Synthesis, characterization and solubility of a new anthelmintic salt: Mebendazole nitrate

Rational design, supramolecular synthesis and solid state characterization of two bicomponent solid forms of mebendazole

“…20 In contrast, there is not much literature about multicomponent drug crystals incorporating perchloric acid and. 21 among the cocrystals and salts reported in the literature [23][24][25][26][27][28] , including one nitrate salt previously reported by us 29 .…”

“…After 48 hours in contact with the solvent, samples of MBZH⋅ClO 4 salt suffered a transformation process. As shown in Figure S10, the comparison of powder X-ray diffraction patterns of those samples, before and after the experiment, with those of MBZ polymorphs, shows that MBZH⋅ClO 4 transforms into MBZ A while previous reports indicate that other MBZ salts transforms into MBZ C in similar conditions 29,30 . This transformation can be justified by the great difference in solubility of the two components of the salt: the perchlorate anions completely dissolve in the solution, while the MBZ molecules precipitate to form the polymorph A.…”

“…Drug salts usually tend to convert to the raw APIs. Previous reports show that MBZ salts undergo a solvent-mediated transformation to pure MBZ polymorph C 29,30 . Here we focus mainly on the description of the crystal structure of these systems, the study of its thermal stability and the corresponding suspension stability of both new solid forms.…”

Analysis of Structure-Property Relationship for an Anthelmintic Drug, Mebendazole Nitrate Salt, using Density Functional Theory Approach

“…The optimized molecular structure of MBZ-N obtained from GAUSSIAN 09W program, calculated at B3LYP 6-311++G(d,p) is shown in Figure 1. The geometrical parameters such as bond lengths, bond angles and dihedral angles obtained fromoptimized MBZ-N structure compared with experimental values [9]are presented in Table1.…”

“…Therefore, many multicomponent structures from pure polymorph A has been synthesized and studied for fiding a better therapeutic activity level and greater solubility [6][7][8]. Recently, new MBZ multicomponent, Mebendazole nitrate salt (MBZ-N) has been synthesized by Eduardo L. Gutierrez et al [9]. To the best of our knowledge Mebendazole nitrate salt (MBZ-N) has not been investigated at theoritical level.…”