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首页> 外文期刊>Biomolecules & therapeutics >Enhanced Local Anesthetic Efficacy of Bioadhesive Ropivacaine Gels
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Enhanced Local Anesthetic Efficacy of Bioadhesive Ropivacaine Gels

机译：生物粘附性罗哌卡因凝胶增强的局部麻醉功效

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In relieving local pains, ropivacaine has been widely used. In case of their application such as ointments and creams, it is difficult to expect their effects for a significant period of time, because they are easily removed by wetting, movement and contacting. Therefore, the new formulations that have suitable bioadhesion were needed to enhance local anesthetic effects. The effect of drug concentration and temperature on drug release was studied from the prepared 1.5% Carboxymethyl cellulose (CMC) (150 MC) gels using synthetic cellulose membrane at 37 ? 0.5癈. As the drug concentration and temperature increased, the drug release increased. A linear relationship was observed between the logarithm of the permeability coefficient and the reciprocal temperature. The activation energy of drug permeation was 3.16 kcal/mol for a 1.5% loading dose. To increase the skin permeation of ropivacaine from CMC gel, enhancers such as saturated and unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants were incorporated into the ropivacaine-CMC gels. Among the enhancers used, polyoxyethyl-ene 2-oleyl ether showed the highest enhancing effects. For the efficacy study, the anesthetic action of the formulated ropivacaine gel containing an enhancer and vasoconstrictor was evaluated with the tail-flick analgesimeter. According to the rat tail-flick test, 1.5% drug gels containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed the best prolonged local analgesic effects. In conclusion, the enhanced local anesthetic gels containing penetration enhancer and vasoconstrictor could be developed using the bioadhesive polymer.
机译：在缓解局部疼痛中，罗哌卡因已被广泛使用。在使用它们如软膏和乳膏的情况下，很难在相当长的一段时间内预期其效果，因为它们很容易通过润湿，移动和接触而除去。因此，需要具有适当生物粘附力的新制剂来增强局部麻醉作用。使用合成纤维素膜在37°C下从制备的1.5％羧甲基纤维素（CMC）（150 MC）凝胶中研究了药物浓度和温度对药物释放的影响。 0.5癈随着药物浓度和温度升高，药物释放增加。在渗透系数的对数与倒数温度之间观察到线性关系。对于1.5％负载剂量，药物渗透的活化能为3.16kcal / mol。为了增加罗哌卡因从CMC凝胶中透入皮肤的能力，将诸如饱和和不饱和脂肪酸，吡咯烷酮，丙二醇衍生物，甘油酯和非离子表面活性剂等增强剂掺入罗哌卡因-CMC凝胶中。在使用的增强剂中，聚氧乙烯-2-油基醚显示出最高的增强效果。为了进行功效研究，使用甩尾式止痛仪评估了含有增强剂和血管收缩剂的罗哌卡因凝胶的麻醉作用。根据大鼠甩尾试验，含有聚氧乙烯2-油基醚和四氢唑啉的1.5％药物凝胶具有最佳的延长的局部镇痛作用。总之，可以使用生物粘附性聚合物开发包含渗透增强剂和血管收缩剂的增强型局部麻醉凝胶。

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