OBJECTIVES: This study was undertaken to investigate the effect of d-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) on the dissolution of carbamazepine (CBZ) commercial tablets (Tegretol(®)) as a function of temperature and to modify the reaction-limited model of dissolution for the description of classical supersaturated dissolution data. METHODS: Solubility studies were performed using various concentrations of (i) TPGS and (ii) silicon dioxide and microcrystalline cellulose, which are excipients of Tegretol(®) at 10, 25 and 37°C. Dissolution studies were carried out using Tegretol(®) tablets, 200 mg/tab. KEY FINDINGS: The solubility of CBZ in the presence of TPGS was found to increase in a concentration-dependent manner at all temperatures studied. Classical supersaturated dissolution curves with concentration maxima higher than the corresponding solubility values in the presence of TPGS were observed only at 10°C. The model developed was based on a time-dependent expression for the forward microconstant of the CBZ-TPGS reaction at the solid-liquid interface and it was fitted successfully to the dissolution data of CBZ in the presence of TPGS at 10°C. CONCLUSIONS: Vitamin E TPGS increased the solubility of CBZ at all temperatures studied. The modification of the reaction-limited model of dissolution allowed us to describe classical supersaturated dissolution curves.
OBJECTIVES: This study was undertaken to investigate the effect of d-alpha-tocopheryl polyethylene glycol 1000 succinate (vitamin E TPGS) on the dissolution of carbamazepine (CBZ) commercial tablets (Tegretol(®)) as a function of temperature and to modify the reaction-limited model of dissolution for the description of classical supersaturated dissolution data. METHODS: Solubility studies were performed using various concentrations of (i) TPGS and (ii) silicon dioxide and microcrystalline cellulose, which are excipients of Tegretol(®) at 10, 25 and 37°C. Dissolution studies were carried out using Tegretol(®) tablets, 200 mg/tab. KEY FINDINGS: The solubility of CBZ in the presence of TPGS was found to increase in a concentration-dependent manner at all temperatures studied. Classical supersaturated dissolution curves with concentration maxima higher than the corresponding solubility values in the presence of TPGS were observed only at 10°C. The model developed was based on a time-dependent expression for the forward microconstant of the CBZ-TPGS reaction at the solid-liquid interface and it was fitted successfully to the dissolution data of CBZ in the presence of TPGS at 10°C. CONCLUSIONS:Vitamin E TPGS increased the solubility of CBZ at all temperatures studied. The modification of the reaction-limited model of dissolution allowed us to describe classical supersaturated dissolution curves.
Authors: Arvind Sharma; Kanika Arora; Harapriya Mohapatra; Rakesh K Sindhu; Madalin Bulzan; Simona Cavalu; Gulsheen Paneshar; Hosam O Elansary; Ahmed M El-Sabrout; Eman A Mahmoud; Abdullah Alaklabi Journal: Molecules Date: 2022-05-06 Impact factor: 4.927