暗黑鳃金龟性信息素增效缓释凝胶剂的研制

发布时间：2018-04-16 03:10

本文选题：暗黑鳃金龟甲性信息素 + 乙酸顺式-3-己烯酯　；参考：《青岛科技大学》2017年硕士论文

【摘要】：本课题以暗黑鳃金龟性信息素L-异亮氨酸甲酯盐酸盐和芳樟醇,及对其有增效作用的植物源挥发物乙酸顺式-3-己烯酯和乙酸反式-2-己烯酯为目标药物,进行气体增效缓释凝胶剂的制备和工艺优化,并制定了四种增效缓释凝胶剂的质量标准体系草案,具体分为五部分。第一部考察了暗黑鳃金龟性信息素的吸湿性和挥发性,确定其有较强的吸湿性和挥发性,具有制备气体缓释凝胶剂的可行性。并以暗黑鳃金龟性信息素主药复合成分1为代表确定了所用凝胶基质为羧甲基纤维素钠、溶剂为无水乙醇,并确定了其比例范围和药物比例范围。第二部分为暗黑鳃金龟性信息素增效缓释凝胶剂的处方和工艺优化,以药物残余量为指标,采用正交实验法筛选出最优处方,结果表明四种暗黑鳃金龟性信息素增效缓释凝胶剂30d内缓释效果良好。采用红外色谱法对所制备的缓释凝胶剂进行结构表征,表明所用辅料不影响药物的化学结构。第三部分将四种暗黑鳃金龟性信息素增效缓释凝胶剂在自然环境中的释放数据与6种释药模型(零级、一级、Higuchi、Ritger-Peppas、Baker-Lonsdale和Hixon-Crowell模型)相拟合,表明四种暗黑鳃金龟性信息素增效缓释凝胶剂中活性成分的释放分别符合Baker-Lonsdale、Hixon-Crowell、Hixon-Crowell和一级模型,释药机制以扩散为主,溶蚀为辅。第四部分建立了暗黑鳃金龟性信息素增效缓释凝胶剂的质量标准检测体系,参照《中国药典》2015版制剂质量标准的内容,对四种增效缓释凝胶剂的性状、鉴别、酸碱度、粘度、粒度等项目进行了考察,采用紫外分光光度法和气相色谱法对活性成分进行含量分析方法的建立,方法学考察结果表明,两种方法操作简单准确,精密度、稳定性和回收率均良好,紫外分光光度法适用于工业化生产,气相色谱法适用于精密分析。第五部分对所制备暗黑鳃金龟性信息素增效缓释凝胶剂进行了稳定性研究,结果表明,四种增效缓释凝胶剂的影响因素、加速和长期试验中,四种增效缓释凝胶剂的外观形状、pH值、含量等指标均无显著变化,低温条件下保存9个月性质稳定。综上所述,本课题成功研制的四种暗黑鳃金龟性信息素增效缓释凝胶剂,外观均匀细腻,性质稳定,pH值、粒度等均符合药典要求,分析方法简便准确,适用于工业化生产。
[Abstract]:In this study, the target drugs were methyl L-isoleucine methyl ester hydrochloride and linalool, and their synergistic plant volatiles, cis-3-hexene acetate and trans--2-hexene acetate.The preparation and process optimization of gas synergistic sustained-release gel were carried out, and the draft quality standard system of four synergistic slow-release gels was formulated, which is divided into five parts.In the first part, the hygroscopicity and volatility of the sex pheromone were investigated. It was confirmed that the pheromone had strong hygroscopicity and volatility, and it was feasible to prepare the gas sustained-release gel.The gel matrix is sodium carboxymethyl cellulose and the solvent is anhydrous ethanol.The second part is about the formulation and process optimization of the synergistic slow-release gel with the pheromone. The best prescription was screened by orthogonal experiment with the drug residue as the index.The results showed that the slow release effect of four kinds of sex pheromones was good within 30 days.The structure of the prepared sustained-release gel was characterized by IR chromatography, which showed that the chemical structure of the drug was not affected by the excipients.In the third part, the release data of four kinds of black-branched tortoise sex pheromone synergistic slow-release gel in natural environment were fitted to six drug release models (zero stage, Ritger-Peppaspas-Baker-Lonsdale and Hixon-Crowell model).The results showed that the release of active components from the four kinds of pheromones were in accordance with the Baker-Lonsdalesier Hixon-Crowellerian Hixon-Crowell model and the first-order model. The drug release mechanism was mainly diffusion and the dissolution was secondary.In the fourth part, the quality standard system of the synergistic slow-release gel was established. According to the content of the quality standard of the 2015 edition of Chinese Pharmacopoeia, the properties, identification, acidity, alkalinity and viscosity of the four synergistic slow-release gels were studied.The content of active components was analyzed by UV spectrophotometry and gas chromatography. The results showed that the two methods were simple, accurate and accurate.The stability and recovery are good. Ultraviolet spectrophotometry is suitable for industrial production and gas chromatography is suitable for precision analysis.In the fifth part, the stability of the four synergistic slow-release gels was studied. The results showed that the factors affecting the four synergistic slow-release gels were accelerated and long-term tests were carried out.The appearance shape, pH value and content of the four synergistic slow-release gels did not change significantly, but the properties of the four kinds of synergistic slow-release gels were stable at low temperature for 9 months.To sum up, four kinds of synergistic slow-release gel with pheromone were successfully developed in this paper. They are uniform in appearance, stable in pH value and particle size. The analytical method is simple and accurate and suitable for industrial production.
【学位授予单位】：青岛科技大学
【学位级别】：硕士
【学位授予年份】：2017
【分类号】：TQ453

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