Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University, Amman 11931, Jordan.
Technical Competence Center, JRS PHARMA GmbH & Co. KG, 73494 Rosenberg, Germany.
Int J Pharm. 2021 May 15;601:120512. doi: 10.1016/j.ijpharm.2021.120512. Epub 2021 Mar 22.
Alginates are biopolymers that have been investigated for their use in food and medical fields. Minimal information is available regarding their potential application as tablet superdisintegrants. Here we studied the disintegration action of sodium alginate (SA), calcium alginate (CA) and alginic acid (AA). Initially, we characterised the swelling and wicking abilities and the disintegration mechanism of pure disintegrants. We found that the liquid uptake of both CA and AA is more swelling-driven in phosphate buffer and more wicking-driven in hydrochloric acid and water. CA acts by shape-recovery, AA by a combination of swelling and shape-recovery mechanisms. SA cannot be used as disintegrant due to gelling. In the second part of the paper, the disintegration time of formulations with different physico-chemical properties and different alginate concentrations (i.e. 4% and 10%) was measured, thus delivering a direct readout for the ranges of application of alginates as tablets disintegrants. The main observations are: i) CA and AA often provide very rapid disintegration, similarly to the superdisintegrants used as controls; ii) the action of CA is more susceptible to the medium conditions than AA; iii) CA underperforms in hard tablets containing a binder; iv) both CA and AA have slightly slower disintegration than other superdisintegrants in tablets containing a hydrophobic component. While the suitability of CA as a disintegrant is formulation- and medium- dependent, AA appears as a promising tablet superdisintegrant, particularly for the development of uncomplicated hydrophilic formulations for the nutraceutical and supplement industry, where natural ingredients are favoured.
藻酸盐是一种生物聚合物，已被研究用于食品和医疗领域。关于其作为片剂超级崩解剂的潜在应用，信息很少。在这里，我们研究了海藻酸钠（SA）、海藻酸钙（CA）和海藻酸（AA）的崩解作用。首先，我们对纯崩解剂的溶胀和吸液能力以及崩解机制进行了表征。我们发现，在磷酸盐缓冲液中，CA 和 AA 的液体吸收主要是溶胀驱动的，而在盐酸和水中，主要是吸液驱动的。CA 通过形状恢复起作用，AA 通过溶胀和形状恢复机制的组合起作用。由于凝胶化，SA 不能用作崩解剂。在本文的第二部分，我们测量了具有不同物理化学性质和不同藻酸盐浓度（即 4%和 10%）的配方的崩解时间，从而为藻酸盐作为片剂崩解剂的应用范围提供了直接的读数。主要观察结果是：i）CA 和 AA 通常提供非常快速的崩解，类似于用作对照的超级崩解剂；ii）CA 的作用比 AA 更容易受到介质条件的影响；iii）CA 在含有粘合剂的硬片中表现不佳；iv）CA 和 AA 在含有疏水性成分的片剂中的崩解速度略慢于其他超级崩解剂。虽然 CA 作为崩解剂的适用性取决于配方和介质，但 AA 似乎是一种有前途的片剂超级崩解剂，特别是对于开发用于营养保健品和补充剂行业的简单亲水性配方，在这些行业中，天然成分更受欢迎。
