BACKGROUND: Eprosartan mesylate is a poorly water-soluble drug. It does not dissolve well in the aqueous gastrointestinal fluid, which means it is not absorbed well via the oral route, because a drug can cross cell membranes when it is dissolved in the gastrointestinal fluid. OBJECTIVES: The purpose of this research was to enhance the aqueous solubility and dissolution rate of eprosartan mesylate using the solid dispersion technique. Enhancing the solubility and dissolution leads to better absorption via the oral route. MATERIAL AND METHODS: A number of eprosartan mesylate-laden polymeric solid dispersions were prepared with hydroxypropyl methylcellulose (HPMC) and polysorbate 80 by means of the solvent evaporation technique. The impact of the weight ratios of the constituents on the solubility and dissolution rate was studied in comparison with the plain drug. The formulation presenting the optimal solubility and dissolution underwent the solid-state characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR). RESULTS: Both polysorbate 80 and HPMC positively affected the solubility and dissolution of eprosartan mesylate. CONCLUSIONS: In particular, a ternary solid dispersion consisting of eprosartan mesylate, HPMC and polysorbate 80 at a weight ratio of 1:4.2:0.3 showed the highest solubility (36.39 ± 3.95 mg/mL) and dissolution (86.19 ±4.09% in 10 min). Moreover, the drug was present in the amorphous form in the solid dispersion with no covalent drug-excipient interactions.
BACKGROUND:Eprosartan mesylate is a poorly water-soluble drug. It does not dissolve well in the aqueous gastrointestinal fluid, which means it is not absorbed well via the oral route, because a drug can cross cell membranes when it is dissolved in the gastrointestinal fluid. OBJECTIVES: The purpose of this research was to enhance the aqueous solubility and dissolution rate of eprosartan mesylate using the solid dispersion technique. Enhancing the solubility and dissolution leads to better absorption via the oral route. MATERIAL AND METHODS: A number of eprosartan mesylate-laden polymeric solid dispersions were prepared with hydroxypropyl methylcellulose (HPMC) and polysorbate 80 by means of the solvent evaporation technique. The impact of the weight ratios of the constituents on the solubility and dissolution rate was studied in comparison with the plain drug. The formulation presenting the optimal solubility and dissolution underwent the solid-state characterization using X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier-transform infrared spectroscopy (FTIR). RESULTS: Both polysorbate 80 and HPMC positively affected the solubility and dissolution of eprosartan mesylate. CONCLUSIONS: In particular, a ternary solid dispersion consisting of eprosartan mesylate, HPMC and polysorbate 80 at a weight ratio of 1:4.2:0.3 showed the highest solubility (36.39 ± 3.95 mg/mL) and dissolution (86.19 ±4.09% in 10 min). Moreover, the drug was present in the amorphous form in the solid dispersion with no covalent drug-excipient interactions.
Authors: Abdul Ahad; Yousef A Bin Jardan; Mohd Zaheen Hassan; Mohammad Raish; Ajaz Ahmad; Abdullah M Al-Mohizea; Fahad I Al-Jenoobi Journal: Drug Deliv Date: 2022-12 Impact factor: 6.819