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一项关于局部麻醉药从硅氧烷基质中的释放能力的研究。

An study of the release capacity of the local anaesthetics from siloxane matrices.

作者信息

Preda Gabriela, Rogobete Alexandru Florin, Săndesc Dorel, Bedreag Ovidiu Horea, Cradigati Carmen Alina, Sarandan Mirela, Papurica Marius, Popovici Sonia Elena, Dragomirescu Monica

机构信息

Faculty of Chemistry, Biology, Geography, West University of Timisoara, Timisoara, Romania.

Faculty of Medicine, "Victor Babes" University of Medicine and Pharmacy, Timisoara, Romania.

出版信息

Rom J Anaesth Intensive Care. 2016 Oct;23(2):123-131. doi: 10.21454/rjaic.7518/232.vit.

Abstract

AIMS

In the field of anaesthesia and intensive care, the controlled release systems capable of delivering constantly local anaesthetics are of interest because of the advantages brought to pain management. In this paper we presented the release profiles by usage of siloxane matrices of two common local anaesthetics, lidocaine and bupivacaine, analysed .

METHODS

The siloxane matrices were obtained in accordance with the methods described in the specialized literature, tetraethoxysilane (TEOS) and tetramethoxysilane (TMOS) were used as precursors. Lidocaine and bupivacaine were encapsulated in the synthesized gels. The controlled release was performed artificial systems in which temperature (30°C, 36.5°C, 40°C) and pH (6, 7, 8) have varied.

RESULTS

Following the analysis of the artificial systems similar profiles were highlighted for both local anaesthetics. Statistically significant differences were identified (p < 0.05) for systems where the release occurred at temperatures above 36.5°C. There were no statistically significant differences regarding the influence of pH, the type of the entrapped anaesthetic or the type of the precursor used in the synthesis of siloxane matrices.

CONCLUSIONS

According to this experimental study, the pH, the type of precursor or the type of anaesthetic does not statistically influence the release profile from the studied system. In conclusion, these systems are promising for obtaining pharmaceutical preparations which can be used in current clinical practice. Several studies on controlled release siloxane systems should be carried out both and in order to exclude possible toxicity and histopathological effects.

摘要

目的

在麻醉和重症监护领域,能够持续释放局部麻醉剂的控释系统因给疼痛管理带来的优势而备受关注。在本文中,我们展示了使用硅氧烷基质对两种常见局部麻醉剂利多卡因和布比卡因的释放曲线,并进行了分析。

方法

按照专业文献中描述的方法制备硅氧烷基质,使用四乙氧基硅烷(TEOS)和四甲氧基硅烷(TMOS)作为前驱体。将利多卡因和布比卡因封装在合成凝胶中。在温度(30°C、36.5°C、40°C)和pH值(6、7、8)变化的人工系统中进行控释实验。

结果

对人工系统进行分析后,两种局部麻醉剂呈现出相似的释放曲线。在温度高于36.5°C的系统中,发现了具有统计学意义的差异(p < 0.05)。在pH值的影响、所包裹麻醉剂的类型或用于合成硅氧烷基质的前驱体类型方面,未发现具有统计学意义的差异。

结论

根据本实验研究,pH值、前驱体类型或麻醉剂类型在统计学上不会影响所研究系统的释放曲线。总之,这些系统有望用于制备可应用于当前临床实践的药物制剂。为了排除可能的毒性和组织病理学影响,应在体内和体外对控释硅氧烷系统进行多项研究。

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