Getachew Afewerk, Yilma Zewdu, Abrha Solomon
Department of Pharmaceutics, School of Pharmacy, College of Health Sciences, Mekelle University, P.O. Box 1871, Mekelle, Ethiopia.
Department of Pharmacy, College of Medicine and Health Sciences, Bahir Dar University, P.O. Box 79, Bahir Dar, Ethiopia.
Adv Pharmacol Pharm Sci. 2020 Mar 12;2020:2708063. doi: 10.1155/2020/2708063. eCollection 2020.
Taro Boloso-I (TB1), a newly improved variety, is a potential source of starch with high yield. However, to improve some limitations of the native starches (NS), such as flowability and compactibility, different physical and chemical starch modifications have been employed. Acetylation is one of the chemical modifications which improves the flow and compaction of the NS, which are prerequisite during direct compression (DC) of tablets. Hence, in this study, TB1 starch was acetylated using acetic anhydride and evaluated as an ideal excipient for direct compression. Starch acetates (SA) with a degree of substitution (DS) of 0.072 (SA) and 0.695 (SA) were produced and evaluated. FTIR spectra of the SAs were used to verify the acetylation of the NS. Powder flow evaluation parameters showed significant improvement in the flow properties of the NS following acetylation. In addition, the swelling power, solubility, and compactibility were also improved. Tensile strength (TS) of the tablets comprising SAs only, SA (41.40) and SA (63.43 Kg/cm), was significantly higher than tablets made of the NS (31.96) and Starch 1500® (15.12 Kg/cm). The SAs also showed lower sensitivity towards lubrication than the NS and Starch 1500® as lower lubricant sensitivity ratios were recorded. In addition, tablets comprising the SAs satisfactorily accommodated at least up to 50 % w/w paracetamol-compared to 30 % w/w by Starch 1500®-upon DC processing. The paracetamol tablets comprising SAs also complied with the United States Pharmacopeia specifications for disintegration and dissolution studies. Therefore, taking all the facts into consideration, the SAs could be potential DC excipients in tablet formulations.
新改良品种塔罗博洛索 - I(TB1)是一种高产淀粉的潜在来源。然而,为了改善天然淀粉(NS)的一些局限性,如流动性和可压性,已采用了不同的物理和化学淀粉改性方法。乙酰化是一种化学改性方法,可改善NS的流动性和可压性,这是片剂直接压片(DC)过程中的先决条件。因此,在本研究中,使用乙酸酐对TB1淀粉进行乙酰化,并将其评估为直接压片的理想辅料。制备并评估了取代度(DS)为0.072(SA)和0.695(SA)的淀粉醋酸酯(SA)。利用SA的傅里叶变换红外光谱(FTIR)来验证NS的乙酰化。粉末流动评估参数表明,乙酰化后NS的流动性能有显著改善。此外,溶胀力、溶解度和可压性也得到了改善。仅由SA制成的片剂的抗张强度(TS),SA(41.40)和SA(63.43 Kg/cm),显著高于由NS(31.96)和淀粉1500®(15.12 Kg/cm)制成的片剂。SA对润滑的敏感性也低于NS和淀粉1500®,因为记录的润滑敏感性比率较低。此外,与淀粉1500®在直接压片过程中容纳30% w/w的扑热息痛相比,包含SA的片剂在直接压片过程中令人满意地容纳了至少高达50% w/w的扑热息痛。包含SA的扑热息痛片剂也符合美国药典关于崩解和溶出度研究的规范。因此,综合所有因素考虑,SA可能是片剂配方中潜在的直接压片辅料。