College of Pharmacy, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, Republic of Korea.
College of Pharmacy, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon 34134, Republic of Korea.
Int J Pharm. 2021 Dec 15;610:121247. doi: 10.1016/j.ijpharm.2021.121247. Epub 2021 Nov 2.
Many new chemical entities (NCEs) have been discovered with the development of the pharmaceutical industry. However, the main disadvantage of these drugs is their low aqueous solubility, which results in poor bioavailability, posing a challenge for pharmaceutical scientists in the field of drug development. Solid dispersion (SD) technology is one of the most successful techniques used to resolve these problems. SD has been widely used to improve the solubility and bioavailability of poorly water-soluble drugs using several methods such as melting, supercritical fluid (SCF), solvent evaporation, spray drying, hot-melt extrusion, and freeze-drying. Among them, SCF with carbon dioxide (CO) has recently attracted great attention owing to its enhanced dissolution and bioavailability with non-toxic, economical, non-polluting, and high-efficiency properties. Compared with the conventional methods using organic solvents in the preparation of the formulation (solvent evaporation method), SCF used CO to replace the organic solvent with high pressure to avoid the limitation of solvent residues. The solubility of a substance in CO plays an important role in the success of the formulation. In the present review, the various processes involved in SCF technology, application of SCF to prepare SD, and future perspectives of SCF are described.
随着制药工业的发展,已经发现了许多新的化学实体(NCE)。然而,这些药物的主要缺点是其低水溶解度,导致生物利用度差,这对药物开发领域的制药科学家构成了挑战。固体分散体(SD)技术是解决这些问题最成功的技术之一。SD 已广泛用于通过多种方法(如熔融、超临界流体(SCF)、溶剂蒸发、喷雾干燥、热熔挤出和冷冻干燥)来提高难溶性药物的溶解度和生物利用度。其中,最近由于其具有增强的溶解和生物利用度、无毒、经济、无污染和高效的特性,使用二氧化碳(CO)的 SCF 引起了极大的关注。与使用有机溶剂制备配方(溶剂蒸发法)的常规方法相比,SCF 使用 CO 以高压代替有机溶剂,以避免溶剂残留的限制。物质在 CO 中的溶解度在配方的成功中起着重要作用。在本综述中,描述了 SCF 技术涉及的各种过程、SCF 在制备 SD 中的应用以及 SCF 的未来前景。