칸데사르탄 실렉세틸 고체분산체 개발 및 평가

Development and Evaluation of Candesartan Cilexetil Solid Dispersion

Candesartan cilexetil (CDST) is belongs to the Biopharmaceutics Classification System (BCS) class II and is widely used to treat hypertension. The commercial product as Atacand®Tab contains 16 mg of CDST out of a total weight of 130 mg. The purpose of this study is to solubilize and stabilize CDST, and develop a CDST solid dispersion (SD) containing a carrier and a polymer without a weak base. Therefore, a CDST-SD was developed using a solvent evaporation method. The dissolution (%) of CDST in final formulation (SB-SD1) improved by 4.1-, 21.6-, and 19.8-fold compared to that of Atacand®Tab at 60 min in pH 1.2 media, distilled water (DW), and pH 6.8 buffer, respectively. The physicochemical properties of the SB-SD1 formulation changed the melting point and crystallinity of CDST. Additionally, stability for six months was secured. In conclusion, the SB-SD1 formulation improved the dissolution of CDST and secured stability due to changes in physicochemical properties.