| 학회 | 한국화학공학회 |
| 학술대회 | 2017년 가을 (10/25 ~ 10/27, 대전컨벤션센터) |
| 권호 | 23권 2호, p.1643 |
| 발표분야 | 분리기술 |
| 제목 | Co-amorphization of Linagliptin by Evaporation Method |
| 초록 | Linagliptin is a drug belonging to COX 2 which inhibits DPP-4 enzyme whose oral dosage forms were approved by US FDA in 2011. Even though linagliptin is classified as the BCS class Ⅲ, it is very slightly soluble in water. Accordingly, the bioavailability of linagliptin-based drugs shall be substantially enhanced by improving the dissolution rate of the drug substance. Amorphization has attracted attentions recently as a solubilization technology for insoluble APIs. In this study, various additive substances were employed to manufacture co- amorphous solid forms with the linagliptin by evaporation method. Among them, sorbitol was found to be greatly effective as co-amorphization agent. Resulting amorphous materials were pretreated suitably and characterized via powder x-ray diffraction and differential scanning calorimetry. It was observed that the pathway to the co-amorphous solid formation was significantly dependent upon the mass ratio between the drug substance and co-amophization agent. The stability of the co-amorphous powders was estimated. As anticipated, the co-amorphous solid powders showed substantially improved solubility compared to the pure linagliptin powder. |
| 저자 | 김가영, 최광진 |
| 소속 | 순천향대 |
| 키워드 | 결정화 |
| 원문파일 | 초록 보기 |
