Abstract
The aim of this work was to evaluate the effectiveness of mesoporous clays or silicas to develop fast-dissolving glyburide tablets based on a liquisolid approach. Selected clay (Neusilin®US2) and silica (Aeroperl®300) allowed preparation of innovative drug liquisolid systems containing dimethylacetamide or 2-pyrrolidone as drug solvents, without using coating materials which are necessary in conventional systems. The obtained liquisolid powders were characterized for solid-state properties, flowability, compressibility, morphology, granulometry, and then used for directly compressed tablet preparation. The developed liquisolid tablets provided a marked drug dissolution increase, reaching 98% dissolved drug after 60 min, compared to 40% and 50% obtained from a reference tablet containing the plain drug, and a commercial tablet. The improved glyburide dissolution was attributed to its increased wetting properties and surface area, due to its amorphization/solubilization within the liquisolid matrix, as confirmed by DSC and PXRD studies. Mesoporous clay and silica, owing to their excellent adsorbent, flow, and compressibility properties, avoided use of coating materials and considerably improved liquid-loading capacity, reducing the carrier amount necessary to obtain freely flowing powders. Neusilin®US2 showed a superior performance than Aeroperl®300 in terms of the tablet’s technological properties. Finally, simplicity and cost-effectiveness of the proposed approach make it particularly advantageous for industrial scale-up.
Highlights
Glyburide (GLY) belongs to the second generation of sulfonylurea antidiabetic drugs, and it is one of the most widely utilized oral hypoglycemic agents [1]
Its ability to prevent cerebral ischemia and hemorrhagic stroke has been recently proved [2,3], and from 2015 it has been included in the model list of Essential Medicines of World Health Organization [4]
Mesoporous clays and silicas can be considered as potentially suitable materials for liquisolid systems preparation. Based on all these premises, we considered it worthy of interest to investigate the effectiveness of the liquisolid approach in the development of fast dissolving tablets of GLY with improved drug dissolution performance, by replacing the mixture of carrier and coating materials commonly used for their formulation with suitable mesoporous silicas or clays which would be able to simultaneously perform both such functions
Summary
Glyburide (GLY) belongs to the second generation of sulfonylurea antidiabetic drugs, and it is one of the most widely utilized oral hypoglycemic agents [1]. The dissolution rate of poorly water-soluble drugs often represents the main limiting factor in their absorption rate [6,7]. Problems of bio-inequivalence among pharmaceutically equivalent dosage forms of the drug were confirmed by a multinational post-market comparative study of various marketed products of the drug [9]. Such findings were found to be related to the unsatisfactory and variable dissolution behavior of GLY, further supporting the previously reported problems of formulation-dependent oral absorption of the drug [10]
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