Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics

In the present study, co-crystals (CCs) of Paliperidone (PPD) with coformers like benzoic acid (BA) and P-amino benzoic acid (PABA) were synthesized and characterized to improve the physicochemical properties and dissolution rate. CCs were prepared by the solvent evaporation (SE) technique and were...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Radha-Rani Earle, Venkata-Radha Gadela
Formato:	article
Lenguaje:	SR
Publicado:	Pharmaceutical Association of Serbia, Belgrade, Serbia 2021
Materias:	paliperidone cocrystal coformer solubility dissolution Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/b86944cd7ee04a94a8afe94c6d04f2cc
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:b86944cd7ee04a94a8afe94c6d04f2cc
record_format	dspace
spelling	oai:doaj.org-article:b86944cd7ee04a94a8afe94c6d04f2cc2021-12-05T18:01:41ZEngineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics0004-19632217-876710.5937/arhfarm71-32997https://doaj.org/article/b86944cd7ee04a94a8afe94c6d04f2cc2021-01-01T00:00:00Zhttps://scindeks-clanci.ceon.rs/data/pdf/0004-1963/2021/0004-19632105393R.pdfhttps://doaj.org/toc/0004-1963https://doaj.org/toc/2217-8767In the present study, co-crystals (CCs) of Paliperidone (PPD) with coformers like benzoic acid (BA) and P-amino benzoic acid (PABA) were synthesized and characterized to improve the physicochemical properties and dissolution rate. CCs were prepared by the solvent evaporation (SE) technique and were compared with the products formed by neat grinding (NG) and liquid assisted grinding (LAG) in their enhancement of solubility. The formation of CCs was confirmed by the IR spectroscopy, powder X-ray diffraction and thermal analysis methods. The saturation solubility studies indicate that the aqueous solubility of PPD-BA and PPD-PABA CCs was significantly improved to 1.343±0.162mg/ml and 1.964±0.452mg/ml, respectively, in comparison with the PPD solubility of 0.473mg/ml. This increase in solubility is 2.83-and 3.09-fold, respectively. PPD exhibited a poor dissolution of 37.8% in 60min, while the dissolution of the CCs improved tremendously to 96.07% and 89.65% in 60min. CCs of PPD with BA and PABA present a novel approach to overcome the solubility challenges of poorly water-soluble drug PPD.Radha-Rani EarleVenkata-Radha GadelaPharmaceutical Association of Serbia, Belgrade, SerbiaarticlepaliperidonecocrystalcoformersolubilitydissolutionPharmacy and materia medicaRS1-441SRArhiv za farmaciju, Vol 71, Iss 5, Pp 393-409 (2021)
institution	DOAJ
collection	DOAJ
language	SR
topic	paliperidone cocrystal coformer solubility dissolution Pharmacy and materia medica RS1-441
spellingShingle	paliperidone cocrystal coformer solubility dissolution Pharmacy and materia medica RS1-441 Radha-Rani Earle Venkata-Radha Gadela Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics
description	In the present study, co-crystals (CCs) of Paliperidone (PPD) with coformers like benzoic acid (BA) and P-amino benzoic acid (PABA) were synthesized and characterized to improve the physicochemical properties and dissolution rate. CCs were prepared by the solvent evaporation (SE) technique and were compared with the products formed by neat grinding (NG) and liquid assisted grinding (LAG) in their enhancement of solubility. The formation of CCs was confirmed by the IR spectroscopy, powder X-ray diffraction and thermal analysis methods. The saturation solubility studies indicate that the aqueous solubility of PPD-BA and PPD-PABA CCs was significantly improved to 1.343±0.162mg/ml and 1.964±0.452mg/ml, respectively, in comparison with the PPD solubility of 0.473mg/ml. This increase in solubility is 2.83-and 3.09-fold, respectively. PPD exhibited a poor dissolution of 37.8% in 60min, while the dissolution of the CCs improved tremendously to 96.07% and 89.65% in 60min. CCs of PPD with BA and PABA present a novel approach to overcome the solubility challenges of poorly water-soluble drug PPD.
format	article
author	Radha-Rani Earle Venkata-Radha Gadela
author_facet	Radha-Rani Earle Venkata-Radha Gadela
author_sort	Radha-Rani Earle
title	Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics
title_short	Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics
title_full	Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics
title_fullStr	Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics
title_full_unstemmed	Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics
title_sort	engineering cocrystals of paliperidone with enhanced solubility and dissolution characteristics
publisher	Pharmaceutical Association of Serbia, Belgrade, Serbia
publishDate	2021
url	https://doaj.org/article/b86944cd7ee04a94a8afe94c6d04f2cc
work_keys_str_mv	AT radharaniearle engineeringcocrystalsofpaliperidonewithenhancedsolubilityanddissolutioncharacteristics AT venkataradhagadela engineeringcocrystalsofpaliperidonewithenhancedsolubilityanddissolutioncharacteristics
_version_	1718371260230008832

Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics

Ejemplares similares