Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib.
Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib.
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DOI：
10.3390/pharmaceutics15061669
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发表时间：
2023-06-07
期刊：
影响因子：
5.4
通讯作者：
Jang DJ
中科院分区：
文献类型：
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作者：
Kim YH;Kim SB;Choi SH;Nguyen TT;Ahn SH;Moon KS;Cho KH;Sim TY;Heo EJ;Kim ST;Jung HS;Jee JP;Choi HG;Jang DJ
本研究的目的是开发和评价一种自微乳化给药系统（SMEDDS），以改善难水溶性奥拉帕尼的口服吸收。通过奥拉帕尼在各种油脂、表面活性剂和助表面活性剂中的溶解度试验，选择药用辅料。将所选材料以不同比例混合，确定了自乳化区域，并综合这些结果构建了伪三元相图。通过考察奥拉帕尼微乳的形态、粒径、zeta电位、药物含量和稳定性，确定了奥拉帕尼微乳的各种理化性质。此外，通过溶出度试验和药代动力学研究，也证实了奥拉帕尼的溶出度和吸收改善。在Capmul®MCM 10%、Labrasol®80%和PEG 400 10%的配方中获得最佳微乳液。制备的微乳液在水溶液中分散性好，且保持良好，不存在物理或化学稳定性问题。与粉末相比，奥拉帕尼的溶出曲线明显改善。由于奥拉帕尼的高溶出度，药代动力学参数也得到了很大的改善。综上所述，该微乳可作为奥拉帕尼等类似药物的有效制剂。
The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected. Self-emulsifying regions were identified by mixing the selected materials at various ratios, and a pseudoternary phase diagram was constructed by synthesizing these results. The various physicochemical properties of microemulsion incorporating olaparib were confirmed by investigating the morphology, particle size, zeta potential, drug content and stability. In addition, the improved dissolution and absorption of olaparib were also confirmed through a dissolution test and a pharmacokinetic study. An optimal microemulsion was generated in the formulation of Capmul® MCM 10%, Labrasol® 80% and PEG 400 10%. The fabricated microemulsions were well-dispersed in aqueous solutions, and it was also confirmed that they were maintained well without any problems of physical or chemical stability. The dissolution profiles of olaparib were significantly improved compared to the value of powder. Associated with the high dissolutions of olaparib, the pharmacokinetic parameters were also greatly improved. Taken together with the results mentioned above, the microemulsion could be an effective tool as a formulation for olaparib and other similar drugs.
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影响因子：
5.8
作者：
Jannin, Vincent;Chevrier, Stephanie;Demarne, Frederic
通讯作者：
Demarne, Frederic
影响因子：
5.4
作者：
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3.3
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影响因子：
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通讯作者：
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影响因子：
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