A Menthol-Based Solid Dispersion Technique for Enhanced Solubility and Dissolution of Sulfamethoxazole from an Oral Tablet Matrix
Journal Title: AAPS PharmSciTech - Year 2015, Vol 16, Issue 4
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.
Authors and Affiliations
Bibi F. Choonara, Yahya E. Choonara, Pradeep Kumar, Lisa C. du Toit, Lomas K. Tomar, Charu Tyagi, Viness Pillay
Keywords
Related Articles
- EP ID EP682242
- DOI 10.1208/s12249-014-0271-z
- Views 92
- Downloads 0
The Role of Caprylate Ligand Ion on the Stabilization of Human Serum Albumin
Sodium caprylate was added to a pharmaceutical-grade human serum albumin (HSA) to stabilize the product. In this study we have aimed to establish how caprylate ligand protects HSA from thermal degradation. The fatty acid...
Pharmaceutical Thermal Processing
The Effect of Moisture on the Flowability of Pharmaceutical Excipients
The effect of moisture content on flowability of six pharmaceutical powders (microcrystalline cellulose (MCC), hydroxypropyl methylcellulose (HPMC), carboxymethyl cellulose (CMC), polyvinylpyrrolidone (PVP), corn starch,...
Coatings of Eudragit® RL and L-55 Blends: Investigations on the Drug Release Mechanism
In a previous study, generally lower drug release rates from RL:L55 blend coated pellets in neutral/basic release media than in acidic release media were reported. The aim of this study was to obtain information on the d...
Controlled Porosity Solubility Modulated Osmotic Pump Tablets of Gliclazide
A system that can deliver drug at a controlled rate is very important for the treatment of various chronic diseases such as diabetes, asthma, and heart disease. Poorly water-soluble drug with pH-dependent solubility such...