Pharmaceutical Development, GlaxoSmithKline, 1250 S. Collegeville Rd, Collegeville, Pennsylvania 19426, USA.
Pharm Res. 2010 Apr;27(4):576-88. doi: 10.1007/s11095-010-0061-6. Epub 2010 Feb 9.
In order to enhance the delivery of drugs with limited absorption due to poor solubility/dissolution, approaches are being developed to improve the dissolution rates and solubility of drug molecules. These approaches include identification of water-soluble salts of parent drugs, preparation of stable amorphous drug formulations, inclusion of solubility-enhancing agents in the dosage form, and particle size reduction. Technologies to reduce drug particle size to sub-micrometer range are being applied to product development more frequently. Electrospinning is being considered as one of the technologies which can produce nanosized drugs incorporated in polymeric nanofibers. In vitro and in vivo studies have demonstrated that the release rates of drugs from these nanofiber formulations are enhanced compared to those from original drug substance. This technology has the potential to be used for enhancing the oral delivery of poorly soluble drugs.
为了提高由于溶解度/溶解差而吸收有限的药物的递送效率，正在开发各种方法来提高药物分子的溶解速率和溶解度。这些方法包括识别母体药物的水溶性盐，制备稳定的无定形药物制剂，在剂型中加入增溶剂，以及减小粒径。将药物粒径减小到亚微米范围的技术越来越频繁地应用于产品开发。静电纺丝被认为是可以将纳米级药物纳入聚合物纳米纤维的技术之一。体外和体内研究表明，与原始药物相比，这些纳米纤维制剂中药物的释放速率得到了提高。该技术有可能用于增强难溶性药物的口服递送。
