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泊洛沙姆407盐酸利多卡因凝胶的流变学特性

Rheological characterization of Poloxamer 407 lidocaine hydrochloride gels.

作者信息

Ricci E J, Bentley M V L B, Farah M, Bretas R E S, Marchetti J M

机构信息

Laboratory of Pharmaceutical Technology, Department of Pharmaceutical Sciences, School of Pharmaceutical Sciences of Ribeirão Preto, University of São Paulo, Av. do Café s/n, 14040-903 Ribeirão Preto, SP, Brazil.

出版信息

Eur J Pharm Sci. 2002 Nov;17(3):161-7. doi: 10.1016/s0928-0987(02)00166-5.


DOI:10.1016/s0928-0987(02)00166-5
PMID:12393144
Abstract

Thermal gelation of Poloxamer 407 lidocaine hydrochloride gels was characterized by rheological studies. Lidocaine, a local anesthetic used for treatment of acute and chronic pain, presents short duration action; thus a long-action single-dose injection would be of clinical importance. Poloxamer 407 gel can extend the release and the action of lidocaine. In the present work, aqueous gels with lidocaine containing different concentrations of Poloxamer 407 and additives like inorganic salts (NaCl, NaH(2)PO(4), Na(2)CO(3)) and PEG 400 were obtained. Viscosity measurements and the optimal sol-gel transition temperature were obtained by these rheological studies. Poloxamer 407 gels are viscoelastic materials because they have elastic modulus (G'), characteristic of solid materials, and viscous modulus (G"), characteristic of liquid materials. Poloxamer 407 gels are pseudoplastic; therefore, when shear deformed, their viscosity decreases. Increase of the polymer concentration increases the viscosity of the gels, which can change the releasing process of lidocaine from the gel. The sol-gel transition temperature was decreased by increasing the polymer concentration and by the presence of additives. The rheological behaviour of Poloxamer gels characterized in this work can be useful for understanding further studies of drug release.

摘要

泊洛沙姆407盐酸利多卡因凝胶的热凝胶化通过流变学研究进行表征。利多卡因是一种用于治疗急慢性疼痛的局部麻醉剂,作用持续时间短;因此,长效单剂量注射具有临床重要性。泊洛沙姆407凝胶可延长利多卡因的释放和作用时间。在本研究中,制备了含有不同浓度泊洛沙姆407以及无机盐(氯化钠、磷酸二氢钠、碳酸钠)和聚乙二醇400等添加剂的利多卡因水凝胶。通过这些流变学研究获得了粘度测量值和最佳溶胶-凝胶转变温度。泊洛沙姆407凝胶是粘弹性材料,因为它们具有固体材料特有的弹性模量(G')和液体材料特有的粘性模量(G")。泊洛沙姆407凝胶是假塑性的;因此,当受到剪切变形时,它们的粘度会降低。聚合物浓度的增加会提高凝胶的粘度,这可能会改变利多卡因从凝胶中的释放过程。通过增加聚合物浓度和添加添加剂,溶胶-凝胶转变温度会降低。本研究中表征的泊洛沙姆凝胶的流变行为有助于进一步理解药物释放研究。

相似文献

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Rheological characterization of Poloxamer 407 lidocaine hydrochloride gels.

Eur J Pharm Sci. 2002-11

[2]
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