Salarvand Motahareh, Ramezani Vahid, Salarvand Fatemeh, Aref Darabi Zeinab, Akrami Maryam
Department of Pharmaceutics, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran.
Department of Psychiatry, Faculty of Medicine, Arak's University of Medical Sciences, Arak, Iran.
Iran J Pharm Res. 2021 Spring;20(2):183-196. doi: 10.22037/ijpr.2020.112230.13621.
Aimed to improve the dissolution profile of risperidone and increase the compliance of psychotic patients, we designed a fast dissolution tablet (FDT) containing nanoparticles. Risperidone nanoparticles were prepared by the acid-alkali neutralization method, and their size and stability were evaluated. Spray freeze-drying (SFD) process was then employed to fabricate the nanoaggregates using sugars. The physicochemical properties of the dried powders were assessed. Finally, nanoaggregates were compressed into tablets, and their properties were evaluated. The results show that the synergic effect of cremophore EL and hydroxypropyl methyl cellulose E can give rise to the formation of risperidone nanosuspension with the particle size of 188 nm. Moreoevr, it is shown that the fabrication of risperidone nanoaggregate enhanced the drug dissolution and decreased that to 2 min, which is faster than coarse risperidone powder (with dissolution time of 60 min). The formulations of FDT containing 9.5% of sodium starch glycolate and 83.2% microcrystalline cellulose were selected with a disintegration time of less than 30 s and a dissolution time of 10 min. This investigation shows that the preparation of FDT containing nanoparticles using SFD is an easy and feasible method for improving the dissolution profile of many drugs with low solubility.
为改善利培酮的溶出曲线并提高精神病患者的服药依从性，我们设计了一种含纳米颗粒的速溶片（FDT）。采用酸碱中和法制备利培酮纳米颗粒，并对其粒径和稳定性进行评估。然后采用喷雾冷冻干燥（SFD）工艺，用糖类制备纳米聚集体。对干燥粉末的物理化学性质进行评估。最后，将纳米聚集体压制成片剂，并对其性质进行评估。结果表明，聚氧乙烯蓖麻油EL和羟丙基甲基纤维素E的协同作用可促使形成粒径为188 nm的利培酮纳米混悬液。此外，结果表明，利培酮纳米聚集体的制备提高了药物溶出度，溶出时间缩短至2分钟，比粗利培酮粉末（溶出时间为60分钟）更快。选择含9.5%淀粉乙醇酸钠和83.2%微晶纤维素的FDT制剂，崩解时间小于30秒，溶出时间为10分钟。本研究表明，采用SFD制备含纳米颗粒的FDT是改善许多低溶解度药物溶出曲线的一种简便可行的方法。
