Impact of Compression Force on Mechanical, Textural, Release and Chewing Perception Properties of Compressible Medicated Chewing Gums.

Medicated chewing gums (MCGs) represent a beneficial platform for realizing drugs intended for dental prophylaxis and treatment. The present study aimed to investigate the impact of compression force on the mechanical, textural, release, and chewing perception characteristics of compressible MCGs with the combination of lysozyme hydrochloride (LH) and ascorbic acid (AsA). Four batches of MCGs were obtained on a laboratory single-punch tablet machine applying different forces, i.e., 5, 7, 10, and 15 kN, and evaluated by their geometrical parameters, mechanical resistance, surface and internal structure characteristics, texture profile, release behavior, and perception attributes during mastication. It was found that increasing compression force slightly affected resistance to crushing and friability of MCGs, but resulted in surface smoothing and formation of a thicker layer with highly compacted particle arrangement. According to the texture analysis, increasing compression force led to harder and more adhesive gums, indicating possible difficulties in chewing and, therefore, impairment of their consumer properties. Lower compression forces were also found to be preferable in terms of better drug release from the obtained chewing gums. The volunteers' assessment showed that an increase of compression force led to significantly raising the initial hardness and crumbliness as well as to decreasing the rate of the integral gum mass formation during mastication, which may negatively affect perceptive sensations when using MCGs. Based on the results obtained, the optimal compressing force was selected to be 7 kN, which allows obtaining MCGs with good organoleptic, mechanical, textural, and release properties.

Development and uniformity evaluation of low-dose medicated chewing gums prepared by compression method.

The aim of this work was to develop medicated chewing gums (MCGs) containing 10 mg of lysozyme hydrochloride (LH) and 20 mg of ascorbic acid (AsA) obtained by the compression method with Health in Gum® (HiG®) PWD 01 as a compressible gum base. Because of a low content of active ingredients, it was essential to choose the way of adding them to the tableting mass and evaluate their distribution homogeneity in the dosage units. The blends for compression were prepared by two methods: the first one was simple mixing of all components; the second one included the step of wet granulation of a three-component mixture - LH, sucralose and a taste additive. Flow properties of LH, AsA, HiG®, LH granules and blends for compression were studied. MCGs were evaluated according to Ph.Eur. 9.0 Chapters 2.9.5, 2.9.6 and 2.9.40. AsA and HiG® were characterized as free flowing, while LH had insufficient flow properties. Compared with a simple mixed blend, the granulation step allowed significantly improving flow properties of the final blend for compression. Unlike MCGs compressed from the simple mixed blend, MCGs prepared through the granulation step met Ph.Eur. 9.0 Chapter 2.9.40 requirements. The propriety of MCG preparation method involving the step of wet granulation also has been confirmed by mass and drug content uniformity tests.

In Vitro Bioavailability Study of an Antiviral Compound Enisamium Iodide.

An investigation into the biopharmaceutics classification and a study of the in vitro bioavailability (permeability and solubility) of the antiviral compound enisamium iodide (4-(benzylcarbamoyl)-1-methylpyridinium iodide) were carried out. The solubility of enisamium iodide was determined in four different buffers. Apparent intestinal permeability (Papp) of enisamium iodide was assessed using human colon carcinoma (Caco-2) cells at three concentrations. The solubility of enisamium iodide in four buffer solutions from pH 1.2 to 7.5 is about 60 mg/mL at 25 °C, and ranges from 130 to 150 mg/mL at 37 °C, depending on the pH. Based on these results, enisamium iodide can be classified as highly soluble. Enisamium iodide demonstrated low permeability in Caco-2 experiments in all tested concentrations of 10-100 µM with permeability coefficients between 0.2 × 10-6 cm s-1 and 0.3 × 10-6 cm s-1. These results indicate that enisamium iodide belongs to class III of the Biopharmaceutics Classification System (BCS) due to its high solubility and low permeability. The bioavailability of enisamium iodide needs to be confirmed in animal and human studies.