包含在直接压片中的赋形剂的两个关键性质是流动性和密实性。糯米淀粉(GRS)流动性差,这限制了它在直接压片中的使用。本研究旨在通过共沉淀方法从GRS产生具有改善的流动性的多功能直接压缩赋形剂(填充剂粘合剂崩解剂)。研究了共沉淀GRS(cpGRS)的理化和药学特性。生产cpGRS(0.43M氢氧化钠溶液,7.09%PVPK30,14.02%碳酸钙,95分钟的混合时间和6.97的pH)导致68.80%的产率,良好的流动性,可接受的片剂强度,快速解体。cpGRS的FT-IR光谱显示关键峰无明显位移,这表明cpGRS内没有化学相互作用。X射线衍射图也没有明显变化,表明GRS颗粒,碳酸钙,和PVPK30组分在共沉淀过程中保持不变。当使用扑热息痛作为模型药物时,cpGRS还表现出50%的稀释能力。当cpGRS与多潘立酮或盐酸普萘洛尔组合时,它显示出比物理混合物更好的变形能力。尽管cpGRS对润滑剂很敏感,硬度和拉伸强度高于一般用途的片剂的普通强度。与物理混合物相比,预糊化淀粉和可直接压缩的碳酸钙,结果表明,两种模型药物的cpGRS片都通过了脆碎度测试,表现出最好的崩解性质,为普萘洛尔提供了最快和最高的药物释放曲线,并改善了多潘立酮的药物释放曲线。对于普萘洛尔-cpGRS片剂,不同pH下的溶出介质不影响溶出曲线。对于多潘立酮-cpGRS片剂,溶出介质的pH确实影响片剂的溶出曲线。这是根据API溶解度。这些结果表明,cpGRS是一种优异的多功能,即填料,活页夹,和适用于直接压片的崩解剂赋形剂。主要成分是天然的。制备方法简单,快,高效。这种方法不产生有害废物,只需要基本设备,和负担得起的反应物和设备。
Two key properties of excipients for inclusion in direct compression tablets are flowability and compactibility. Glutinous rice starch (GRS) has poor flowability, which limits its use in direct compression tablets. This study aimed to create a multifunctional direct compression excipient (filler binder disintegrant) with improved flowability from GRS by the co-precipitation method. The physicochemical and pharmaceutical properties of the co-precipitated GRS (cpGRS) were investigated. The optimum conditions for producing cpGRS (0.43 M sodium hydroxide solution, 7.09% PVP K30, 14.02% calcium carbonate, 95 min of mixing time and pH of 6.97) resulted in 68.80% yield, fair to good flowability, acceptable tablet strength, and fast disintegration. The FT-IR spectra of cpGRS showed no significant shifts in the key peaks, which indicates that there was an absence of chemical interactions within cpGRS. X-ray diffractograms also showed no significant changes, indicating that the GRS granules, calcium carbonate, and PVP K30 components remained unaltered during co-precipitation. cpGRS also demonstrated a dilution capacity of 50% when paracetamol was used as model drug. When cpGRS was combined with domperidone or propranolol hydrochloride it showed a better deformation capability than the physical mixtures. Although cpGRS was sensitive to lubricant, the hardness and tensile strength were higher than common strength for general purpose use in tablets. When compared to the physical mixture, pregelatinized starch and directly compressible calcium carbonate, the results showed that cpGRS tablets of both model drugs passed the friability test, demonstrated the best disintegration property, provided the fastest and highest drug release profile for propranolol, and improved the drug release profile for domperidone. For propranolol-cpGRS tablets, dissolution medium at different pH did not affect the dissolution profile. For domperidone-cpGRS tablets, the pH of dissolution medium did affect the dissolution profile of the tablets. This was according to the API solubility. These results reveal that cpGRS is an excellent multifunctional i.e., filler, binder, and disintegrant excipient suitable for direct compression tablets. The main component is natural. The preparation method is simple, quick, and efficient. This method does not produce harmful waste and requires only basic equipment, and affordable reactants and devices.