Abstract
Achieving adequate content uniformity (CU) is a significant challenge in the development and manufacturing of low dose oral tablets. Using four model active pharmaceutical ingredients (APIs), we show that loading APIs into a grade of mesoporous silica, Aeroperl®, is effective for achieving excellent CU. All APIs in the Aeroperl® composites were amorphous. After six months under accelerated stability conditions, the drug-Aeoperl composites exhibited good physical stability for all four APIs. The performance of Aeroperl®-based formulations was robust since their good CU and manufacturability were insensitive to model APIs. In addition, the dissolution rate of composite-based formulations was higher than corresponding physical mixtures. Overall, the Aeroperl®-based platform formulation is a promising approach for successfully developing low dose oral tablet products.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 184-189 |
| Number of pages | 6 |
| Journal | International journal of pharmaceutics |
| Volume | 539 |
| Issue number | 1-2 |
| DOIs | |
| State | Published - Mar 25 2018 |
Bibliographical note
Funding Information:This work was supported by a grant from Eli Lilly through the Lilly Research Award Program. W-J. Sun is grateful to the Department of Pharmaceutics, University of Minnesota for a David and Marilyn Grant Fellowship in Physical Pharmacy (2015-2017) and the Dane O. Kildsig Center for Pharmaceutical Processing Research (CPPR) for partial financial support.
Publisher Copyright:
© 2018 Elsevier B.V.
Keywords
- Aeroperl®
- Amorphous
- Neusilin®
- Particle engineering
- Stability