QbD 기반 이중 방출 제어 매트릭스 정제의 개발 및 용출 특성

Development and Dissolution Behavior of Dual-Release Matrix Tablet Based on QbD

In this study, a dual-release matrix tablet (DRMT) containing sarpogrelate HCl (SGH) was developed by varying the amount HPMC K100M and Eudragit® RSPO according to approach of quality by design (QbD). For this experimental, we were evaluated dissolution rate at 2, 8 and 24 hours and compared it with the commercially available Sapodifil® SR 300 mg for application as DRMT system. Optimization was achieved through a 2-factor, 3-level full factorial design, focusing on the total amount of polymer (X1) and Eudragit® RSPO (X2) within it, with a defined design space for these variables. The dissolution rate at 2 and 8 hours of the prepared DRMT was affected by the total amount of polymer and amount of Eudragit® RSPO to polymer and either showed a linear or quadratic pattern (p<0.05), but it was not affected at 24 hours. Based on the results, we could confirm that the mechanism of drug release from DRMT follows Korsmeyer-Peppas model by Fickian diffusion. The optimized DRMT with a total amount of polymer in sustained release granule part of 52.51% and Eudragit® RSPO of 12.54% showed high overall satisfaction (0.8753). Also, the difference factor and similarity factor were 5.47 and 84.30, respectively, and there was no significant difference in bioequivalence between the optimized DRMT and Sapodifil® SR 300 mg. Overall, the study highlights successful formulation development and process optimization, providing valuable insights for industrial applications and confirming the efficacy of the dualrelease formulation system.