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含青蒿琥酯的直肠栓剂制剂

Preparations of Rectal Suppositories Containing Artesunate.

作者信息

Persaud Suzanne, Eid Sandra, Swiderski Natalia, Serris Ioannis, Cho Hyunah

机构信息

School of Pharmacy and Health Sciences, Fairleigh Dickinson University, Florham Park, NJ 07932, USA.

出版信息

Pharmaceutics. 2020 Mar 2;12(3):222. doi: 10.3390/pharmaceutics12030222.

Abstract

Rectal artesunate suppositories are a useful option for pre-referral treatment of severe malaria, specifically in children under 6 years of age in remote malaria-endemic areas. The main challenges are to improve the solubility of drugs in the rectal fluids and prevent the product from turning rancid or melting in a tropical climate. In this short proof-of-concept study, three types of rectal suppositories of artesunate were prepared: (i) polyethylene glycol (PEG)-based suppositories carrying free artesunate (non-modified artesunate), (ii) PEG-based suppositories carrying artesunate-loaded micelles and (iii) 3D-printed suppositories carrying a PEG/artesunate mixture. Physical parameters of suppositories, release profiles of artesunate (the fastest to the slowest: ii≥i>iii) and thermostability (the most stable to the least stable: iii>ii>i) of suppositories at increased temperature were assessed to determine the advantages and disadvantages of each formulation.

摘要

直肠青蒿琥酯栓是严重疟疾转诊前治疗的一种有用选择,特别是在偏远疟疾流行地区的6岁以下儿童中。主要挑战是提高药物在直肠液中的溶解度,并防止产品在热带气候中变质或融化。在这项简短的概念验证研究中,制备了三种类型的青蒿琥酯直肠栓:(i)携带游离青蒿琥酯(未修饰青蒿琥酯)的聚乙二醇(PEG)基栓剂,(ii)携带载有青蒿琥酯的胶束的PEG基栓剂,以及(iii)携带PEG/青蒿琥酯混合物的3D打印栓剂。评估了栓剂的物理参数、青蒿琥酯的释放曲线(从最快到最慢:ii≥i>iii)以及在升高温度下栓剂的热稳定性(从最稳定到最不稳定:iii>ii>i),以确定每种制剂的优缺点。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/25f6/7150883/d56b6bf464d8/pharmaceutics-12-00222-g001.jpg

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