Effect of Hydroxypropyl Cellulose Level on Twin-Screw Melt Granulation of Acetaminophen
- PDF / 2,355,491 Bytes
- 14 Pages / 595.276 x 790.866 pts Page_size
- 79 Downloads / 122 Views
Research Article Theme: Pharmaceutical Thermal Processing - An Update Guest Editors: Feng Zhang, Michael Repka and Suresh Bandari
Effect of Hydroxypropyl Cellulose Level on Twin-Screw Melt Granulation of Acetaminophen Tongzhou Liu,1 Shubhajit Paul,2 Brian T Beeson,1 Johnny Alexander,1 Fengyuan Yang,3 Vivian Bi,3 Thomas Durig,3 Changquan Calvin Sun,2 and Feng Zhang1,4
Received 22 May 2020; accepted 10 August 2020 Abstract.
This study investigated the effect of binder level on the physicochemical changes and tabletability of acetaminophen (APAP)-hydroxypropyl cellulose (HPC) granulated using twin-screw melt granulation. Even at 5% HPC level, the tablet tensile strength achieved up to 3.5 MPa. A minimum of 10% HPC was required for the process robustness. However, 20% HPC led to tabletability loss, attributable to the high mechanical strength of APAP granules. The over-granulated APAP granules had thick connected HPC scaffold and low porosity. Consequently, these granules were so strong that they underwent a lower degree of fracture under compression and higher elastic recovery during decompression. HPC was enriched on the surface of APAP extrudates at all HPC levels. Amorphous APAP was also observed on the extrudate surface at 20% HPC level, and it recrystallized within 24 h storage. To achieve a robust process and optimal improvement in APAP tabletability, the preferred HPC level was 10 to 15%.
KEY WORDS: Twin-screw melt granulation; Binder content; Over-granulation; Granule mechanical properties; Granule structure.
INTRODUCTION Granulation of powder blends is a unit operation widely used to produce solid dosage forms such as tablets and capsules. The main purpose of granulation is to improve flowability, content uniformity, and tabletability of powder blends. Depending on the binder types and manufacturing processes, pharmaceutical granulation can be categorized as dry, wet, and melt granulation (MG). Melt granulation holds certain advantages over wet granulation, since it avoids solvent-induced physicochemical changes to the drugs. Melt granulation also holds certain advantages over dry
Guest Editors: Feng Zhang, Michael Repka and Suresh Bandari Electronic supplementary material The online version of this article (https://doi.org/10.1208/s12249-020-01785-y) contains supplementary material, which is available to authorized users. 1
Division of Molecular Pharmaceutics and Drug Delivery, College of Pharmacy, University of Texas at Austin, 2409 University Avenue, A1920, Austin, Texas 78712, USA. 2 Department of Pharmaceutics, University of Minnesota, Minneapolis, Minnesota, USA. 3 Pharmaceutical Technology, Ashland Specialty Ingredients, Wilmington, Delaware, USA. 4 To whom correspondence should be addressed. (e–mail: [email protected])
granulation, since melt granulation is more effective in improving tabletability (1). Traditionally, melt granulation is carried out in batch mode using a high-shear or fluid-bed granulator. Recently, continuous melt granulation using a twin-screw extruder (TSMG) has ga
Data Loading...
