New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization
Cocrystallization is an important route to tuning the solubility in drugs development, including improving and reducing. Five cocrystals of aripiprazole (ARI) with resveratrol (RSV) and kaempferol (KAE), ARI-RSV, ARI<sub>2</sub>-RSV<sub>1</sub>·MeOH, ARI-KAE, ARI-KAE·EtOH, AR...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/26/9/2414 |
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| author | Wenwen Liu Ru Ma Feifei Liang Chenxin Duan Guisen Zhang Yin Chen Chao Hao |
| author_facet | Wenwen Liu Ru Ma Feifei Liang Chenxin Duan Guisen Zhang Yin Chen Chao Hao |
| author_sort | Wenwen Liu |
| collection | DOAJ |
| description | Cocrystallization is an important route to tuning the solubility in drugs development, including improving and reducing. Five cocrystals of aripiprazole (ARI) with resveratrol (RSV) and kaempferol (KAE), ARI-RSV, ARI<sub>2</sub>-RSV<sub>1</sub>·MeOH, ARI-KAE, ARI-KAE·EtOH, ARI-KAE·IPA, were synthesized and characterized. The single crystal of ARI<sub>2</sub>-RSV<sub>1</sub>·MeOH, ARI-KAE·EtOH, and ARI-KAE·IPA were analyzed by single crystal X-ray diffraction (SCXRD). The SCXRD showed multiple intermolecular interactions between API and the coformers, including hydrogen bond, halogen bond, and π-π interactions. Dissolution rate of the two nonsolvate ARI-RSV and ARI-KAE cocrystals were investigated through powder dissolution experiment in pH = 4.0 acetate buffer and pH = 6.8 phosphate buffer. The result showed that RSV could reduce the dissolution rate and solubility of ARI in both medium through cocrystallization. However, KAE improved the dissolution rate and solubility of ARI in pH = 4.0 medium, on the contrary, the two solubility indicators of ARI were both reduced for ARI-KAE cocrystal. |
| first_indexed | 2024-03-10T12:08:05Z |
| format | Article |
| id | doaj.art-dc356333e88d46c99d17f27866485722 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T12:08:05Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-dc356333e88d46c99d17f278664857222023-11-21T16:28:38ZengMDPI AGMolecules1420-30492021-04-01269241410.3390/molecules26092414New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through CocrystallizationWenwen Liu0Ru Ma1Feifei Liang2Chenxin Duan3Guisen Zhang4Yin Chen5Chao Hao6School of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaSchool of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaSchool of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaSchool of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaSchool of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaSchool of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaSchool of Pharmacy, Jiangsu Ocean University, Lianyungang 222005, ChinaCocrystallization is an important route to tuning the solubility in drugs development, including improving and reducing. Five cocrystals of aripiprazole (ARI) with resveratrol (RSV) and kaempferol (KAE), ARI-RSV, ARI<sub>2</sub>-RSV<sub>1</sub>·MeOH, ARI-KAE, ARI-KAE·EtOH, ARI-KAE·IPA, were synthesized and characterized. The single crystal of ARI<sub>2</sub>-RSV<sub>1</sub>·MeOH, ARI-KAE·EtOH, and ARI-KAE·IPA were analyzed by single crystal X-ray diffraction (SCXRD). The SCXRD showed multiple intermolecular interactions between API and the coformers, including hydrogen bond, halogen bond, and π-π interactions. Dissolution rate of the two nonsolvate ARI-RSV and ARI-KAE cocrystals were investigated through powder dissolution experiment in pH = 4.0 acetate buffer and pH = 6.8 phosphate buffer. The result showed that RSV could reduce the dissolution rate and solubility of ARI in both medium through cocrystallization. However, KAE improved the dissolution rate and solubility of ARI in pH = 4.0 medium, on the contrary, the two solubility indicators of ARI were both reduced for ARI-KAE cocrystal.https://www.mdpi.com/1420-3049/26/9/2414cocrystalaripiprazoleresveratrolkaempferoldissolution rate |
| spellingShingle | Wenwen Liu Ru Ma Feifei Liang Chenxin Duan Guisen Zhang Yin Chen Chao Hao New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization Molecules cocrystal aripiprazole resveratrol kaempferol dissolution rate |
| title | New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization |
| title_full | New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization |
| title_fullStr | New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization |
| title_full_unstemmed | New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization |
| title_short | New Cocrystals of Antipsychotic Drug Aripiprazole: Decreasing the Dissolution through Cocrystallization |
| title_sort | new cocrystals of antipsychotic drug aripiprazole decreasing the dissolution through cocrystallization |
| topic | cocrystal aripiprazole resveratrol kaempferol dissolution rate |
| url | https://www.mdpi.com/1420-3049/26/9/2414 |
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