【作者】 刘莉；

【导师】 代龙；

【作者基本信息】 山东中医药大学 ， 中药学， 2003， 硕士

【摘要】 目的：实验小儿易接受又有可靠疗效的治疗小儿外感发热的中药制剂，对小儿退热按摩乳的制备工艺、透皮吸收、质量标准、初步稳定性和药效学、毒理学进行了研究。方法：小儿退热按摩乳主要由黄芩、柴胡、青蒿等中药组成。根据儿科用药剂型的特点，结合药物特性及中药经皮给药和推拿的理论与方法，选择了以卡波姆为基质的外用凝胶新剂型。采用正交设计法和气相—质谱联用等技术分别优选了柴胡、青蒿、桂枝、荆芥穗的提取工艺和黄芩中黄芩苷的提取工艺。选择适宜的基质、透皮吸收促进剂，制成外用凝胶剂。以产品的成型性、细腻度、涂展性、树脂化现象和稳定性为指标考察凝胶的制备工艺。采用体外透皮实验，毛细管电泳法检测，以黄芩苷累积透皮吸收量为指标，优选氮酮的最佳加入浓度。对凝胶剂进行药物透皮吸收的研究。对方中四味药做了定性鉴别，主药黄芩以高效液相色谱法做了黄芩苷的含量测定，制定了质量标准。考察了制剂的初步稳定性。进行了药效学和毒理学的研究。结果：以超临界CO₂提取柴胡、青蒿、桂枝、荆芥穗中挥发性成分，以水煎二次酸沉法提取黄芩苷粗品兑入。选用高分子水溶性基质卡波姆为基质，二组分系统氮酮一丙二醇为透皮吸收促进剂，制成凝胶剂。优选氮酮的最佳加入浓度为2％。透皮试验研究表明制剂以近零级速率释放药物透过皮肤。药效与毒理实验表明该制剂具有明显的解热、抗炎、抗病毒作用。对家兔皮肤无毒性、无刺激性。结论：小儿退热按摩乳为理想的治疗小儿外感发热的中药凝胶剂。样品细腻、均匀、不油腻、易涂展，质量可控，稳定性好。功能发汗解表，清里退热。无毒副作用。更多还原

【Abstract】 Subject: To study an ideal preparation of Traditional Chinese Medicine for treating infatile high fever. Xiao’er Tui’re Anmo Ru is selected. Extracting Process, moulding technics and characteristics such as percutaneous absorption, qulity standards, tentative stability and Pharmacodynamics, toxicology will be studied.Methods: Xiao’er Tui^re Anmo Ru is mainly constituted by Bupleurum chinense DC. ; Scutellaria baicalensis Georgi, Artemisia annua L. ;Cinnamomum cassia Presl.and Schizonepeta tenuifolia Briq . etc. According to characteristics of infatile clinical medical treatments and theories of TCM, choosed transdemal gel as proper pharmaceutical type. Orthogonal experiments and GC/MS technics were performed to study the optimum extracting technics of Bupleurum chinense DC. and Scutellaria baicalensis Georgi etc. Though selecting, choosed suitable excipient and osmotic-promoting regents to make gel. Produced the moulding technics of Gel with different influence factors such as moulding, fining, smearing and stability. Adopted Franz diffusion cell , HPEC technics and used percutaneous contents of Baicalin from gel into skin as an index to select the best ratio of adding Azone in Gel. Studied Percutaneous Absorption of drug. Propertyidentification of four Herbs were made by TLC. Baicalin was measured by HPLC to establishe the qulity standards. Studied tentative stability. Produced Pharmacodynamics and toxicology of the gel.Results: Through the experiments, SFE was used to extract volatile oil in four herbs, water-extracting and acid-depositing were used to extract Baicalin. Carbomer was used as excipient, Azone and Propylene were used as osmotic-promoting regents to make gel. The best ratio of adding Azone in Gel is 2%. Experiments of Percutaneous Absorption in Vitro showed the permeation of drug from gel into skin conformed to zero-order kinetics.it can keep stable drug cenconcentration in blood. The qulity standards of Preparation and tentative stability were established . The studies of Pharmacodynamics and toxicology indicated that it holdes obvious febrilfuge, antiphlogistic and abirritation effects and has non-toxcicity or stimulus to skin.Conclutions: Xiao’er Tui’re Anmo Ru is an optimum percutaneous gel which is used to infatile high fever. It is fine,even, easy to smear and has suitable quality standards . It has the effect of eliminating sweat , relieving exterior syndrome and clearing away heat. It has no toxcicity or stimulus to skin.更多还原