【作者】 庞纪平；

【导师】 高文远；

【作者基本信息】 天津大学 ， 应用化学， 2008， 博士

【摘要】 元胡止痛方是临床常用有效方剂,该方由延胡索和白芷两味中药组成,具有理气、活血、止痛的功效,用于气滞血瘀的胃痛、胁痛、头痛和月经疼痛。将元胡止痛方由普通片剂改为控释片,可以达到快速止痛,长期镇痛的效果。元胡止痛控释片研究主要从以下四个方面进行:采用正交设计,考察延胡索和白芷的提取参数,确定延胡索和白芷的最佳提取工艺,提取、精制元胡止痛片的有效部位群。采用双层片制剂工艺,将元胡止痛控释片设计为速释片层和控释片层两部分。通过实验确定各部分药物与骨架材料的最佳配比。以延胡索乙素和欧前胡素为考察指标,采用HPLC法对元胡止痛控释片的主要有效成分进行了含量测定,提高了质量标准。考察元胡止痛控释片的体外溶出度,探讨释药模式。凝胶剂是近年来出现的新剂型,制法简便,使用方便。儿童口服型凝胶剂是针对儿童服药难的问题研发的一种中药创新剂型。清热凝胶处方源于我国名老中医验方,具有疏风清热、养阴活血、利咽止痛之功效,用于治疗小儿发热、咽喉肿痛等症。清热凝胶的研发包括六方面内容:以卡拉胶和魔芋粉为主要基质材料,采用正交设计和实验,确定凝胶成型的最佳处方配比。在文献调研和参考生产实际的基础上,对金银花、连翘、薄荷、丹皮等以挥发油为主要有效成分的四味药材采用水蒸气蒸馏法提取挥发油;对赤芍、板蓝根、地黄、白茅根等以皂苷、黄酮、萜类为主要有效成分的八味中药,采用正交设计和实验,确定水提醇沉的最佳工艺;对大黄、川贝母、玄参等以蒽醌、生物碱为主要有效成分的四味中药,采用正交设计和实验,确定乙醇提取的最佳工艺。按照基质成型和药材提取确定的工艺参数,进行中试生产,验证工艺路线的合理性和可行性。采用TLC法对赤芍、金银花、板蓝根、玄参等药材进行定性鉴别。采用HPLC法,对药品中大黄素和大黄酚进行含量测定,制定定量限度。从抗炎、解热、镇痛等三方面着手,进行体外和体内实验,揭示其治疗机理。进行急性毒性和长期毒性试验,评价其安全性。更多还原

【Abstract】 Yuanhuzhitong tablet is an effective prescription commonly used in clinic. It is made up with Rhizaoma Corydalis and Radix Angelica Dahuricae and has the effect of regulating qi, promoting blood circulation and relieving pain, the prescription is usually used in stomachalgia, hypohondriac pain, headache and menstruation pain due to qi stagnation and blood stasis. In this dissertation, we try to reform it to be controlled-release preparation, which can promptly and permanently take analgesia effect. The R&D of Yuanhuzhitong controlled-release tablet(CRT)is performed as follows. Firstly, we confirm the optimizing extract process of Rhizaoma Corydalis and Radix Angelica Dahuricae by applying orthogonal design and test, in order to extract and purify the effective constituent groups of Yuanhuzhitong tablet. Secondly, we design the Yuanhuzhitong CRT as double layers tablets by applying double layers tablet manufacture procedure, one is the quickly releasing lamella, the other is sustained releasing lamella. Thirdly, we confirm the optimizing ratio of active constituents and excipients in the different lamella. Fourthly, taking tetrahydropalmatine and imperatorin as index, we establish the content examination by HPLC, enhance the quality standard. Fifthly, we conduct dissolution test of Yuanhuzhitong CRT to discuss the drug releasing model.Gel is a new preparation emerging in recent years, which can easily be manufactured and used. The child gel is a new Chinese medicine preparation, which can resolve the children’s difficulty when taking medicine. Qingre gel is a prescription derived from an old proved recipe, which has the effect of dispelling wind and clearing away heat, nourishing yin and activate blood, and smoothing throat and reliving pain. And this preparation can treat child fever, sore throat, and so on. The R&D of Qingre gel includes in six aspects as below. The first, taking carrageenin and konjaku flour as main fundamental material, we confirm the optimizing ratio by applying orthogonal design and test. The second, as to Flos Lonicerae Japonicae, Fructus Forsythiae, Herba Menthae, which active constituent is essential oil, we use steam distillation to extract the essential oil; as to Radix Paeoniae Rubra, Radix Isatidis, Radix Rehmanniae, Rhizoma Imperatae, which active constituent is saponins, flavone, terpene, we confirm the optimizing process of water extract and alcohol sediment by applying orthogonal design and test; as to Radix et Rhizoma Rhei , Bulbus Fritillariae Cirrhosae, Radix scrophulariae, which active constituent is anthraquinones , alkaloid, we confirm the optimizing process of alcohol extract by applying orthogonal design and test. The third, according to the result of above tests, we try to manufacture the Qingre gel, in order to verify the rationality and feasibility of process. The fourth, establishing the qualitative analysis method of Flos Lonicerae, Radix scrophulariae, Radix Paeoniae Rubra, Radix Isatidis by TLC, and establishing quantitative analysis method to examine the content of emodin and chrysophanol by HPLC. The fifth, conducting experiments in vivo and in vitro to illustrate the therapeutical mechanism from the different aspects, such as antiflammatiom, antipyretic analgesic, antivirus, antisepsis. The sixth, conducting the acute toxicity and chronical toxicity to evaluate the safety of the Qingre gel.更多还原