Department of Pharmaceutical Chemistry, Government College of Pharmacy, Karad Maharashtra-415124, India.
Acta Pharm. 2009 Dec;59(4):453-61. doi: 10.2478/v10007-009-0037-4.
Dissolution behaviour of a poorly water-soluble drug, tadalafil, from its solid dispersion systems with poloxamer 407 has been investigated. Solid dispersion systems of tadalafil were prepared with poloxamer 407 in 1:0.5, 1:1.5 and 1:2.5 ratios using the melting method. Characterization of binary systems with FTIR and XRPD studies demonstrated the presence of strong hydrogen bonding interactions, a significant decrease in crystallinity and the possibility of existence of amorphous entities of the drug. In the binary systems tested, 1:0.5 proportion of tadalafil/poloxamer 407 showed rapid dissolution of tadalafil (DE(30) 70.9 + or - 3.6 %). In contrast, higher proportions of poloxamer 407 (1:1.5 and 1:2.5) offered no advantage towards dissolution enhancement of the drug, indicating altered rheological characteristics of the polymer at its higher concentration, which might have retarded the release rate of tadalafil.
已研究了将泊洛沙姆 407 用作固体分散体系统来改善他达拉非（一种水溶性差的药物）的溶解行为。使用熔融法，将泊洛沙姆 407 与他达拉非以 1:0.5、1:1.5 和 1:2.5 的比例制成固体分散体系统。通过 FTIR 和 XRPD 研究对二元系统进行了表征，结果表明存在强氢键相互作用，药物的结晶度显著降低，并且可能存在无定形物质。在所测试的二元系统中，他达拉非/泊洛沙姆 407 的 1:0.5 比例显示出他达拉非的快速溶解（DE(30) 70.9 ± 3.6%）。相比之下，泊洛沙姆 407 的较高比例（1:1.5 和 1:2.5）对药物的溶解增强没有优势，这表明聚合物在较高浓度下的流变特性发生了变化，这可能会延迟他达拉非的释放速率。
