Preparation and characterization of insulin-loaded thiolated hyaluronic acid nanoparticles

多肽类药物口服给药的研究一直是国内外药剂学研究者热衷的领域，但这类药物由于自身理化性质等特点，口服生物利用度低。这其中研究者尤为关注的是胰岛素。胰岛素是临床上治疗Ⅰ型糖尿病的一线药物，但存在的突出问题是药物半衰期短，需长期频繁地注射给药。而胰岛素口服给药是一种患者顺应性好、服用方便的给药方式，符合内源胰岛素的分泌模式。然而，胰岛素直接口服给药时遭遇胃肠道酶降解以及膜透过性差等诸多障碍。生物黏附性聚合物纳米粒可以通过延长胃肠道药物滞留时间和减少胃肠道中消化酶对胰岛素的降解等方式，有效改善胰岛素口服生物利用度。 本研究将生物黏附性聚合物透明质酸与L-半胱氨酸通过酰胺键连接制备了巯基化透明质酸(H...The research of oral route of administration of peptide drugs has been a hotspot for pharmacy researchers at home and abroad, but because of their physical and chemical properties and other characteristics, oral bioavailability of these drugs is very low. Among these drugs, researchers are particularly concerned about the insulin. Insulin injections are clinically first-line drug for Type 1 diabet...学位：理学硕士院系专业：医学院_药理学学号：2452011115341

Risk factors of gastrointestinal bleeding with dabigatran etexilate for stroke prevention in atrial fibrillation patients and its preventive strategies

新型口服直接凝血酶抑制剂达比加群酯预防卒中疗效确切,但消化道出血风险不容小视。本文结合近5年达比加群酯用于预防心房颤动患者脑卒中时致消化道出血的临床随机试验和详细个案报道,对达比加群酯致消化道出血的可能危险因素、预防达比加群酯致消化道出血的措施等作一综述。临床医师应权衡应用达比加群酯的利弊,保证治疗的安全、有效。Dabigatran etexilate, a new direct thrombin inhibitor, has precise clinical curative effect on reducing the risk of stroke in patients with atrial fibrillation, but the risk for major gastrointestinal bleeding is significant. This paper reviewed risk factors and preventive strategies of gastrointestinal bleeding with dabigatran etexilate for stroke in atrial fibrillation patients according to randomized trials and case reports in recent five years. Clinician should balance the risk of bleeding with treatment outcome of dabigatran etexilate to ensure the effectiveness and safety of treatment

尼美舒利胶囊致体温过低1例

患者男,18岁,体重70 kg,既往体健,因“咳嗽、咽痛伴畏寒、发热4 d“为主诉于2015年1月25日就诊。既往史无特殊,无药物、食物过敏史。入院体检:T 40.2℃,P 82次/MIn,r 20次/MIn,bP 112/60 MM Hg。神志清楚,对答切题。口唇红润,伸舌居中,口腔黏膜无异常,双侧扁桃体Ⅱ度肿大,表面可见散在脓点,见白色分泌物,咽部后壁充血水肿,见淋巴滤泡,咽反射正常,余未见明显异常。血常规:WbC 14.99x109·l-1,n 76.4%,Hb 141 g·l-1,PlT 231x109·l-1;C反应

盐酸溴己新葡萄糖注射液致耳鸣耳痛1例

1病例介绍患者,女,26岁。因畏寒、发热7 d,伴咳嗽咯痰、咽痛,最高体温39.3℃,于2016年7月12日入院,行胸部CT检查,结果示\"左肺大片模糊斑片影\"。患者否认肝炎、结核、疟疾等传染病史,否认高血压、糖尿病病史,否认食物、药物过敏。入院体格检查:体温37.6℃,脉搏86次·min-1,呼吸22次·min-1,血压126/68 mm Hg(1 mm Hg

口服非甾体类抗炎药的使用分析

目的了解医院口服非甾体类抗炎药（NSAIDs）的使用情况及用药趋势,为临床合理用药提供一定的参考依据。方法对2011-2015年解放军第175医院口服NSAIDs的主要品种、销售金额、用药频度（DDDs）以及药品的销售金额和用药频度的排序比值（B/A）等情况进行统计分析。结果 5年来,该院口服NSAIDs的销售金额与用药频度逐年呈上升趋势,塞来昔布在单药销售金额排序最高;阿司匹林肠溶片在DDDs排序中居于首位;且B/A平均值最高,5年来均大于2。结论该院口服NSAIDs的用药现状及倾向基本符合我国当前药物消耗总趋势,对阿司匹林、塞来昔布、洛索洛芬钠片的选择倾向大。解放军第175医院青年苗圃基金课题（15Y008

