Solubility enhancement of ebastine through natural solid dispersion: formulation and pharmacokinetics
DOI:
https://doi.org/10.60988/p.v37i2S.137Keywords:
ebastine; sodium alginate; natural solid dispersion; solvent evaporation; xyloglucanAbstract
Natural solid dispersion (NSD) is a clever pharmaceutical technology technique that is used in order to improve the physicochemical characteristics of pharmaceuticals, such as their solubility and dissolution. Ebastine (EBS) is a medication used for the treatment of pruritic skin problems and the symptoms of allergic illnesses, such as rhinitis. The aim of this work was to improve the solubility and rate of dissolution of EBS by using an NSD system. Utilizing solvent evaporation as a preparation technique, eight EBS formulations were created as solid dispersions through the use of two natural polymers, namely sodium alginate (SA) and xyloglucan, at various drug to polymer ratios (1:0.5, 1:1, 1:2, and 1:3). The produced formulations were assessed for their in vivo pharmacokinetics, their solubility, and their dissolution. According to our results, the employed polymers improved the drug solubility. In comparison to pure EBS, the optimal formula (EBS:SA at a 1:1 ratio) exhibited a significant increase in solubility. Additional analysis of the ideal formula revealed that EBS is amorphous. In vivo experiments in rats revealed a superior pharmacokinetic performance in terms of bioavailability of the ideal formula compared to pure EBS. It may be inferred that the NSD can be used in order to address the issue of EBS solubility under the chosen conditions, which may lead to improved EBS bioavailability.
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