Abstract
Background: Intestinal nematode infections are usually treated with benzimidazole drugs, but the emergence of resistance to these drugs has led to an increasing demand of new anthelmintic strategies. A new microemulsion formulation (ME) consisting of an Artemisia absinthium extract with proven nematocidal efficacy was previously developed. The aim of our study is to implement a D-optimal mixture design methodology to increase the amount of a silica material (loaded with this ME) in a tablet formulation, considering its tensile strength and disintegration time. Methods: 16 experiments or combinations of the 6 tablet components (loaded silica, microcrystalline cellulose, polyvinylpyrrolidone, croscarmellose, Syloid® 244 FP and magnesium stearate) were assessed. Tensile strength and disintegration time models were developed, and an optimization process was carried out. Results: Tensile strength was improved by increasing the polyvinylpyrrolidone content, while croscarmellose decreased the disintegration time. The optimized powder mixture contains 49.7% w/w of the loaded silica material. A compression force of 12 kN was applied to the powder mixture to form tablets with a tensile strength of 2.0 MPa and a disintegration time of 3.8 min. Conclusions: Our results show that D-optimal mixture designs provide a promising approach to formulate liquid-loaded silica materials.
Highlights
Intestinal nematode infections are usually treated with benzimidazole drugs, but recent studies [1] have evidenced a worrying increase of the cases of resistance to these drugs leading to potential failures of the commonly used therapies
Mattsson et al showed that powder mixtures containing polyvinylpyrrolidone (PVP), as a dry binder, and compressed at 200 MPa had higher axial and radial tensile strength than pregelatinized starch mixtures at the same proportion [24]. These results suggest that PVP may improve the tensile strength of silica tablets, an efficient disintegrant is required to diminish disintegration times, improving the galenic properties [23]
Our results show that D-optimal designs provide a promising tool to improve the formulation of liquid-loaded silica materials in tablets, as it quantifies the effect of the excipients on the properties of the tablets under the conditions of the study
Summary
Intestinal nematode infections are usually treated with benzimidazole drugs, but recent studies [1] have evidenced a worrying increase of the cases of resistance to these drugs leading to potential failures of the commonly used therapies. This illustrates the importance of searching for new alternative strategies for the treatment of these kinds of illnesses. The aim of our study is to implement a D-optimal mixture design methodology to increase the amount of a silica material (loaded with this ME) in a tablet formulation, considering its tensile strength and disintegration time. Conclusions: Our results show that D-optimal mixture designs provide a promising approach to formulate liquid-loaded silica materials
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