Crystal products of lamotrigine-citric acid for improvement of in vitro drug release in simulated gastric fluid

Abstract

Crystal engineering is an integral part of the drug development research. Crystal forms can modify the physicochemical properties of the parent drug molecule. The present work was aimed at the synthesis and characterization of crystalline product of lamotrigine (LT), a FDA approved anti-epileptic drug, with citric acid (CA) to improve its release in gastric region and oral absorption. The crystalline products of LT-CA were developed by solvent evaporation method using ethanol-water as the solvent system. Appearance of new charac-teristic peaks in the FTIR spectra for the crystal products indicated formation of new crystal state. In DSC thermogram, melting point of the experimental crystal products was different than that of the pure drug. Further, formation of new crystalline phase was confirmed from XRD data through the identification of new sharp peaks for the selected crystal products. A higher cumulative percen-tage of drug release was observed for the crystal products than the free drug within 60 min of drug release in simulated gastric fluid. However, in vivo studies are warranted for the future technology transfer of the product at industrial scale.

Aspirin-hydrogel ocular film for topical delivery and ophthalmic anti-inflammation

“…In vitro dissolution of aspirin of the films was carried out in the USP type II dissolution apparatus (Electolab, TDT06L, India) by utilizing 200 ml phosphate buffer (pH 6.8) as dissolution media at 34.0 ± 0.2 °C and 50 rpm for 6 h. 18,[31][32][33] A piece of film, weighing between 55-72 mg was cut and attached to the glass slide using cyanoacrylate glue and carefully placed it into the bottom of the vessel containing the dissolution medium. At different time intervals, 10 ml of the samples were withdrawn through a membrane filter (0.45 µm, syringe driven) and the same volume was replaced in each vessel with fresh medium.…”

Preparation of Atorvastatin Calcium-Dipicolinic Acid Multicomponent Solids by Liquid-Assisted Grinding Method to Increase Solubility

“…DSC characterization produces a thermogram that can provide information about the thermal properties and solids phase transformation of the sample due to interactions between components in the sample (Satapathy et al, 2021;Thorat et al, 2021;Wicaksono et al, 2020). DSC thermograms of solids of atorvastatin calcium, dipicolinic acid, and atorvastatin calcium-dipicolinic acid are shown in Figure 3.…”

“…The molecules of atorvastatin calcium and dipicolinic acid in the multicomponent solids form intermolecular interactions that produce a new solids phase. The multicomponent solids atorvastatin calcium-dipicolinic acid has a different molecular arrangement than the individual solids of its constituent materials (Satapathy et al, 2021). Different molecular arrangements cause changes in the pattern of molecular arrangement in the solids system and produce new crystal packing with different crystal lattice energies (Volodin et al, 2020;Kilinkissa et al, 2020;Ejarque et al, 2021).…”

“…FTIR Spectra FTIR spectroscopy is a common technique for analyzing functional groups and intermolecular interactions in multicomponent solids (Salim et al, 2021). The presence of intermolecular interactions between constituent components in multicomponent solids is indicated by changes in the intensity and shift of absorption peaks in the FTIR spectra of multicomponent solids compared to absorption peaks of constituent materials (Hermanto et al, 2020;Satapathy et al, 2021). The FTIR spectra of atorvastatin calcium, dipicolinic acid, and atorvastatin calcium -dipicolinic acid are shown in Figure 4.…”

Improved dissolution of ibuprofen after crystallization from polymeric solution: Correlation with crystal parameter

“…Similar reports for the use of water as release medium for poorly soluble drugs have already been reported earlier including ibuprofen. 17,[23][24][25][26][27][28][29][30][31][32][33] Hu et al reported in vitro drug release of IBU from the experimental micro emulsion in distilled water. 26 It was found that in vitro release profiles of IBU did not show much change in different drug release medium, i.e.…”