CXB-029(CXB-029) - 药物靶点：CB1R_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

CB1R

作用机制

CB1拮抗剂(大麻素受体CB1拮抗剂)

治疗领域

神经系统疾病内分泌与代谢疾病眼部疾病

在研适应症-

非在研适应症

中枢神经系统疾病青光眼肥胖+ [1]

原研机构

PharmaNess Neuroscience

在研机构-

非在研机构

CeNeRx BioPharma, Inc.

最高研发阶段终止药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 CXB-029 相关的临床结果

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100 项与 CXB-029 相关的转化医学

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100 项与 CXB-029 相关的专利（医药）

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1

项与 CXB-029 相关的文献（医药）

2019-10-01·Journal of Pharmaceutical Sciences3区 · 医学

In Vitro and In Vivo Evaluation of Core–Shell Mesoporous Silica as a Promising Water-Insoluble Drug Delivery System: Improving the Dissolution Rate and Bioavailability of Celecoxib With Needle-Like Crystallinity

3区 · 医学

Article

作者: Zhang, Shanqiang ; Huang, Haitao ; Zhu, Wenquan ; Jian, Baiyu ; Dong, Yan ; Sui, Xiaoyu ; Han, Cuiyan

The objective of our study was to prepare mesoporous silica nanoparticles with a core-shell structure (CSMSNs) and improve the dissolution and bioavailability of celecoxib (Cxb), a water-insoluble drug, by changing its needle-like crystal form. CSMSNs are prepared by a core-shell segmentation self-assembly method. The S_BET and V_t of CSMSNs were 890.65 m²/g and 1.23 cm³/g, respectively. Cxb was incorporated into CSMSNs by the solvent evaporation method. The gastrointestinal irritancy of the CSMSNs was evaluated by a gastric mucosa irritation test. In vitro dissolution and in vivo pharmacokinetic tests were carried out to study the improvement in the dissolution behavior and oral bioavailability of Cxb. In conclusion, gastric mucosa irritation study indicated the good biocompatibility of CSMSNs. The cumulative dissolution of CSMSNs-Cxb is 86.2% within 60 min in SIF solution, which may be ascribed to the crystal form change caused by control of the nanochannel for CSMSNs. Moreover, CSMSNs could enhance the 9.9-fold AUC of Cxb. The cumulative dissolution and bioavailability of Cxb were both significantly enhanced by CSMSNs. CSMSNs with a core-shell structure are suitable as a carrier for a poorly water-soluble drug (Cxb).

100 项与 CXB-029 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
中枢神经系统疾病	药物发现	美国	CeNeRx BioPharma, Inc.	2007-05-30
青光眼	药物发现	美国	CeNeRx BioPharma, Inc.	2007-05-30
肥胖	药物发现	美国	CeNeRx BioPharma, Inc.	2007-05-30
疼痛	药物发现	美国	CeNeRx BioPharma, Inc.	2007-05-30