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...
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| Format: | Article |
| Language: | srp |
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Pharmaceutical Association of Serbia, Belgrade, Serbia
2021-01-01
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| Series: | Arhiv za farmaciju |
| Subjects: | |
| Online Access: | https://scindeks-clanci.ceon.rs/data/pdf/0004-1963/2021/0004-19632105393R.pdf |
| _version_ | 1819038189093912576 |
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| author | Radha-Rani Earle Venkata-Radha Gadela |
| author_facet | Radha-Rani Earle Venkata-Radha Gadela |
| author_sort | Radha-Rani Earle |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-21T08:33:21Z |
| format | Article |
| id | doaj.art-b86944cd7ee04a94a8afe94c6d04f2cc |
| institution | Directory Open Access Journal |
| issn | 0004-1963 2217-8767 |
| language | srp |
| last_indexed | 2024-12-21T08:33:21Z |
| publishDate | 2021-01-01 |
| publisher | Pharmaceutical Association of Serbia, Belgrade, Serbia |
| record_format | Article |
| series | Arhiv za farmaciju |
| spelling | doaj.art-b86944cd7ee04a94a8afe94c6d04f2cc2022-12-21T19:10:08ZsrpPharmaceutical Association of Serbia, Belgrade, SerbiaArhiv za farmaciju0004-19632217-87672021-01-0171539340910.5937/arhfarm71-329970004-19632105393REngineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristicsRadha-Rani Earle0Venkata-Radha Gadela1Maharajah's College of Pharmacy, Vizianagaram, IndiaGITAM Deemed to be University, GITAM Institute of Pharmacy, Visakhapatnam, IndiaIn 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.https://scindeks-clanci.ceon.rs/data/pdf/0004-1963/2021/0004-19632105393R.pdfpaliperidonecocrystalcoformersolubilitydissolution |
| spellingShingle | Radha-Rani Earle Venkata-Radha Gadela Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics Arhiv za farmaciju paliperidone cocrystal coformer solubility dissolution |
| title | 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_short | Engineering cocrystals of Paliperidone with enhanced solubility and dissolution characteristics |
| title_sort | engineering cocrystals of paliperidone with enhanced solubility and dissolution characteristics |
| topic | paliperidone cocrystal coformer solubility dissolution |
| url | https://scindeks-clanci.ceon.rs/data/pdf/0004-1963/2021/0004-19632105393R.pdf |
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