中药复方研发与专利保护协调发展之积极影响分析

中药复方研发成果与日俱增,而成果的专利保护状况却不容乐观.中药复方专利保护与中药新药研发、产业发展、中药国际化等诸多领域息息相关,促成中药复方研发与专利保护的协调发展对于国内乃至国际社会影响深远.     

盐酸头孢吡肟中N-甲基吡咯烷的离子色谱-电导检测法测定

建立了直接进样离子色谱电导检测法测定盐酸头孢吡肟中的N-甲基吡咯烷.选用高容量阳离子交换柱,进样量25 μl,流动相为9 mmol/L硝酸(含15%乙腈),流速0.9 ml/min,35 min内洗脱所有成分.N-甲基吡咯烷在0.9～25μg/ml浓度范围内线性关系良好(r=0.999 7),检出限为0.095μg/ml,回收率为95.3%.     

脂质体肺部给药的研究

由于脂质体肺部给药具有刺激性小、吸收迅速、生物利用度高、安全性好、可实现持续缓慢释药等独特优势而成为近年来制剂领域的研究热点之一。本文论述脂质体肺部给药的特点、稳定性以及在药代动力学、药效学和安全性等方面的最新研究进展。     

不同产地金银花挥发油GC-MS的比较分析

金银花为忍冬科植物忍冬 Lonicera japonicaThunb.的干燥花蕾 ,具有清热解毒、凉散风热的功效。金银花分布广泛 ,山东和河南是我国传统的道地产区 ,而产地不同 ,其有效成分含量存在着较大差异 [1,2 ] 。有关挥发油的成分研究曾有报道[3～ 5] ,为全面了解其挥发油成分的差异及变化 ,提高金银花的质量 ,我们采用 GC- MS首次对山东、河南及江苏等地金银花的挥发油成分做了比较分析。1　实验部分1 .1　样品及挥发油的提取 :样品分别采自山东平邑、日照 ,河南封丘、新密 ,江苏南京等地 ,经鉴定为L.japonica Thunb.。称取新鲜的花蕾 1 0 0 g,…     

固精丹对急性肾功能衰竭模型的保护作用

目的:研究中药复方固精丹对庆大霉素致大鼠急性肾功能衰竭的保护作用。方法:将大鼠随机分成空白组、模型组、固精丹高、中、低(4、2、1g/kg)剂量组和阳性对照组(肾康宁2g/kg)。除空白组外,其余各组均腹腔注射庆大霉素(100mg/kg-1.d-1),连续7天;于注射庆大霉素的第2天,除空白组和模型组其余各组分别灌胃固精丹和肾康宁,连续灌胃7天,在末次给药后4h,接24h尿测尿蛋白和N-乙酰-β氨基葡萄糖苷酶(NAG);眶静脉采血测血肌酐(SCR)、尿素氮(BUN);取肾脏作光镜和电镜检查。结果:固精丹治疗组大鼠的尿糖、NAG及肌酐、尿素氮、明显低于模型组;肾脏病理:光镜和电镜检查结果,固精丹高剂量和中剂量组明显好于模型组和阳性对照组。结论:固精丹对庆大霉素引起的急性肾功能衰竭具有保护作用。     

活血熄风方对MCAO局灶性脑缺血模型大鼠脑皮质ICAM-1蛋白表达的影响

目的：观察活血熄风方对局灶性脑缺血大鼠的神经保护作用,并进一步探讨其作用机制。方法：采用线栓法阻断大鼠一侧大脑中动脉（MCAO）,制备局灶性脑缺血模型,观察活血熄风方对MCAO模型大鼠脑缺血后相关蛋白ICAM-1表达的影响,以此探讨活血熄风方对脑缺血的神经保护作用机制。结果：活血熄风方能抑制MCAO模型大鼠大脑皮质ICAM-1蛋白表达。结论：活血熄风方对大鼠局灶性脑缺血具有保护作用,其机理可能与活血熄风方影响抑制炎症反应相关蛋白ICAM-1的表达有关。     

