Elan Pharmaceuticals, 800 Gateway Blvd., South San Francisco, California 94080, USA.
J Pharm Sci. 2010 Oct;99(10):4107-48. doi: 10.1002/jps.22151.
It is estimated that more than 40% of new chemical entities (NCEs) coming out of the current drug discovery process have poor biopharmaceutical properties, such as low aqueous solubility and/or permeability. These suboptimal properties pose significant challenges for the oral absorption of the compounds and for the development of orally bioavailable dosage forms. Development of soft gelatin capsule (softgel) dosage form is of growing interest for the oral delivery of poorly water soluble compounds (BCS class II or class IV). The softgel dosage form offers several advantages over other oral dosage forms, such as delivering a liquid matrix designed to solubilize and improve the oral bioavailability of a poorly soluble compound as a unit dose solid dosage form, delivering low and ultra-low doses of a compound, delivering a low melting compound, and minimizing potential generation of dust during manufacturing and thereby improving the safety of production personnel. However, due to the very dynamic nature of the softgel dosage form, its development and stability during its shelf-life are fraught with several challenges. The goal of the current review is to provide an in-depth discussion on the softgel dosage form to formulation scientists who are considering developing softgels for therapeutic compounds.
据估计，目前药物发现过程中出现的 40%以上的新化学实体（NCE）具有较差的生物制药特性，例如低水溶性和/或渗透性。这些不理想的特性给化合物的口服吸收和口服生物利用度剂型的开发带来了重大挑战。软明胶胶囊（软胶囊）剂型的开发对于口服传递水溶性差的化合物（BCS 类 II 或类 IV）越来越感兴趣。软胶囊剂型相对于其他口服剂型具有许多优势，例如提供旨在溶解和提高水溶性差的化合物的口服生物利用度的液体基质作为单剂量固体剂型，提供低剂量和超低剂量的化合物，提供低熔点化合物，并在制造过程中最大限度地减少潜在粉尘的产生，从而提高生产人员的安全性。然而，由于软胶囊剂型的非常动态的性质，其在货架期内的开发和稳定性充满了许多挑战。本综述的目的是为正在考虑为治疗性化合物开发软胶囊的制剂科学家提供对软胶囊剂型的深入讨论。
