Context: Astilbin is considered to be a new and promising immunosuppressant for immune related diseases, but limited in clinical application due to its poor water solubility, difficult oral absorption and low bioavailability.
Objective: The present work studied the effect of PVP and surfactant combined carrier on its capability to improve drug absorption.
Materials and methods: PVP K30-Tween 80 combined carries was applied into the astilbin solid dispersions, tested both in vivo in beagle dogs and in vitro in transport experiments across Caco-2 cell monolayers.
Results and discussion: In the animal studies a many fold increase in plasma AUC was observed for the solid dispersions of drug in PVP K30-Tween 80 combined carries compared to active pharmaceutical ingredient (API). The applicability of Caco-2 monolayers as a tool for predicting the in vivo transport behavior of Astilbin in combination with a solubility enhancing carries was shown. In vitro transport studies confirmed the effect of combined carries on the absorption behavior of the astilbin. MTT studies showed the cell viability gradually decreased with the increase of the drug concentration in a dose dependent manner for astilbin and that in solid dispersions. The permeability and apparent permeability coefficients (Papp) increased with drug in the Caco-2 cell.
Conclusion: In this study, it was found that PVP K30 and Tween 80 promoted the permeability of drugs best within a certain amount. For astilbin PVP K30 and surfactant combined carrier had a strong potential to improve oral bioavailability. 相似文献
This study compares the reliability of nMOSFETs with low- and high-doped ultra-thin body and buried oxide (UTBB) with fully depleted (FD) and partially depleted (PD) silicon on insulator (SOI). The high-doped devices display lower off-current leakage performance but more degradation in both hot-carrier stress (HCS) and positive bias temperature instability (PBTI) test at both room temperature and elevated temperature compared with the low-doped devices. The PBTI test indicates that the high-doped devices induce high tunneling leakage and that the degradation is highly associated with temperature. The degradation stabilizes with an increase in stress time. The thinner PD-SOI demonstrates low variation at the threshold voltage and low drive current under HCS. The FD-SOI has better drain leakage control than the PD-SOI. 相似文献