“Felodipine-indomethacin” co-amorphous supersaturating drug delivery systems: “Spring-parachute” process, stability, in vivo bioavailability, and underlying molecular mechanisms.
作者：Ya-Wei Li, Hong-Mei Zhang, Bai-Ji Cui, et al... Nian-Qiu Shi*(通訊）.
關鍵字：Molecular mechanisms; Stability; Supersaturating drug delivery systems (SDDS); “Drug-drug” co-amorphous systems (CAS); “Spring-parachute” process.
論文來源：期刊
具體來源：Eur J Pharm Biopharm. 2021 Sep;166:111-125.
發表時間：2021年
Amorphous solid dispersions (ASD) are one of most commonly used supersaturating drug delivery systems (SDDS) to formulate insoluble active pharmaceutical ingredients. However, the development of polymer-guided stabilization of ASD systems faces many obstacles. To overcome these shortcomings, co-amorphous supersaturable formulations have emerged as an alternative formulation strategy for poorly soluble compounds. Noteworthily, current researches around co-amorphous system (CAS) are mostly focused on preparation and characterization of these systems, but more detailed investigations of their supersaturation ("spring-parachute" process), stability, in vivo bioavailability and molecular mechanisms are inadequate and need to be clarified. In present study, we chose pharmacological relevant BCS II drugs to fabricate and characterize "felodipine-indomethacin" CAS. To enrich the current inadequate but key knowledge on CAS studies, we carried out following highlighted investigations including dissolution/solubility, semi-continuous "spring-parachute" process, long-term stability profile of amorphous state, in vivo bioavailability and underlying molecular mechanisms (molecular interaction, molecular miscibility and crystallization inhibition). Generally, the research provides some key information in the field of current "drug-drug" CAS supersaturable formulations.