INFLUENCE OF CO-CRYSTALLIZATION OF CARBAMAZEPINE AND BENZAMIDE ON SOLUBILITY AND DISSOLUTION

• Main Author: Irena Suharti, Florencia
• Format: Final Project
• Language: Indonesia
• Online Access: https://digilib.itb.ac.id/gdl/view/78389
• Institution: Institut Teknologi Bandung

Carbamazepine is a primary antiepileptic drug that is also used to treat trigeminal neuralgia and pain associated with other neurological disorders. It belongs to class II in the Biopharmaceutical Classification System (BCS), indicating low solubility. The limited water solubility of carbamazepine results in slow dissolution and consequently, its absorption is hindered, leading to irregular and delayed absorption. This ultimately affects the effectiveness of carbamazepine. An approach to enhance the physical and chemical properties as well as the effectiveness of carbamazepine involves creating cocrystals. This study aimed to evaluate how cocrystallization with benzamide affects the solubility and dissolution of carbamazepine. The potential formation of cocrystals between these two substances was determined using contact method. X-ray diffractogram shows the formation of a new crystal phase. Calorimetry test (DSC) showed that the melting points of carbamazepine, benzamide, dissolving cocrystal, ethanol LAG cocrystal, and methanol LAG cocrystal were 185.51°C, 112.88°C, 185.57°C, 104,78°C, and 105.01°C respectively. The cocrystal thermogram shows a new endothermic peak that is different from the peak of pure carbamazepine. The results of the solubility test showed that the solubility of carbamazepine, dissolution cocrystal, ethanol LAG cocrystal, and methanol LAG cocrystal at 72 hours were 304.746 ppm, 244.69 ppm, 246.251 ppm, and 260.402 ppm respectively. The solubility test results for carbamazepine from cocrystals were lower than the solubility of pure carbamazepine. The dissolution of powder carbamazepine after 5, 15, and 45 minutes respectively was 16.149%, 26.262%, 42.455%. The dissolution of carbamazepine from the cocrystal after 5, 15, and 45 minutes was 10.512%, 17.832% and 29.243%, respectively. The dissolution of carbamazepine from LAG ethanol cocrystal after 5, 15, and 45 minutes was 8.643%, 16.270%, and 27.771%, respectively. The dissolution of carbamazepine from methanol LAG cocrystals after 5, 15, and 45 minutes were 9.497%, 16.635%, and 26.738%, respectively. These data show that the dissolution rate of carbamazepine from the cocrystal is lower than the dissolution rate of carbamazepine from the powder.