A Menthol-Based Solid Dispersion Technique for Enhanced Solubility and Dissolution of Sulfamethoxazole from an Oral Tablet Matrix

Abstract

Abstract. A menthol-based solid dispersion was designed to improve the intrinsic solubility of the poorly soluble sulfamethoxazole-a class II drug molecule of Biopharmaceutics Classification System (BCS) displaying widespread antibacterial activity. Solid dispersions of menthol and sulfamethoxazole were compressed with hydroxypropyl methylcellulose (HPMC) into suitable sulfamethoxazole-loaded matrix tablets for oral drug delivery. The sulfamethoxazole-loaded solid dispersions and compressed tablets were characterized for their physicochemical and physicomechanical properties such as changes in crystallinity, melting point, molecular transitions, and textural analysis for critical analysis of their effects on the solubility and dissolution of sulfamethoxazole. The formulations were further evaluated for swelling, degradation, solubility, and in vitro drug release behavior. In vitro drug release from the sulfamethoxazole-loaded matrix tablets displayed a minimum and maximum fractional release of 0.714 and 0.970, respectively. The tablets further displayed different release rate profiles over the study periods of 12, 16, 48, and 56 h which were attributed to the varying concentrations of menthol within each formulation. Menthol was determined as a suitable hydrophilic carrier for sulfamethoxazole since it functioned as a solubilizing and release-retarding agent for improving the solubility and dissolution of sulfamethoxazole as well as controlling the rate at which it was released.

An attempt to enhance solubility of metoclopramide base by Solid dispersion strategy and its application on development of Transdermal device

“…Figure 7b, PVP K30-Met base 5:1 SD showed ruptured surface morphology with tiny lucid formation. This kind of morphology confirms the complex formation between drug and carrier (Koh et al, 2013;Choonara et al, 2014). The pure drug loaded patch (Figure 7c) showed fractional amorphous nature of matrix of the film.…”

Terpene-Based Natural Deep Eutectic Systems as Efficient Solvents To Recover Astaxanthin from Brown Crab Shell Residues

“…From the obtained FTIR-ATR spectra displayed in Figure , PA (Figure i,ii), as a terpene alcohol, exhibited a strong, broad peak at 3313 cm –1 , which indicates the O–H stretching vibration. Similarly, ME (Figure ii–v) exhibited O–H stretching at 3257 cm –1 . , The CA FTIR-ATR spectrum (Figure i,iii) showed a strong absorption band at 1738 cm –1 . This peak is characteristic of ketones, resulting from the C=O stretching vibration. , EU (Figure iv) exhibited a characteristic response of an ether, with absorption peaks at 1080 and 1215 cm –1 , corresponding to the symmetrical and asymmetrical stretching vibrations of the C–O–C system, respectively .…”

Formulation Development, Characterization and In-vitro Evaluation of Tamoxifen Loaded Liposomes

“…To characterize the drug release in different experimental conditions, T25%, T50% (mean dissolution time) and T80% were calculated from dissolution data according to the following equations, [29]  T25%= (0.25/k)…”