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Dual mechanism of microenvironmental pH modulation and foam melt extrusion to enhance performance of HPMCAS based amorphous solid dispersion
| Content Provider | Scilit |
|---|---|
| Author | Vo, Anh Q. Feng, Xin Zhang, Jia Xiang Zhang, Feng Repka, Michael A. |
| Copyright Year | 2018 |
| Description | Journal: International journal of pharmaceutics Hydroxypropyl methylcellulose acetate succinate (HPMCAS) is an excellent polymeric carrier for melt extrusion amorphous solid dispersion. However, its pH-dependent solubility limits its application, especially for narrow absorption window drugs. The current study proposed a novel dual approach of foam extrusion and microenvironmental pH modulation to overcome this limitation. Sodium bicarbonate was used as a blowing agent and the remaining sodium carbonate acted as an internal pH modifier. Compared with conventional extrusion, foam extrusion dramatically lowered the extrudate physical strength (breaking force and hardness decreased by 20-fold; breaking energy and deformation energy decreased by more than 30-fold). Milling efficiency of foam extrudate was largely improved compared with that of conventional extrudates, demonstrating smaller particle size, larger specific surface area, and ability to pass through a smaller milling screen. The foam extrudate could generate a supersaturation concentration up to 8-fold higher than the solubility of the pure drug. It also significantly enhanced drug dissolution in a two-step biorelevant medium (p < 0.05). This novel approach improved both manufacturing processability and dissolution of HPMCAS-based solid dispersions. |
| Related Links | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6158015/pdf |
| Ending Page | 228 |
| Page Count | 13 |
| Starting Page | 216 |
| ISSN | 03785173 |
| e-ISSN | 18733476 |
| DOI | 10.1016/j.ijpharm.2018.08.042 |
| Journal | International journal of pharmaceutics |
| Issue Number | 1-2 |
| Volume Number | 550 |
| Language | English |
| Publisher | Elsevier BV |
| Publisher Date | 2018-08-21 |
| Access Restriction | Open |
| Subject Keyword | Journal: International journal of pharmaceutics Pharmacology and Pharmacy Foam Melt Extrusion Amorphous Solid Dispersion Hydroxypropyl Methylcellulose Acetate Succinate (hpmcas) |
| Content Type | Text |
| Resource Type | Article |
| Subject | Pharmaceutical Science |
