Loratadine is a non-sedating antihistamine that belongs to BCS class II. The purpose of this study was to make effective loratadine tablets using a liquisolid system with various levels of surfactant to increase solubility. The interaction test between loratadine and solvent was carried out using the insilico method with Autodock program to obtain the minimize energy (E) and binding energy (ΔG) value, while the solubility test was carried out by laboratory experiments. The solvents used were glycerin, propylene glycol and polyethylene glycol 400. While the surfactants used were polysorbate 20, 40, 60 and 80. The tablets were tested for the hardness, friability, disintegration time and dissolution test. To determine the effect of solvents and surfactants on the physical properties and dissolution of tablets, one-way annova statistical test was carried out. To determine the interaction of active ingredients and excipients, a test using infrared spectroscopy and Difference Scaning Calorymetry (DSC) was carried out, while to determine the crystal formation of the drug substance, X-ray diffraction was used.
The results showed that there was a linear relationship between the results of the in silico test (E and ΔG) and the results of the laboratory solubility test (% w/v) between loratadine and solvents (propylene glycol, glycerin and PEG 400). Tablet hardness, friability and disintegration time showed that all formulas met the requirements. Dissolution test showed that the tablets that had the highest dissolution were tablets containing polysorbate 20 with a concentration of 0.3%. The results of the infrared spectroscopy test showed that there was no interaction between the active ingredient and excipients. DSC and X-ray test results showed that loratadine in the liquisolid system was in amorphous or dissolved form.
The conclusion is that changing the solvent content increases tablet hardness, decreases tablet friability, accelerates tablet disintegration time and increases % of loratadine content dissolved in liquisolid tablets while increasing polysorbate content of can increase % of loratadine content dissolved in liquisolid tablets. The formula that produced liquisolid tablets that met the requirements and had the highest dissolution % content of loratadine was the formula containing polysorbate 20 with a concentration of 0.3%.
Keywords: loratadine, liquisolid, surfactan, tablet