College of Pharmacy, Freie Universität Berlin, Kelchstrasse 31, 12169 Berlin, Germany; Faculty of Pharmacy, Padjadjaran University Sumedang, Jl. Raya Jatinangor Km 21,5, Sumedang 45363, Indonesia.
College of Pharmacy, Freie Universität Berlin, Kelchstrasse 31, 12169 Berlin, Germany; College of Pharmacy, University of Sulaimani, City Center Campus, Sulaimani, Kurdistan Region, Iraq.
Int J Pharm. 2020 Mar 15;577:119050. doi: 10.1016/j.ijpharm.2020.119050. Epub 2020 Jan 25.
The aim of this work was to develop a mathematical model to estimate the drug release from a conventional single-compartment reservoir pellet and extend its applicability to multi-compartment reservoir pellets. Conventional pellets were prepared by layering the drug onto starter-core then applying various ethylcellulose/HPC coatings for drug release control. Multi-layered pellets comprised a first drug layer of propranolol HCl (D) followed by a first controlled release coating (C) and consecutively a second drug layer of carbamazepine or caffeine (D) and then a second controlled-release coating (C). Drug release from single- and multi-compartment pellets generally increased with an increase of the water-soluble HPC in the coatings. The response described a sigmoidal curve, which agreed with a cumulative normal distribution function. The developed mathematical model facilitated quantification of the drug release of pellets as a function of the porogen content and the coating level. Additionally, the model was applied successfully in multi-compartment pellets to calculate theses effects on the release of drugs with a broad range of aqueous solubility.
本工作旨在开发一种数学模型来估算从常规单室储库微丸中释放药物，并将其应用扩展到多室储库微丸。常规微丸是通过将药物分层到起始核芯上，然后施加各种乙基纤维素/HPC 涂层来控制药物释放来制备的。多层微丸包含盐酸普萘洛尔（D）的第一层药物，接着是第一层控释涂层（C），然后是卡马西平或咖啡因（D）的第二层药物，然后是第二层控释涂层（C）。单室和多室微丸的药物释放通常随着涂层中水溶性 HPC 的增加而增加。该响应描述了一个 S 形曲线，与累积正态分布函数一致。所开发的数学模型便于定量描述微丸的药物释放作为致孔剂含量和涂层水平的函数。此外，该模型成功应用于多室微丸，以计算这些对具有广泛水溶性的药物释放的影响。
