[Crystalline molecular complexes generated between surfactants and various additive compounds: an attempt to modify sparingly water soluble drugs to easily water soluble drugs].

[Crystalline molecular complexes generated between surfactants and various additive compounds: an attempt to modify sparingly water soluble drugs to easily water soluble drugs].
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[表面活性剂和各种添加剂化合物之间产生的结晶分子复合物:将难溶于水的药物改性为易溶于水的药物的尝试]。

DOI:
10.1002/chin.200145284
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发表时间:
2001
期刊:
Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
影响因子:
--
通讯作者:
N. Iimura
N. Iimura
中科院分区:
--
文献类型:
--
作者:
H. Hirata;N. Iimura

文献摘要

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已证实,离子表面活性剂,无论是阳离子还是阴离子,都能稳定地与各种芳香族化合物作为添加剂提供结晶分子络合物。在各种添加剂中,酚类化合物尤其有利于这两种表面活性剂的存在。除了这些添加剂,阳离子表面活性剂很容易与碱性物质,甚至与非极性物质,如联苯和菲,提供结晶分子络合物。对分离得到的表面活性剂分子络合物进行了X-射线分析。到目前为止,所获得的表面活性剂分子络合物的数量已超过200种或更多,其中30种或更多已进行了结构分析。结果表明,这些表面活性剂分子络合物是一种不同于母体的新型表面活性物质,对络合添加剂具有较好的增溶作用。我们将这些特性应用于难溶于水的药物作为复合添加剂,将其修饰成易溶于水的药物。与纯药物相比,得到的复合药物在溶解度和溶出度方面均有改善。
It has been established that ionic surfactants, whether cationic or anionic, provide crystalline molecular complexes stably with various aromatic compounds as additives. Among various additives phenolic compounds are especially favorable for both surfactant species. Other than these additives, cationic surfactants easily provide crystalline molecular complexes with basic materials and even with non-polar substances such as biphenyl and phenanthrene. The isolated surfactant molecular complexes were analyzed by X-ray. To date the number of the obtained surfactant molecular complexes exceeds two hundred species or more and thirty or more of them were structurally analyzed. These surfactant molecular complexes were shown to be novel surfactant species different from their mother species, supplied with enhanced solubility to the complex additives. We applied these characteristics to sparingly water soluble drugs as the complex additive to modify them into easily water soluble drugs. The obtained complex drugs revealed an improved behavior in solubility and dissolution rate compared with pure drugs.