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Synthesis of novel superdisintegrants for pharmaceutical tableting based on functionalized nanocellulose hydrogels
International Journal of Biological Macromolecules ( IF 7.7 ) Pub Date : 2020-11-26 , DOI: 10.1016/j.ijbiomac.2020.11.173
Shabnam Sheikhy , Ali Akbar Safekordi , Marjan Ghorbani , Khosro Adibkia , Hamed Hamishehkar

Superdisintegrants have an important function in Fast dissolving tablets (FDT). It's believed that an increase in surface to the mass (size reduction) can enhance their performance. Due to the obligation of pharmaceutical excipients being in GRAS (generally recognized as safe) list, we've devoted our research to modify one of the routinely used and important natural polymer, cellulose, as superdisintegrant. Nanocrystalline cellulose (NCC) was extracted from microcrystalline cellulose (MCC) via the sulfuric acid hydrolysis process. NCC derivatives have been synthesized by Itaconic acid/Hydroxyethyl methacrylate (IA/HEMA) via maleic anhydride (MA) to acquire unique swellability properties in to achieve superabsorbent cellulose-based nano hydrogel with the cross-linking system. The disintegration performance of prepared tablets was compared with tablets composed of sodium starch glycolate (SSG) and MCC as positive and negative controls. The results show that the disintegration time of tablets formulated with synthesized modified NCC (m-NCC) decreased dramatically compared to other disintegrants. The dissolution analysis showed suitable condition for complete drug release in a shorter time. The in vitro cytotoxic experiments proved the biocompatibility of newly synthesized superdisintegrant. The dissolution Analysis findings suggest that our developed novel superdisintegrant paves the way for the formulation of fast dissolving tablets containing rapidly acting medicines such as zolpidem.



中文翻译:

基于功能化纳米纤维素水凝胶的新型药物超崩解剂的合成

超崩解剂在速溶片剂(FDT)中具有重要作用。可以认为,增加表面质量(减小尺寸)可以提高其性能。由于药用赋形剂必须列入GRAS(通常被认为是安全的)清单,因此我们致力于研究,以将一种常用且重要的天然聚合物纤维素作为超级崩解剂进行修饰。通过硫酸水解工艺从微晶纤维素(MCC)中提取出纳米晶纤维素(NCC)。衣康酸/甲基丙烯酸羟乙酯(IA / HEMA)通过顺丁烯二酸酐(MA)合成了NCC衍生物,以获得独特的溶胀性,从而实现了具有交联体系的超吸收性纤维素纳米水凝胶。将制备的片剂的崩解性能与由乙醇酸淀粉钠(SSG)和MCC组成的片剂作阳性对照和阴性对照进行比较。结果表明,与其他崩解剂相比,使用合成改良NCC(m-NCC)配制的片剂的崩解时间显着减少。溶出度分析显示了在较短时间内完全释放药物的合适条件。体外细胞毒性实验证明了新合成的超级崩解剂的生物相容性。溶出度分析结果表明,我们开发的新型超级崩解剂为配制含有速效药物(如唑吡坦)的速溶片剂铺平了道路。结果表明,与其他崩解剂相比,使用合成改良NCC(m-NCC)配制的片剂的崩解时间显着减少。溶出度分析显示了在较短时间内完全释放药物的合适条件。体外细胞毒性实验证明了新合成的超级崩解剂的生物相容性。溶出度分析结果表明,我们开发的新型超级崩解剂为配制含有速效药物(如唑吡坦)的速溶片剂铺平了道路。结果表明,与其他崩解剂相比,使用合成改良NCC(m-NCC)配制的片剂的崩解时间显着减少。溶出度分析显示了在较短时间内完全释放药物的合适条件。体外细胞毒性实验证明了新合成的超级崩解剂的生物相容性。溶出度分析结果表明,我们开发的新型超级崩解剂为配制含有速效药物(如唑吡坦)的速溶片剂铺平了道路。体外细胞毒性实验证明了新合成的超级崩解剂的生物相容性。溶出度分析结果表明,我们开发的新型超级崩解剂为配制含有速效药物(如唑吡坦)的速溶片剂铺平了道路。体外细胞毒性实验证明了新合成的超级崩解剂的生物相容性。溶出度分析结果表明,我们开发的新型超级崩解剂为配制包含速效药物(如唑吡坦)的速溶片剂铺平了道路。

更新日期:2020-11-27
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