槐葛降糖口腔速崩片的制备工艺及初步药效学研究

发布时间：2017-12-31 00:04

  本文关键词：槐葛降糖口腔速崩片的制备工艺及初步药效学研究　出处：《陕西科技大学》2017年硕士论文　论文类型：学位论文

  更多相关文章： 槐葛降糖口腔速崩片 II型糖尿病 制备工艺 质量控制 药效学

【摘要】：本文以槐米—葛根配伍为主的治疗糖尿病的民间验方为基础(原验方为汤剂,其主要有效成分为芦丁和葛根素),结合现代药物制剂技术,将芦丁和葛根素等中药提取物组合,制备出具有降糖作用的槐葛降糖口腔速崩片,对其进行质量控制及初步药效学研究。在制备工艺的研究中,采用正交实验等方法,以粉末流动性、崩解时限、口感等为指标,分别对辅料的种类、比例、用量进行了考察,得到处方:崩解剂(45%,MCC:L-HPC为8:1)、填充剂(42%,甘露醇:乳糖为3:2)、发泡剂(2.4%,柠檬酸:NaHCO3为0.8:1)、矫味剂(0.3%,甜蜜素)、润滑剂(0.3%,硬脂酸镁)、主药(10%)。制备的槐葛降糖口腔速崩片能在25s内崩解,口感良好。采用薄层色谱法,对槐葛降糖口腔速崩片中的槐米和葛根进行定性鉴别,采用高效液相色谱法建立了槐葛降糖口腔速崩片中芦丁和葛根素的含量测定方法,并进行了方法学考察,其回收率分别为98.70%和99.13%,RSD分别为1.66%和1.37%,该方法准确可靠。根据三批次样品测定结果,确定槐葛降糖口腔速崩片中芦丁含量不少于30mg/g,葛根素含量不少于60mg/g。根据2015版《中国药典》制剂通则对制剂进行了水分、崩解时限、脆碎度、片重差异、微生物限度等检查,均符合药典要求。在室温下进行了槐葛降糖口腔速崩片的初步稳定性研究,结果显示在6个月内三批样品的各项指标均符合规定。药效学研究采用连续2d腹腔注射低剂量(75mg/kg?d)链脲佐菌素(STZ)的方法制备II型糖尿病小鼠模型,槐葛降糖口腔速崩片高(1.5g/kg?d)、中(1g/kg?d)、低(0.75g/kg?d)剂量灌胃给药保护30d。以空腹血糖、糖耐量、血清总胆固醇(TC)、甘油三酯(TG)、高密度脂蛋白胆固醇(HDL-C)、低密度脂蛋白胆固醇(LDL-C)及主要脏器中丙二醛(MDA)、蛋白羰基化(PCO)、一氧化氮(NO)、谷胱甘肽(GSH)、超氧化物歧化酶(SOD)、过氧化氢酶(CAT)含量为测定指标,验证槐葛降糖口腔速崩片的治疗效果,探索其作用机理。结果显示,中、高剂量的槐葛降糖口腔速崩片能够显著降低模型血糖(P0.01),增强糖耐量,改善小鼠体重下降的趋势,降低血清中TC、TG、LDL-C的含量(P0.05),增加血清中HDL-C含量(P0.05),增强SOD、CAT、GSH活性(P0.05),降低MDA、PCO、NO含量(P0.05),并呈一定的剂量依赖性。槐葛降糖口腔速崩片能够调节II型糖尿病小鼠的糖脂代谢,改善氧化应激,对II型糖尿病小鼠有较好的保护作用。本文提出的槐葛降糖口腔速崩片制备工艺合理可行,质量可控,抗糖尿病作用显著。
[Abstract]:Based on the treatment of diabetes - Compatibility of Radix Sophorae folkremedy based (the original prescription for the decoction, the main active ingredient of rutin and Ge Gensu), combined with modern pharmaceutical technology, rutin and Ge Gensu extract of traditional Chinese medicine combination is prepared for the hypoglycemic Huai Ge Jiangtang oral disintegrating tablet studies on the quality control and preliminary efficacy. In the study of preparation process, orthogonal experiment method, the powder fluidity, disintegration time and taste as indexes, respectively, the ratio of the excipients, dosage were investigated, and get prescription: disintegrating agent (45%, MCC:L-HPC, 8:1) the filler (42%, mannitol: 3:2 lactose), foaming agent (citric acid: NaHCO3 2.4%, 0.8:1), correctant (0.3%, cyclamate), lubricants (0.3%, magnesium stearate), the main drug (10%). Huai Ge Jiangtang preparation of orally disintegrating tablets could disintegrate, in 25s in good taste. TLC of Huai Ge Jiangtang oral disintegrating tablet in the bud and root were identified, chromatographic method to establish a method for the determination of Huai Ge Jiangtang oral disintegrating tablets in Ge Gensu and the content of rutin by high performance liquid, and the method of study, the recovery rate was 98.70% and 99.13% respectively, RSD 1.66% and 1.37%, the method is accurate and reliable. According to the determination results of three batches of samples, determine the Huai Ge Jiangtang oral disintegrating tablets of not less than 30mg/g the content of rutin, Puerarin Content of not less than 60mg/g. according to the 2015 edition of < > of China Pharmacopoeia rules of preparations for the preparation of water, friability, disintegration time and tablet weight difference. Microbiological examination, the results met the Pharmacopoeia requirements. Preliminary study on stability at room temperature of Huai Ge Jiangtang oral disintegrating tablet. The results showed that in 6 months the indicators of the three samples were in accordance with the provisions. The study of pharmacodynamics even 缁，

本文编号：1357147