Relationship Between Phase Solubility Diagrams and Crystalline Structures During Dissolution of Cimetidine/Cyclodextrin Complex Crystals

Using singular value decomposition to analyze drug/β-cyclodextrin mixtures: insights from X-ray powder diffraction patterns

“…Namely, the CIM/β-CD complex formed the polymorph different from the plain β-CD. 51 Such channel form was not found in the INM/β-CD, DCF/β-CD, and FAM/β-CD mixtures. The signal at the two by theta angle of 12.02 degrees would be of Millar's indices of hkl = 002 (corresponding to the signal at the two by theta angle of 12.18 degrees in the reference diffractogram of the channel form).…”

“…As previously reported, the CIM complexes with β-CD and γ-CD (the cyclic octamer of glucosides) formed the polymorph of channel form, while the non-complexed CDs and the CIM complex with α-CD (the cyclic hexamer of glucosides) induced the structure of the cage form, which was confirmed with the simulated pattern from BCDEXD03 (1994). 51 The channel form was verified with the diffraction angles of the para -hydroxybiphenyl complex with β-CD from the reference code OFAXID (2007).…”

“…2y from 5 to 40 degrees is customary in pharmaceutical analysis. 51 Angles smaller than 5 degrees fall within the range of X-ray Small-Angle Scattering (SAXS) measurements, which offer distinct information from the molecular-level details obtained from XRPD. 52 Whereas, the use of high theta (higher angle than 40 degrees) data is used to obtain resolution at a small distance and to obtain total scattering profiles (such as pair distribution functions, i.e., PDF, or similar Diff(r) functions), that are very useful in materials science.…”

Comparative study on the effects of the inclusion complexes of non-steroidal anti-inflammatory drugs with 2-hydroxypropyl-β-cyclodextrins on dissociation rates and supersaturation

“…RSC Pharmaceutics higher solubility of the API, then the API concentration-time diagram requires regression analysis as a linear correlation. If the dissociation curve traces a saturation curve, then non-linearly curve fitting with the Noyes-Whitney integral expression (eqn (4)) was applied using the Solver module of Microsoft Excel 2016 with the implemented GRG nonlinear option 39,42 C ¼ C eq À ðC eq À C 0 ÞexpðÀkStÞ ð 4Þ…”

Quantification of crystallinity during indomethacin crystalline transformation from α- to γ-polymorphic forms and of the thermodynamic contribution to dissolution in aqueous buffer and solutions of solubilizer

“…Additionally, the salt formation of an API affects the stability and dissolution performance of the solid dispersion. 10 In addition to the previous ingenuities of solid states, measures such as hydrotropes, [11][12][13] nanoparticulation, 2 chemical modications, 14 cyclodextrin inclusion complexes, 15 and pH adjustment 16 can be used to manipulate solubility. 17,18 Approximately 40% of market-approved medicines and 90% of molecules in the discovery pipeline have low aqueous solubility, while only 8% of new drug candidates exhibit high aqueous solubility and intestinal permeability.…”