Hydrated Moxonidine SaccharinateSalt: Synthesis, Characterization, Crystal structure determination and dissolution enhancement

Saccharinates of active pharmaceutical ingredients (APIs) are often prepared for improving different physical properties like solubility, bioavailability,and stability of the drug product. Present work deals with the preparation, characterization and crystal structure determination of a novel salt Moxonidine saccharinate hydrate (MSH) with improved solubility. Preliminary characterization by TGA (thermo-gravimetric analysis), DSC (differential scanning calorimetry)and XRPD (X-ray powder diffraction) indicated the formation of a novel solid form. Further, the solid form was characterized by SC-XRD (single crystal XRD) to understand the supramolecular orientation of Moxonidine and saccharinate. The single crystal X-ray diffraction data indicated that the MSH has Moxonidine cation, saccharinateanion and water in 1:1:1 molar ratio, having N(+)-H----N(-) type hydrogen bonding between saccharin and Moxonidine. The MSH crystallized into the triclinic space group P-1 [a = 8.3239(14), b = 9.0147(15) and c = 13.723(2) A; α = 84.037(2), β = 89.214(2) and γ = 74.187(2) °, Z = 2]. MSH has shown significant improvement in dissolution rate (p