Multifunctional Properties of Co-processed Dioscorea rotundata Starch and Abelmoschus esculentus Fruit Gum in Direct Compression of Metronidazole Tablets

O. Olayemi, J. John, Rashidat Abdullahi, C. Isimi
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Abstract

Background: Co-processing is a process that manipulates available excipients to produce better functional excipients. Objectives: This study aims to prepare a co-processed excipient from starch extracted from Dioscorea rotundata (WYS) and gum extracted from pods of Abelmoschus esculentus fruit (OKG). Methods: The co-processed excipients (CYG) were prepared by co-fusing WYS and OKG at concentrations of 99:1, 97:3, 95:5 to produce CYG1, CYG3, and CYG5, respectively. Then, they were evaluated for their flow and swelling properties. Metronidazole tablets (MT1, MT3, and MT5) were prepared by direct compression. Similarly, tablets containing reference excipients of CombiLac® (MTC) and Prosolv® (MTP) were prepared. The tablets were evaluated for uniformity of weight, crushing strength, friability, disintegration time, and in vitro release. Fourier Transform Infra-Red (FTIR) was used to monitor the interaction between the excipients and metronidazole. Results: CYG1, CYG3, and CYG5 have good flow; their swelling profile was between 170% and 200%, more than WYS (80%). FTIR spectra showed no interaction between the excipients and metronidazole. The crushing strength-friability ratio was 42.03>39.65>25.63 for MT3, MT5, and MT1, respectively. MT5 had a longer disintegration time (63.87 s) than MT1 and MT3, which were similar to that of MTC; however, MTP had the longest disintegration time (111.50 s). The disintegration efficiency ratio showed that CYG1 and CYG3 have better disintegration properties than Prosolv®. All the co-processed excipients produced robust tablets comparable to those of CombiLac®. Conclusion: CYG can be exploited as a multifunctional excipient in preparing oral tablet formulations.
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直接压缩甲硝唑片剂中圆薯蓣淀粉与沙棘果胶共加工的多功能特性
背景:协同加工是一个过程,操纵现有的辅料,以生产更好的功能辅料。目的:以圆形薯蓣(Dioscorea rotundata, WYS)淀粉为原料,与香豆(Abelmoschus esculentus, OKG)果荚胶为原料,制备共加工辅料。方法:将WYS和OKG按99:1、97:3、95:5的浓度共熔制备共加工辅料(CYG),分别得到CYG1、CYG3和CYG5。然后,评估它们的流动和膨胀性能。采用直接加压法制备甲硝唑片MT1、MT3、MT5。同样,制备了含有参比辅料CombiLac®(MTC)和Prosolv®(MTP)的片剂。对其重量均匀性、抗压强度、脆性、崩解时间和体外释放度进行了评价。采用傅里叶变换红外光谱(FTIR)监测辅料与甲硝唑的相互作用。结果:CYG1、CYG3、CYG5血流良好;肿胀分布在170% ~ 200%之间,高于WYS(80%)。FTIR光谱显示辅料与甲硝唑无相互作用。MT3、MT5和MT1的破碎强度-脆性比分别为42.03>39.65>25.63。MT5的崩解时间(63.87 s)较MT1和MT3长,与MTC相似;而MTP的崩解时间最长(111.50 s),崩解效率比表明CYG1和CYG3的崩解性能优于Prosolv®。所有协同加工的赋形剂生产出与CombiLac®相当的坚固片剂。结论:CYG可作为一种多功能赋形剂用于口服片剂的制备。
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