IMPROVEMENT IN BIOAVAILABILITY OF OXCARBAZEPINE USING SPHERICAL AGGLOMERATIONAbstract
Spherical agglomeration technique enables simultaneous crystallization and agglomeration. Oxcarbazepine spherical agglomerates were prepared by crystallo-co agglomeration technique. Acetone acted as a good solvent, aqueous solution of PEG 6000 served as a bad solvent, and dichloromethane was used as bridging liquid. The optimization was carried out using 23 factorial design, where the factors were rotation speed, polymer-drug ratio and amount of bridging liquid. The responses evaluated were % drug release, mean yield pressure (MYP), and carr’s index. The optimized agglomerates and oxcarbazepine were evaluated by powder x-ray diffractometer (PXRD) and scanning electron microscopy (SEM). The agglomeration improved the micromeritic properties of oxcarbazepine. PXRD showed reduction in crystalline nature of oxcarbazepine, and SEM demonstrated a spherical and smooth surface. In-vitro dissolution increased by 10-fold. The AUC (35.19%), Cmax (23%), and tmax (reduced by 1h) also recorded improvement. From the results, spherical agglomerates are a suitable method and can be used to design immediate-release formulations.
G. S. Shinde and S. Mohite *
Department of Pharmaceutical Chemistry, Rajarambapu College of Pharmacy, Kasegaon, Maharashtra, India.
17 March 2019
11 April 2020
13 April 2020
01 May 2020