Date of Award
1-1-2024
Document Type
Thesis
Degree Name
M.S. in Pharmaceutical Science
First Advisor
Michael A. Repka
Second Advisor
Walter G. Chambliss
Third Advisor
Mohammed Maniruzzaman
Relational Format
dissertation/thesis
Abstract
Carbamazepine (CBZ) is an anti-convulsant and specific analgesic for trigeminal neuralgia that reduces polysynaptic responses and blocks post titanic potentiation. Moreover, CBZ is effective in partial and generalized convulsions and mixed types. It is not effective in petit mal seizures. Carbamazepine extended-release tablets are used to treat episodes of mania (or) mixed episodes i.e., symptoms of mania and depression that happen at the same time, in patients with bipolar disorder. The present study was designed to develop CBZ extended-release tablets with acrylic acid-based polymer (Eudragit® RL PO) using a melt granulation and to match the USP dissolution test specification. Thermal characterization and drug-polymer interactions were evaluated using Differential Scanning Calorimetry and Fourier Transform Infrared Spectroscopy. Initial extrusion was carried out using a HAAKE™ Minilab extruder. A USP Type-II dissolution apparatus was utilized to conduct an in vitro drug release study. Lead formulation met the required USP dissolution test specification (10-30% at 2hr; >70% at 24hr) that contains 15% Eudragit® RL PO and 5% sodium starch glycolate with 50% drug load. Moreover, the process showed retarded drug release compared to the formulation prepared using the direct compression method. The process was scaled up from the HAAKE™ Minilab extruder (Batch size ~ 20g) to the Process 11 Extruder (Batch size ~ 200g) for F9 formulation. Powder characterization and particle size distribution were performed for the melt extruded granules of the lead formulation. The prepared tablets were evaluated for weight variation, hardness (12kP), and friability (<1%) and found to be in the acceptable range. From the in vitro dissolution studies, the tablets prepared using granules obtained from the Process 11 extruder at the processing temperature of 160 °C, met the USP dissolution test specifications. In conclusion, preparing extended-release tablets through Hot-melt Extrusion (HME) has significant value as a continuous manufacturing process.
Recommended Citation
Kalla, Chamundeswara Srinivasa Akash, "Application of Hot-Melt Extrusion Technology for the Preparation of Carbamazepine Extended-Release Tablets" (2024). Electronic Theses and Dissertations. 2755.
https://egrove.olemiss.edu/etd/2755