幽门螺杆菌尿素酶B亚单位Th表位的免疫学特性研究

采用MHC限制性分析、ELISA方法、淋巴细胞增殖实验等方法研究幽门螺杆菌(Hp)尿素酶B亚单位(UreB)的H- 2~d限制性Th表位U_(546-561)、U_(229-244)、U_(237-251)的免疫学特性。发现抗I-E~d抗体能够抑制U_(546-561)对CD4~+T淋巴细胞的刺激,抗I-A~d抗体能够抑制U_(229-244)、U_(237-251)对CD4~+T淋巴细胞的刺激作用。U_(229-244)、U_(229-244)能刺激CD4~+T淋巴细胞分泌IL-4和IL-10,U_(237-251)刺激CD4~+T淋巴细胞分泌IFN-γ、IL-2,且U_(546-561)、U_(229-244)、U_(237-251)三个表位肽免疫BALB/c小鼠能够引起针对各自免疫多肽和rUreB的CD4~+T细胞应答。结果表明U_(546-561)为I-E~d限制性Th2表位,U_(229-244)为I-A~d限制性Th2表位、U_(237-251)为I-A~d限制性Th1表位。三个表位之间具有协同刺激效应,可以用于Hp表位疫苗的研究。     

Qiangli Wuhu mixture alleviates LPS-induced pneumonia by inhibiting the TLR4/NF-κB/NLRP3 pathway: a study based on network pharmacology

ContextQiangli Wuhu (QLWH) mixture is a concoction approved and registered by Ningxia Medical Products Administration. It has therapeutic effects on various types of pneumonia.ObjectiveTo clarify the mechanisms of QLWH in treating pneumonia.Materials and methodsThe potential targets of QLWH in the treatment of pneumonia were predicted by network pharmacology. Male, Institute of Cancer Research (ICR) mice were randomly divided into five groups of 12 mice, control, vehicle, QLWH (10 and 20 mg/kg) and dexamethasone (DXM), and orally treated twice daily with normal saline, QLWH or DXM. The pneumonia model was established by tracheal instillation of lipopolysaccharide (LPS). After treatment five days, ELISA, H&E staining and Western blot were used to investigate protective effects of QLWH.ResultsNine hundred and ninety-four active ingredients were found through network pharmacology, corresponding to 135 targets for the treatment of pneumonia; compared to the vehicle group, QLWH (10 and 20 mg/kg) significantly decreased the levels of TNF-α (14.3% and 28.8%), IL-1β (23.9% and 42.8%) and IL-6 (13.2% and 16.1%), increased the levels of IL-10 (134.3% and 172.9%); in terms of mechanism, QLWH down-regulated TLR4/NF-κB/NLRP3 axis related proteins in lung tissue of pneumonia model mice (p < 0.05).Discussion and conclusionsThis study combined network pharmacology and animal experiments, providing effective evidence for the clinical promotion of QLWH. Meanwhile, it is of significance for further development.     

Triple Therapy-Based on Tegoprazan,a New Potassium-Competitive Acid Blocker,for First-Line Treatment of Helicobacter pylori Infection: A Randomized,Double-Blind,Phase III,Clinical Trial

Background/AimsWe examined the efficacy and safety of tegoprazan as a part of first-line triple therapy for Helicobacter pylori eradication.MethodsA randomized, double-blind, controlled, multicenter study was performed to evaluate whether tegoprazan (50 mg)-based triple therapy (TPZ) was noninferior to lansoprazole (30 mg)-based triple therapy (LPZ) (with amoxicillin 1 g and clarithromycin 500 mg; all administered twice daily for 7 days) for treating H. pylori. The primary endpoint was the H. pylori eradication rate. Subgroup analyses were performed according to the cytochrome P450 (CYP) 2C19 genotype, the minimum inhibitory concentration (MIC) of amoxicillin and clarithromycin, and underlying gastric diseases.ResultsIn total, 350 H. pylori-positive patients were randomly allocated to the TPZ or LPZ group. The H. pylori eradication rates in the TPZ and LPZ groups were 62.86% (110/175) and 60.57% (106/175) in an intention-to-treat analysis and 69.33% (104/150) and 67.33% (101/150) in a per-protocol analysis (non-inferiority test, p=0.009 and p=0.013), respectively. Subgroup analyses according to MICs or CYP2C19 did not show remarkable differences in eradication rate. Both first-line triple therapies were well-tolerated with no notable differences.ConclusionsTPZ is as effective as proton pump inhibitor-based triple therapy and is as safe as first-line H. pylori eradication therapy but does not overcome the clarithromycin resistance of H. pylori in Korea (ClinicalTrials.gov identifier {"type":"clinical-trial","attrs":{"text":"NCT03317223","term_id":"NCT03317223"}}NCT03317223).