Pharma Innovation Lab, Department of Pharmaceutical Sciences & Technology, Maharaja Ranjit Singh Punjab Technical University, Bathinda, 151001, Punjab, India.
University Center of Excellence in Research, Baba Farid University of Health Sciences, Faridkot, 151203, India.
Ther Deliv. 2024;15(9):653-666. doi: 10.1080/20415990.2024.2377948. Epub 2024 Sep 3.
In this study, we aimed to prepare enteric encapsulated spheroids containing inclusion complex using quality by design approach. A Box-Behnken design was employed to determine effects of variables on selected responses. Risk assessment was conducted using Ishikawa fishbone diagram. A model with a -value was less than 0.5 for being a significant error of model was determined based on significance 'lack of fit' value. Spheroids were formulated using the extrusion spheronization technique and were characterized using analytical techniques. release was performed in both acidic (pH 1.2) and simulated intestinal (pH 6.8) conditions. Permeability studies demonstrated tenfold enhancement compared with arteether. studies further validated increase of 51.8% oral bioavailability. studies revealed 3.4-fold enhancement in antimalarial activity compared with arteether. These findings highlight effectiveness of inclusion complexation technique as a viable approach to enhance solubility and bioavailability for drugs with low aqueous solubility.
在这项研究中，我们旨在使用质量源于设计方法制备包含包合物的肠溶性包封微球。采用 Box-Behnken 设计来确定变量对选定响应的影响。使用石川图进行风险评估。根据显著“拟合不足”值确定模型的 - 值小于 0.5 的模型为显著误差。使用挤出滚圆技术制备微球，并使用分析技术对其进行表征。在酸性（pH 1.2）和模拟肠内（pH 6.8）条件下进行释放。与青蒿琥酯相比，渗透性研究显示出十倍的增强。研究进一步验证了口服生物利用度提高了 51.8%。研究表明，与青蒿琥酯相比，抗疟活性提高了 3.4 倍。这些发现强调了包合技术作为提高低水溶性药物溶解度和生物利用度的可行方法的有效性。
