Adam Mickiewicz University in Poznań, Faculty of Chemistry, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
Adam Mickiewicz University in Poznań, Faculty of Chemistry, Uniwersytetu Poznańskiego 8, 61-614 Poznań, Poland.
J Colloid Interface Sci. 2021 Mar 15;586:673-682. doi: 10.1016/j.jcis.2020.10.137. Epub 2020 Nov 13.
Paracetamol is the most commonly used antipyretic and analgesic drug in the world. The key challenge in paracetamol therapy is associated with the frequency of the dosing. Depending on the gastric filling within 10-20 min paracetamol is released and rapidly absorbed from the gastrointestinal tract. Therefore, it must be taken three or four times a day. To address the dose challenge it is desirable that the paracetamol release profile follows the zero-order kinetic model (constant rate of drug release per unit time). This goal can be achieved by using a suitable porous carrier system. Herein, non-toxic wrinkled mesoporous carbons with unique morphology were synthesized via the hard template method as new carriers for paracetamol. These particles can precisely modulate the release of paracetamol over 24 h in a simulated gastric fluid according to the zero-order kinetic model completely eliminating the initial burst release. Overall, these systems could significantly enhance the bioavailability of paracetamol and prolong its therapeutic effect in numerous diseases such as cold, flu, COVID-19, and severe pain.
对乙酰氨基酚是世界上使用最广泛的解热镇痛药。对乙酰氨基酚治疗的关键挑战与给药频率有关。根据 10-20 分钟内胃的充盈情况，对乙酰氨基酚从胃肠道中迅速释放和吸收。因此，它必须每天服用三到四次。为了解决剂量挑战，希望对乙酰氨基酚的释放曲线遵循零级动力学模型（单位时间内药物释放的恒定速率）。这一目标可以通过使用合适的多孔载体系统来实现。本文通过硬模板法合成了无毒的皱状介孔碳，作为对乙酰氨基酚的新型载体，具有独特的形态。这些颗粒可以根据零级动力学模型精确控制对乙酰氨基酚在模拟胃液中的释放长达 24 小时，完全消除初始突释。总的来说，这些系统可以显著提高对乙酰氨基酚的生物利用度，并延长其在感冒、流感、COVID-19 和严重疼痛等多种疾病中的治疗效果。
