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评估基于地质聚合物的药物输送系统对篡改的抵抗力。

Evaluation of the resistance of a geopolymer-based drug delivery system to tampering.

机构信息

Division for Applied Materials Science, Department of Engineering Sciences, The Ångström Laboratory, Uppsala University, Box 534, SE-751 21 Uppsala, Sweden.

Division for Applied Materials Science, Department of Engineering Sciences, The Ångström Laboratory, Uppsala University, Box 534, SE-751 21 Uppsala, Sweden.

出版信息

Int J Pharm. 2014 Apr 25;465(1-2):169-74. doi: 10.1016/j.ijpharm.2014.02.029. Epub 2014 Feb 17.

Abstract

Tamper-resistance is an important property of controlled-release formulations of opioid drugs. Tamper-resistant formulations aim to increase the degree of effort required to override the controlled release of the drug molecules from extended-release formulations for the purpose of non-medical use. In this study, the resistance of a geopolymer-based formulation to tampering was evaluated by comparing it with a commercial controlled-release tablet using several methods commonly used by drug abusers. Because of its high compressive strength and resistance to heat, much more effort and time was required to extract the drug from the geopolymer-based formulation. Moreover, in the drug-release test, the geopolymer-based formulation maintained its controlled-release characteristics after milling, while the drug was released immediately from the milled commercial tablets, potentially resulting in dose dumping. Although the tampering methods used in this study does not cover all methods that abuser could access, the results obtained by the described methods showed that the geopolymer matrix increased the degree of effort required to override the controlled release of the drug, suggesting that the formulation has improved resistance to some common drug-abuse tampering methods. The geopolymer matrix has the potential to make the opioid product less accessible and attractive to non-medical users.

摘要

耐篡改性能是阿片类药物控释制剂的一个重要性质。耐篡改制剂旨在增加破坏药物分子从控释制剂中非医疗用途释放所需的努力程度。在这项研究中,通过比较一种基于地质聚合物的制剂和一种商业控释片剂,使用药物滥用者常用的几种方法来评估基于地质聚合物的制剂的耐篡改性能。由于其抗压强度高且能耐热,因此从基于地质聚合物的制剂中提取药物需要更多的努力和时间。此外,在药物释放试验中,经过研磨后,基于地质聚合物的制剂仍保持其控释特性,而从研磨后的商业片剂中药物立即释放,可能导致剂量突释。尽管本研究中使用的篡改方法并未涵盖滥用者可获得的所有方法,但通过所述方法获得的结果表明,地质聚合物基质增加了破坏药物控制释放所需的努力程度,这表明该制剂提高了对一些常见药物滥用篡改方法的耐受力。地质聚合物基质有可能使阿片类产品对非医疗使用者的可及性和吸引力降低。

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