1089900. Epub 2015 Sep 24.
The preparation of liquisolid systems (LSS) represents a promising method for enhancing a dissolution rate and bioavailability of poorly soluble drugs. The release of the drug from LSS tablets is affected by many factors, including the disintegration time.
The evaluation of differences among LSS containing varying amounts and types of commercially used superdisintegrants (Kollidon® CL-F, Vivasol® and Explotab®).
LSS were prepared by spraying rosuvastatin solution onto Neusilin® US2 and further processing into tablets. Varying amounts of superdisintegrants were used and the differences among LSS were evaluated. The multiple scatter plot method was used to visualize the relationships within the obtained data.
All disintegrants do not showed negative effect on the flow properties of powder blends. The type and concentration of superdisintegrant had an impact on the disintegration time and dissolution profiles of tablets. Tablets with Explotab® showed the longest disintegration time and the smallest amount of released drug. Fastest disintegration and dissolution rate were observed in tablets containing Kollidon® CL-F (≥2.5% w/w). Also tablets with Vivasol® (2.5-4.0% w/w) showed fast disintegration and complete drug release.
Kollidon® CL-F and Vivasol® in concentration ≥2.5% are suitable superdisintegrants for LSS with enhanced release of drug.
液固系统（LSS）的制备是提高难溶性药物溶出速率和生物利用度的一种有前景的方法。药物从LSS片剂中的释放受多种因素影响，包括崩解时间。
评估含有不同用量和类型市售超级崩解剂（交联聚维酮CL-F、维法索尔和羧甲基淀粉钠）的LSS之间的差异。
通过将瑞舒伐他汀溶液喷雾到二号硅酸镁铝上制备LSS，并进一步加工成片剂。使用了不同用量的超级崩解剂，并评估了LSS之间的差异。采用多元散射图方法直观呈现所得数据之间的关系。
所有崩解剂对粉末混合物的流动性均未显示负面影响。超级崩解剂的类型和浓度对片剂的崩解时间和溶出曲线有影响。含有羧甲基淀粉钠的片剂崩解时间最长，药物释放量最小。在含有交联聚维酮CL-F（≥2.5% w/w）的片剂中观察到最快的崩解和溶出速率。含有维法索尔（2.5 - 4.0% w/w） 的片剂也显示出快速崩解和药物完全释放。
浓度≥2.5%的交联聚维酮CL-F和维法索尔是适用于药物释放增强的LSS的超级崩解剂。
