【中文摘要】 皮肤给药分为经皮给药系统(TTS)和皮肽局部给药系统(DTS),经皮给药系统是指药物经由皮肤吸收进入人体血液循环并达到有效血药浓度、实现疾病治疗或预防的一类给药方法,而皮肤局部给药系统是指药物透过角质层到达病变部位的给药方法。止痛活血类中药在中药外用制剂中占有重要地位,主要属于DTS范畴。与化学药物贴剂提高单一成分经皮渗透速率的要求不同,对于复方中药贴剂而言,在保证良好粘附性能的基础上,能够同时提高同一类成分或者各种不同成分的释放速率是压敏胶基质对中药贴剂适应性的主要评价指标。本研究在于结合中药的传统理论将现代的经皮给药技术应用于我国的传统中药外用制剂中,对现代DTS技术在传统外用制剂的适应性展开研究,为制备质量可控,适应性强的现代中药经皮给药制剂提供技术支撑。本研究采用云南白药浸膏与延胡索、川乌、三七、赤芍等六味中药材提取物组成止痛活血浸膏,并选择浸膏中的延胡索乙素,乌头碱,芍药苷,人参皂苷Rg1等四种成分作为模型成分。以丙烯酸酯压敏胶和不同型号SIS热熔胶(KT-A,2501,2501s)为基质制备压敏胶贴剂,考察基质对贴剂粘附性及药物体外释放的影响。对多种溶剂系统进行筛选,在实验...更多室条件下采用溶剂法对各种类型压敏胶基质进行溶胶,发现正庚烷:乙酸乙酯=3:7(w/w)为较理想的组合溶剂。热熔胶的粘性测试结果表明,热塑性弹性体的加入有利于提高热熔胶的粘附性能,丙烯酸酯压敏胶为基质的贴剂粘附性能较好。采用Permcell扩散池考察四种药物在不同基质中的释放行为,实验结果显示丙烯酸酯压敏胶对生物碱类成分释放行为影响较大,KT-A型热熔胶中有效成分释放速率与分子量成较明显的负相关性,2501s型热熔胶制备的贴剂中有效成分的12h累积释放率比较均衡,在29%—43%之间。发现基质中药物有效成分的分子量越小,与基质间相互作用越弱,接收介质越容易渗入基质,有效成分释放速率越高。因此热熔胶对不同成分释放的适应性更高,而丙烯酸酯压敏胶对同一类成分的释放行为有更强的选择性。  还原

【英文摘要】 Skin delivery is divided into transdermal therapeutic systems (TTS) and dermal therapeutic systems (DTS) . TTS are non-conventional dosage forms intended to deliver a drug across the skin for systemic activity and DTS are dosage forms similar to TTS, for the topical treatment of skin diseases. Anti-pain Chinese traditional medicine plays an important role in DTS. The patches with chemical medicine require to improve the percutaneous penetration rate, and the TCM patch which is based on good adhesion is concerned in property release rate of one kind of components or different ones. The purpose of this study is to investigate the applicability of traditional Chinese medicine (TCM) in modern DTS and to provide technical support for preparing different TCM pressure sensitive adhesives which have better adaptability and controlled quality using modern DTS techniques.In this paper, Corydalis, Radix Aconiti, Sanqi, TPG as well as two other substances have been selected in Yunnan White Drug an...d tetrahydropalmatine, aconitine, paeoniflorin and ginsenoside rg1 are used as labeled components. TCM pressure sensitive adhesives have been made with acrylic ester or some different kinds of SIS-based thermosol as matrix. The effects of different matrices on the viscosity and in vitro release percentage of TCM components were investigated. We selected several solvent systems, the thermosol (KT-A, 2501, 2501s) were dissolved by stirring in the mixed solvent in experiment . The better mixed solvent system is determined as heptane: ethyl acetate = 3:7 (w: w) . Viscosity test shows that SIS as an addition can improve the viscosity of thermosol and the patch based on acrylic ester has better viscosity. The in vitro release experiments were carried out with Permcell diffusion cell. Results show that the patch based on acrylic ester takes up significant effects on alkaloid drugs, the components in KT-A matrix indicate good correlation between release rate and molecular weight. The 2501s patch presents a balanced accumulative release rate (29%-43% in 12h) . It was found that good components release rates were abserved with small molecular weight, weak interaction with the matrix and the receiving media easier penetration to the matrix. We find that thermosol have good applicability to TCM-DTS, and the Acrylic PSA shows better selection to one kind of components. 

【中文关键词】 经皮给药; 丙烯酸酯; SIS型热熔胶; 体外释放; 粘附性
【英文关键词】 Transdermal Delivery System; Acrylic Ester; SIS-based Thermosol; in vitro Release; Viscosity