改善紫杉烷类药物低水溶性和低渗透性的策略探讨

被引：12

作者：

郝天云 ^{[1
]}

魏元锋 ^{[1
]}

钱帅 ^{[1
]}

张建军 ^{[2
]}

高缘 ^{[1
]}

机构：

[1] 中国药科大学中药学院

[2] 中国药科大学药学院

来源：

药学学报 | 2018年 / 01期

关键词：

紫杉烷类药物; 口服制剂; 低水溶性; 低渗透性;

D O I：

暂无

中图分类号：

R943 [制剂学];

学科分类号：

100702 [药剂学];

摘要：

紫杉烷类药物作为新一代抗肿瘤药物,对卵巢癌、乳腺癌、非小细胞肺癌及头颈癌等恶性肿瘤均具有良好的临床疗效,然而低水溶性和低渗透性导致的低口服生物利用度严重限制了其口服制剂的开发。目前,已上市制剂均非口服,所开发成的注射剂,因含有大量表面活性剂和有机溶媒,存在体液潴留、超敏反应等不良反应,且注射给药患者用药顺应性差,将其开发成口服制剂是未来紫杉烷类药物发展的方向。作者结合所在课题组对紫杉烷类药物的研究和近几年相关文献,探讨并分析改善该类药物的水溶性和渗透性进而提高其口服生物利用度的技术策略,其中着重探讨了制剂晶体学技术在该领域的应用前景,最终为紫杉烷类药物口服制剂的开发提供理论基础和研究方向。

引用

页码：54 / 61

页数：8

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