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Composing Novel Diclofenac Potassium and L-Proline Salt Cocrystal as a Strategy to Increase Solubility and Dissolution
Nugrahani I.a, Komara S.W.a, Horikawa A.b, Uekusa H.b
a School of Pharmacy, Bandung Institute of Technology, Indonesia
b Department of Chemistry, School of Science, Tokyo Institute of Technology, Japan
[vc_row][vc_column][vc_row_inner][vc_column_inner][vc_separator css=”.vc_custom_1624529070653{padding-top: 30px !important;padding-bottom: 30px !important;}”][/vc_column_inner][/vc_row_inner][vc_row_inner layout=”boxed”][vc_column_inner width=”3/4″ css=”.vc_custom_1624695412187{border-right-width: 1px !important;border-right-color: #dddddd !important;border-right-style: solid !important;border-radius: 1px !important;}”][vc_empty_space][megatron_heading title=”Abstract” size=”size-sm” text_align=”text-left”][vc_column_text]© 2020 American Pharmacists Association®This research dealt with the multicomponent crystal developed from diclofenac potassium and L-proline to improve the pharmaceutical performance of this anti-inflammatory drug. Slow evaporation of the component mixture at a 1:1 M ratio, supported by ultrasonication, yielded a new salt cocrystal, which was characterized using thermal analysis, Karl Fischer titration, infrared spectrophotometry, powder diffractometry, and single crystal diffractometry. This salt cocrystal was confirmed as a tetrahydrate that comprised diclofenac potassium, L-proline, and water (1:1:4), named DKPH. The new salt cocrystal enhanced the solubility of diclofenac potassium by up to 3.56 folds and accelerated the intrinsic dissolution rate of 3.36 folds. It was supported by the solid and solution phase intermolecular interaction study. A different phase, which indicated a monohydrate form of the salt cocrystal, was found from the low humidity chamber during the isotherm sorption study. However, the tetrahydrate, DKPH, was proven as a stable form under ambient conditions.[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Author keywords” size=”size-sm” text_align=”text-left”][vc_column_text]Crystallization,Diclofenac,Drug Stability,Proline,Solubility[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Indexed keywords” size=”size-sm” text_align=”text-left”][vc_column_text]Diclofenac potassium,Hydrate,Intrinsic dissolution,L-proline,Multicomponent,Pseudo polymorph,Salt cocrystal,Solubility,Solute–solute interaction,Stability[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Funding details” size=”size-sm” text_align=”text-left”][vc_column_text][{‘$’: “This research was supported by Research, Community Service, and Innovation Program, from the Research and Community Service Institution, Bandung Institute of Technology, Indonesia, contract number 021.1/SK/I1.C03/KP2019; and collaborated with H. Uekusa’s Laboratory, Department Chemistry and Material Sciences, Tokyo Institute of Technology, was supported by JSPS KAKENHI, Japan Grant Number JP17K05745 and 20H04661 (HU).”}, {‘$’: “This research was supported by Research, Community Service, and Innovation Program, from the Research and Community Service Institution, Bandung Institute of Technology , Indonesia, contract number 021.1/SK/I1.C03/KP2019; and collaborated with H. Uekusa’s Laboratory, Department Chemistry and Material Sciences, Tokyo Institute of Technology, was supported by JSPS KAKENHI, Japan Grant Number JP17K05745 and 20H04661 (HU).”}][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”DOI” size=”size-sm” text_align=”text-left”][vc_column_text]https://doi.org/10.1016/j.xphs.2020.08.002[/vc_column_text][/vc_column_inner][vc_column_inner width=”1/4″][vc_column_text]Widget Plumx[/vc_column_text][/vc_column_inner][/vc_row_inner][/vc_column][/vc_row][vc_row][vc_column][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][/vc_column][/vc_row]