Abstract:The present study proved that grazing incidence X-ray diffraction is a potential novel research tool to reveal crystallographic transformations taking place on the surfaces of the tablets induced, for example, by compression pressure.
“…To understand variation in the phase transformation at the different regions of the tablets, depth profiling was carried out. In pharmaceutical context, GIXD has been employed previously to study phase transformation during dissolution (31) and compaction (22) and to evaluate effective penetration depth of X-rays in the tablets (32). In the current work, the potential of GIXD was further extended to evaluate the difference in stability of the different solid forms of three model drug substances towards the compaction.…”
Section: Discussionmentioning
confidence: 99%
“…For indomethacin and chlorpropamide, it has been observed that compaction leads to polymorphic transformation as well as amorphization (19)(20)(21). Compaction-induced amorphization was also observed for carbamazepine form III and tolbutamide form I (22). Two solvates of celecoxib, dimethyl acetamide and dimethyl formamide, have been shown to undergo desolvation during compaction (23).…”
Section: Introductionmentioning
confidence: 99%
“…The GIXD technique is unique in the sense that it can provide detailed information on the phase composition at the different depths parallel to the tablet surface (22,(30)(31)(32). As the surface is the first part of the tablet that comes into contact with dissolution medium, information on the surface layer is important with respect to the initial dissolution of the tablet.…”
With GIXD measurements, it was possible to probe the solid form composition at the different depths of the tablet surfaces and to obtain depth-dependent information on the compaction-induced amorphization, crystal disordering and dehydration.
“…To understand variation in the phase transformation at the different regions of the tablets, depth profiling was carried out. In pharmaceutical context, GIXD has been employed previously to study phase transformation during dissolution (31) and compaction (22) and to evaluate effective penetration depth of X-rays in the tablets (32). In the current work, the potential of GIXD was further extended to evaluate the difference in stability of the different solid forms of three model drug substances towards the compaction.…”
Section: Discussionmentioning
confidence: 99%
“…For indomethacin and chlorpropamide, it has been observed that compaction leads to polymorphic transformation as well as amorphization (19)(20)(21). Compaction-induced amorphization was also observed for carbamazepine form III and tolbutamide form I (22). Two solvates of celecoxib, dimethyl acetamide and dimethyl formamide, have been shown to undergo desolvation during compaction (23).…”
Section: Introductionmentioning
confidence: 99%
“…The GIXD technique is unique in the sense that it can provide detailed information on the phase composition at the different depths parallel to the tablet surface (22,(30)(31)(32). As the surface is the first part of the tablet that comes into contact with dissolution medium, information on the surface layer is important with respect to the initial dissolution of the tablet.…”
With GIXD measurements, it was possible to probe the solid form composition at the different depths of the tablet surfaces and to obtain depth-dependent information on the compaction-induced amorphization, crystal disordering and dehydration.
“…203 These changes were found to be localized on the surfaces of the tablets, and their degree decreased as a function of distance from the tablet surface. Samples of dry chlorpropamide Form-A were subjected to high pressure (5.5 GPa), but no evidence for a phase transition to Form-C could be obtained.…”
Section: Effects Associated With Secondary Processing Of Crystal Formsmentioning
“…During the manufacturing of drug products containing crystalline active pharmaceutical ingredients (APIs), drug crystals are often subjected to unit operations such as milling and compaction. It is well documented that these pharmaceutical processes can generate various types of defects in API crystals . These crystal defects represent regions of higher disorder and higher energy relative to the average overall energy of the crystalline material .…”
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