Crystal Engineering to Solidify and Chemically Stabilize Oily dl-Butylphthalide
文献类型：期刊论文
| 作者 | Xia, Mengyuan1,2; Ding, Zhenfeng1,2; Tian, Fanyu1,3; Dai, Wenjuan1; Zhang, Zaiyong1; Zhu, Bingqing1; Mei, Xuefeng1,2
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| 刊名 | CRYSTAL GROWTH & DESIGN
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| 出版日期 | 2023-08-01 |
| 页码 | 11 |
| ISSN号 | 1528-7483 |
| DOI | 10.1021/acs.cgd.3c00637 |
| 通讯作者 | Zhu, Bingqing(zhubingq@simm.ac.cn) ; Mei, Xuefeng(xuefengmei@simm.ac.cn) |
| 英文摘要 | dl-3-n-Butylphthalide (dl-NBP)is a well-known neuroprotective drug used for the treatment of ischemicstroke. It is oily in appearance and vulnerable to oxygen and light,resulting in the only developed oral product being NBP soft capsules.However, this conventional dosage form suffers from unsatisfactoryabsorption due to water insolubility and extensive metabolism. Thiswork aimed to solidify and stabilize dl-NBP through cocrystallizationand then combine crystalline NBP with solubilization technologiesfor solid dosage forms to enhance systemic exposure. Cocrystals of dl-NBP with 2,5-dihydroxybenzoic acid (NBP-2,5HBA), 3,5-dihydroxybenzoicacid (NBP-3,5HBA), gallic acid (NBP-GAA MH), and 5-hydroxyisophthalicacid (NBP-5HPA) were first discovered using liquid-assisted grindingand comprehensively characterized. The edible cocrystal NBP-GAA MHwith a melting point of 67 & DEG;C exhibited higher chemical stabilitythan the parent drug. The developed formulation of NBP-GAA MH showedconsiderable improvement in dissolution rates than NBP soft capsulesat pH 2.0 and 4.5. In in vivo study, the cocrystal formulation yielded1.7 and 1.9 times higher C (max) and AUC(0-8h) in rats than the commercial product. Therefore,cocrystallization promises to solidify and stabilize oily/liquid compoundsand enriches their dosage forms in drug development. Oily dl-butylphthalide can besolidified throughcocrystallizing with 2,5-dihydroxybenzoic acid, 3,5-dihydroxybenzoicacid, gallic acid, and 5-hydroxyisophthalic acid, and cocrystal withedible gallic acid demonstrates improved chemical stability and oralexposure. |
| WOS关键词 | ISCHEMIC-STROKE ; LIPOSOMES ; POLYMORPHS ; DRUG |
| 资助项目 | Shanghai Sailing Program[20YF1457400] |
| WOS研究方向 | Chemistry ; Crystallography ; Materials Science |
| 语种 | 英语 |
| 出版者 | AMER CHEMICAL SOC |
| WOS记录号 | WOS:001039161600001 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/306836]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Zhu, Bingqing; Mei, Xuefeng |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xia, Mengyuan,Ding, Zhenfeng,Tian, Fanyu,et al. Crystal Engineering to Solidify and Chemically Stabilize Oily dl-Butylphthalide[J]. CRYSTAL GROWTH & DESIGN,2023:11. |
| APA | Xia, Mengyuan.,Ding, Zhenfeng.,Tian, Fanyu.,Dai, Wenjuan.,Zhang, Zaiyong.,...&Mei, Xuefeng.(2023).Crystal Engineering to Solidify and Chemically Stabilize Oily dl-Butylphthalide.CRYSTAL GROWTH & DESIGN,11. |
| MLA | Xia, Mengyuan,et al."Crystal Engineering to Solidify and Chemically Stabilize Oily dl-Butylphthalide".CRYSTAL GROWTH & DESIGN (2023):11. |
入库方式： OAI收割
来源：上海药物研究所
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