Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals
Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with o...
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| Format: | Article |
| Language: | English |
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MDPI AG
2020-11-01
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| Series: | Crystals |
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| Online Access: | https://www.mdpi.com/2073-4352/10/11/996 |
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| author | Zhengxuan Liang Hongbo Chen Chenguang Wang Changquan Calvin Sun |
| author_facet | Zhengxuan Liang Hongbo Chen Chenguang Wang Changquan Calvin Sun |
| author_sort | Zhengxuan Liang |
| collection | DOAJ |
| description | Loratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development. |
| first_indexed | 2024-03-10T15:07:25Z |
| format | Article |
| id | doaj.art-c422a6b89b4d4aeb9a752d1420b81986 |
| institution | Directory Open Access Journal |
| issn | 2073-4352 |
| language | English |
| last_indexed | 2024-03-10T15:07:25Z |
| publishDate | 2020-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Crystals |
| spelling | doaj.art-c422a6b89b4d4aeb9a752d1420b819862023-11-20T19:38:27ZengMDPI AGCrystals2073-43522020-11-01101199610.3390/cryst10110996Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid CocrystalsZhengxuan Liang0Hongbo Chen1Chenguang Wang2Changquan Calvin Sun3Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USAPharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USAPharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USAPharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USALoratadine (Lor) is an antihistamine drug commonly used to relieve the symptoms of allergy. It has high permeability but low solubility under physiological conditions. To overcome the problem of low solubility, we synthesized and characterized two Loratadine multi-component crystalline phases with oxalic acid (Oxa), i.e., a 1:1 Lor-Oxa conjugate acid-base (CAB) cocrystal (Lor-Oxa CAB) and a 2:1 Lor-Oxa cocrystal monohydrate (Lor-Oxa hydrate). Both cocrystals exhibited an enhanced solubility and intrinsic dissolution rate (IDR) compared to Lor and adequate physical stability. The intrinsic dissolution rate of Lor-Oxa CAB is 95 times that of Lor, which makes it a promising candidate for tablet formulation development.https://www.mdpi.com/2073-4352/10/11/996cocrystalLoratadinesolubilityintrinsic dissolution ratecompression |
| spellingShingle | Zhengxuan Liang Hongbo Chen Chenguang Wang Changquan Calvin Sun Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals Crystals cocrystal Loratadine solubility intrinsic dissolution rate compression |
| title | Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals |
| title_full | Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals |
| title_fullStr | Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals |
| title_full_unstemmed | Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals |
| title_short | Discovery, Characterization, and Pharmaceutical Applications of Two Loratadine–Oxalic Acid Cocrystals |
| title_sort | discovery characterization and pharmaceutical applications of two loratadine oxalic acid cocrystals |
| topic | cocrystal Loratadine solubility intrinsic dissolution rate compression |
| url | https://www.mdpi.com/2073-4352/10/11/996 |
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