Liquigroud technique: a new concept for enhancing dissolution rate of glibenclamide by combination of liquisolid and co-grinding technologies

Abstract

Introduction: The potential of combining liquisolid and co-grinding technologies (liquiground technique) was investigated to improve the dissolution rate of a water-insoluble agent (glibenclamide) with formulation-dependent bioavailability. Methods: To this end, different formulations of liquisolid tablets with a wide variety of non-volatile solvents contained varied ratios of drug: solvent and dissimilar carriers were prepared, and then their release profiles were evaluated. Furthermore, the effect of size reduction by ball milling on the dissolution behavior of glibenclamide from liquisolid tablets was investigated. Any interaction between the drug and the excipient or crystallinity changes during formulation procedure was also examined using X-ray diffraction (XRD) and differential scanning calorimetry (DSC). Results: The present study revealed that classic liquisolid technique did not significantly affect the drug dissolution profile as compared to the conventional tablets. Size reduction obtained by co-grinding of liquid medication was more effective than the implementation of liquisolid technique in enhancing the dissolution rate of glibenclamide. The XRD and DSC data displayed no formation of complex or any crystallinity changes in both formulations. Conclusion: An enhanced dissolution rate of glibenclamide is achievable through the combination of liquisolid and co-grinding technologies.

Formulation and Evaluation of Novel Bilayer Floating and Sustained Release Drug Delivery System of Diltiazem HCl

“…Besides, increasing the amount of DTZ in the outer layer gave a more linear release rate (Figures 3 and 4). Linear regression analysis and model [10] fitting showed that the optimized formulation followed linear probability which had higher value of correlation coefficient, RSQ. Accordingly, the release of DTZ was controlled by linear probability dissolution model.…”

Study of in vitro Therapeutic Equivalence of the 5 mg Glibenclamide Multi-source Tablets Respecting the Reference Medicine Product

“…These studies were carried out in a medium of phosphate buffer solution at pH 6.8.19 Wei H and Löbenberg R., 2006, showed that the dissolution media have an impact on the solubility of glibenclamide [16]. Azharshekoufeh et al, demonstrated that the dissolution speed of glibenclamide is optimal with a combination of liquid-solid and co-grinding technologies [27,28]. Mor et al, have reported that the GLI: POL2 granule fusion provides a higher dissolution rate (85.11%) compared to other polymers [29].…”

“…Unlike that reported by Pereda D and Martínez L., 2007, who when applying factor f2 determined that the generic glibenclamide medication is not equivalent, since the f2 was 41.1.26 Table 4 shows the values of the independent model parameters that characterize the drug release curve for glibenclamide drugs of 5 mg in the three study pH. In the case of dissolution efficiency (EF%), this parameter measures the area under the drug dissolution curve over a period of 90 minutes, and indicates the degree of absorption in vivo and can be theoretically related to the concentration curve plasma activity as a function of the time obtained by deconvolution techniques of in vivo data [28], exhibiting a value of 95.98% for the multi-source drug T, compared to the referent that exhibited a EF of 96.35%, both at a pH of 6.8. While the values of EF% for the multi-source T and reference R to pH 1.2 are 68.66 and 68.22%, and at pH 4.5 it is 56.59 and 59.24%, respectively; In this regard, the resulting value is greater than 50% for immediate-release medications, which is why it shows in vitro equivalence.…”

The Development of Glibenclamide-Saccharin Cocrystal Tablet Formulations to Increase the Dissolution Rate of the Drug

“…Several studies have been reported about methods improving glibenclamide solubility such as fast dissolving tablet (FDT) [6], lipid nanocrystal [7], nanoparticles [8,9], solid dispersion [10,11], selfemulsifying drug delivery systems (SEEDS) [12] and liquisolid technology [13]. Cocrystal is one method that can increase the solubility of the API [14].…”