Mechanism of nanostructured lipid carriers in promotion of absorption of poorly soluble drugs

纳米结构脂质载体(nlC)是药剂学备受关注的研究领域,作为一种性能优良的新型药物传递系统,能促进难溶性药物的口服吸收。探讨并总结纳米结构脂质载体促进难溶性药物口服吸收的机制。Objective Nano-structured lipid carriers(NLC) is a concerned research area in pharmaceutics,which as a novel drug delivery system to promote oral absorption of poorly soluble drugs.The literatures were reviewed to explore and summarize the mechanism that nano-structured lipid carriers in promotion of the absorption of poorly soluble drugs

放疗与化疗所致口腔黏膜损伤防治药物研究进展

综述近年来防治放化疗所致口腔黏膜损伤的药物,拟为开发新制剂提供参考。通过检索国内外相关文献,从作用机制角度对防治药物进行归纳和总结。发现已有较多化学药物与传统中药复方应用于防治口腔黏膜损伤。因此,开发有效的防治放化疗所致口腔黏膜损伤制剂的相关研究需要进一步地深入

Progress on solid self-microemulsifying drug delivery system for oral administration

目的对新近发展的固体自微乳化给药系统(S-SMEddS)文献进行综述。方法查阅近年国内外相关文献并进行归纳和总结。结果对固体自微乳的载体、固化技术以及缓控释制剂进行了探讨,为研究水难溶性药物的生物利用度及适合药物释放特性的S-SMEddS技术提供相关参考。结论固体自微乳化系统可以显著提高难溶性药物的口服生物利用度,且兼顾了液态自微乳和固体制剂二者的优势,是一个极具潜力的新型制剂。Objective To review the newly developed solid self-microemulsifying drug delivery system(S-SMEDDS).Methods Relevant literatures at home and abroad in recent years were consulted and summarized.Results Solid self-microemulsions carrier,solidification technology and controlled release formulations were discussed,in order to provide relevant references for improving the bioavailability of water-insoluble drugs and the SMEDDS technology for drug release characteristics.Conclusion The utilization of the solid self-emulsifying drug delivery system could significantly enhance the oral bioavailability of water-insoluble drugs.As a new formulation,S-SMEDDS presented huge potential

Preparation and evaluation of insulin thiolated hyaluronic acid nanoparticles in vitro

目的制备胰岛素巯基化透明质酸纳米粒(InSulIn THIOlATEd HyAlurOnIC ACId nAnOPArTIClES,InS-HA-CyS-nPS),考察纳米粒的理化性质。方法以合成的具有生物黏附性质的巯基化透明质酸作为载体,采用超声乳化法制备纳米粒,考察其外观、粒径、zETA电位、包封率、载药量,并进行其冻干制剂的冻干保护剂筛选。结果制备的InS-HA-CyS-nPS粒径均一,外观圆整;平均粒径为(178.5±0.8)nM,PdI为(0.214±0.013),zETA电位为-(38.47±0.46)MV,超滤离心法测定载药纳米粒的包封率为(48.85±0.66)%,载药量为(4.79±0.13)%;选择10%的甘露醇为冻干保护剂,复溶后得到具有蓝色乳光的粒径均一的纳米粒混悬液。结论巯基化透明质酸纳米粒是蛋白多肽类药物口服给药的潜在载体,为下一步研究胰岛素纳米粒在大鼠体内药效、药动学研究提供前提和基础。Objective To prepare insulin thiolated hyaluronic acid nanoparticles( Ins-HA-Cys-NPs) and study its physicochemical properties.Methods The Ins-HA-Cys-NPs was prepared by ultrasonic emulsifying method,and the properties of nanoparticles including morphology,mean diameter,Zeta potential,entrapment efficiency and drug loading efficiency were studied,as well as the cryoprotectant selection.Results The prepared nanoparticles was round in appearance and the mean diameter was( 178.5 ± 0.8) nm,the polydispersity index was( 0.214 ± 0.013) and the Zeta potential was-( 38.47 ± 0.46) mV,while the entrapment efficiency was( 48.85 ± 0.66) %,drug loading efficiency was( 4.79 ± 0.13) %; 10%mannitol as cryoprotectant provided uniform and well dispersed suspension of nanoparticles with blue opalescence after redispersion.Conclusion The thiolated hyaluronic acid nanoparticles may be used as the carrier for oral drug delivery system of insulin,and it provides a basis for studies on rats in vivo.福建省自然科学基金(2012J05159