Military Pharmacy, Indonesia Defense University, Sentul, Bogor, Indonesia.
Int J Pharm Compd. 2024 Sep-Oct;28(5):432-439.
The vital regulatory role of estradiol in diverse physiological systems, encompassing the menstrual cycle, cardiovascular, neurologic, skeletal, and vascular systems, underscores its importance. Consequently, this compound is frequently incorporated into diverse pharmaceutical formulations, particularly those in tablet form. Typical inactive ingredients used in estradiol tablet formulations include lactose monohydrate, magnesium stearate, microcrystalline cellulose, and sodium starch glycolate. Chitosan, recognized as a novel excipient, is emerging as a promising alternative to microcrystalline cellulose (MCC). In contrast to MCC, chitosan exhibits noteworthy properties, such as excellent solubility in aqueous solutions, a pleasant odor, superdisintegrant effects, increased porosity, and enhanced liquid absorption. The utilization of chitosan as a tablet disintegrant not only enhances tablet bioavailability but also facilitates the formulation of water-soluble tablet formulations and augments cell penetration in nanoparticle chitosan without any chitosan-estradiol interaction. This article will conduct an in-depth examination of the characteristics of chitosan and its disintegration properties, drawing comparisons with those of microcrystalline cellulose. Furthermore, we will investigate potential formulation strategies for the development of effective tablet formulations employing chitosan as a disintegrant. Additionally, attention will be given to several prior studies on the utilization of chitosan as a disintegrant, providing an analysis of their advantages and limitations in diverse pharmaceutical contexts.
雌二醇在多种生理系统中具有重要的调节作用,包括月经周期、心血管、神经、骨骼和血管系统,这突显了它的重要性。因此,这种化合物经常被纳入各种药物制剂中,特别是片剂形式的制剂。雌二醇片剂制剂中常用的典型非活性成分包括乳糖一水合物、硬脂酸镁、微晶纤维素和交联羧甲基纤维素钠。壳聚糖作为一种新型赋形剂,正逐渐成为微晶纤维素(MCC)的有前途的替代品。与 MCC 相比,壳聚糖具有出色的水溶性、宜人的气味、超级崩解剂效果、增加的孔隙率和增强的液体吸收性等特性。将壳聚糖用作片剂崩解剂不仅可以提高片剂的生物利用度,还可以促进水溶性片剂制剂的配方,并增加纳米粒壳聚糖中的细胞穿透性,而不会发生壳聚糖-雌二醇相互作用。本文将深入研究壳聚糖的特性及其崩解特性,并与微晶纤维素的特性进行比较。此外,我们将研究开发有效片剂制剂的潜在配方策略,将壳聚糖用作崩解剂。此外,还将关注一些关于壳聚糖作为崩解剂的利用的先前研究,分析它们在不同药物环境中的优缺点。