The Development of Lipid-Based Sorafenib Granules to Enhance the Oral Absorption of Sorafenib.
The Development of Lipid-Based Sorafenib Granules to Enhance the Oral Absorption of Sorafenib.
复制标题
DOI：
10.3390/pharmaceutics15122691
复制
发表时间：
2023-11-28
期刊：
影响因子：
5.4
通讯作者：
Dong X
中科院分区：
文献类型：
--
作者：
Mans JC;Dong X
索拉非尼（Sorafenib， SFN）是一种具有巨大治疗潜力的抗癌多激酶抑制剂。然而，SFN的水溶性较低，这限制了其口服吸收。脂质和表面活性剂具有改善水不溶性药物溶解度的潜力。因此，本研究的目的是开发新型脂基SFN颗粒，以改善SFN的口服吸收。用稳定的二元脂质混合物包被SFN粉末，然后在Aeroperl 300上吸附，形成载药量为10%的干燥SFN颗粒。SFN颗粒在室温下至少稳定3个月。与SFN粉相比，SFN颗粒显著增加了模拟胃液和模拟肠液中SFN的释放。对大鼠口服SFN颗粒和散的药代动力学和组织分布进行了测定。与SFN粉末相比，SFN颗粒显著增加了SFN的吸收。总之，脂基SFN颗粒提供了一种很有前途的方法来增强SFN的口服吸收。
Sorafenib (SFN) is an anticancer multi-kinase inhibitor with great therapeutic potential. However, SFN has low aqueous solubility, which limits its oral absorption. Lipids and surfactants have the potential to improve the solubility of water-insoluble drugs. The aim of this study is thus to develop novel lipid-based SFN granules that can improve the oral absorption of SFN. SFN powder was coated with a stable binary lipid mixture and then absorbed on Aeroperl 300 to form dry SFN granules with 10% drug loading. SFN granules were stable at room temperature for at least three months. Compared to SFN powder, SFN granules significantly increased SFN release in simulated gastric fluid and simulated intestinal fluid with pancreatin. Pharmacokinetics and tissue distribution of SFN granules and SFN powder were measured following oral administration to Sprague Dawley rats. SFN granules significantly increased SFN absorption compared to SFN powder. Overall, the lipid-based SFN granules provide a promising approach to enhancing the oral absorption of SFN.
登录
查看更多内容
影响因子：
158.5
作者：
Llovet, Josep M.;Ricci, Sergio;Bruix, Jordi
通讯作者：
Bruix, Jordi
影响因子：
11.2
作者：
Wilhelm, SM;Carter, C;Trail, PA
通讯作者：
Trail, PA
影响因子：
2.5
作者：
Bobin-Dubigeon, Christine;Heurgue-Berlot, Alexandra;Bard, Jean-Marie
通讯作者：
Bard, Jean-Marie
影响因子：
--
作者：
Sandhya, Pamu;Poornima, Pamu;Bhikshapathi, Darna V. R. N.
通讯作者：
Bhikshapathi, Darna V. R. N.
多西他赛口服配方的两步生物溶解方法的设计和评估。
影响因子：
3.3
作者：
通讯作者：
--