FK506滴眼液的高效液相色谱分析及稳定性研究

目的　建立FK5 0 6滴眼液含量检测方法并考察其稳定性。方法　采用反相HPLC测定FK5 0 6含量 ;恒温加速法考察制剂对热及强光的稳定性。结果　线性范围为 6 5 5～ 13 1μg/mL ,平均回收率为 99 88% (RSD 2 88% )。FK5 0 6滴眼液对热和光的稳定性较差 ,预测 2 5℃贮存有效期 70d。结论　反相HPLC分析方法精密、可行。FK5 0 6滴眼液需低温和避光保存。     

Mechanisms of the Bushen Huoxue formula in the treatment of osteoarthritis based on network pharmacology-molecular targets

Background:Osteoarthritis is a common degenerative disease with a high incidence, high disability rate, and poor prognosis. Clinical studies have shown that Bushen Huoxue formula can relieve joint swelling and pain and improve limb function and joint mobility, but there is a lack of high-quality scientific basis. Using network pharmacology and molecular docking technology to study the mechanism of Bushen Huoxue formula in the treatment of osteoarthritis.Methods:First, the active ingredients and corresponding target predictions of the formula were obtained through the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform and the China National Knowledge Infrastructure. Meanwhile, the osteoarthritis disease targets were obtained through the genome annotation database platform (GeneCards) and the DrugBank database, and the target proteins obtained above were standardized using the Uniprot (https://www.uniprot.org) database standardization of names. Then, the Venn diagram was created by taking the intersection of the active ingredient and the target of the disease, and the “active ingredient-target” network was constructed and analyzed using Cytoscape 3.7.2 software. At the same time, the intersecting targets were imported into the Search Tool for the Retrieval of Interaction Gene/Proteins database to build a protein-protein interaction network and to screen the core targets; the intersecting targets were visualized by using the Database for Annotation, Visualization and Integrated Discovery 6.8 database for gene ontology functional analysis and the Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment analysis, and construct the “active ingredient-target-pathway” network. Finally, the main active ingredients of the formula for tonifying the kidney and invigorating the blood were validated by molecular docking with the core targets.Results:A total of 194 active ingredients and 365 targets of the Bushen Huoxue formula were collected, 776 targets for osteoarthritis diseases and 96 targets for the intersection of active ingredients and diseases. The Kyoto Encyclopedia of Genes and Genomes enrichment analysis yielded 104 relevant pathways, including tumor necrosis factor signaling pathways, cancer signaling pathways, nucleotide-binding oligomerization domain-like receptor signaling pathways, Toll-like receptors signaling pathways, and osteoclast differentiation, apoptosis, T-cell receptor signaling pathway, and other related pathways. The molecular docking results showed good binding of the main active ingredients to the core targets.Conclusion:This study shows that the treatment of osteoarthritis involves multicomponent, multitarget, and multipathway processes. The mechanism of anti-inflammatory, antioxidant, inhibition of cartilage matrix degradation, and reduction of subchondral bone destruction may be an important mechanism for the therapeutic effect.     

Cornuside Is a Potential Agent against Alzheimer’s Disease via Orchestration of Reactive Astrocytes

Cornuside is an iridoid glycoside from Cornus officinalis, with the activities of anti-inflammatory, antioxidant, anti-mitochondrial dysfunction, and neuroprotection. In the present research, a triple-transgenic mice model of AD (3 × Tg-AD) was used to explore the beneficial actions and potential mechanism of cornuside on the memory deficits. We found that cornuside prominently alleviated neuronal injuries, reduced amyloid plaque pathology, inhibited Tau phosphorylation, and repaired synaptic damage. Additionally, cornuside lowered the release of interleukin-1β (IL-1β), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), and nitric oxide (NO), lowered the level of malondialdehyde (MDA), and increased the activity of superoxide dismutase (SOD) and the level of glutathione peroxidase (GSH-Px). Cornuside also significantly reduced the activation of astrocytes and modulated A1/A2 phenotypes by the AKT/Nrf2/NF-κB signaling pathway. We further confirmed that LY294002 and Nrf2 silencing could block the cornuside-mediated phenotypic switch of C6 cells induced by microglia conditioned medium (MCM) in response to lipopolysaccharide (LPS), which indicated that the effects of cornuside in astrocyte activation are dependent on AKT/Nrf2/NF-κB signaling. In conclusion, cornuside may regulate the phenotypic conversion of astrocytes, inhibit neuroinflammation and oxidative stress, improve synaptic plasticity, and alleviate cognitive impairment in mice through the AKT/Nrf2/NF-κB axis. Our present work provides an experimental foundation for further research and development of cornuside as a candidate drug for AD management.     

眶壁骨折整复联合泪囊鼻腔吻合术

在眶壁骨折整复术的同时行一期泪囊鼻腔吻合术。术中先整复眶壁骨折再开骨窗，行常规泪囊鼻腔吻合。结果平均观察９．５个月，泪道通畅，复视消失，眼球内陷矫正。结论联合手术，既整复了骨折，又治疗了泪道阻塞，免除了再次手术。术中视野开阔，操作方便。     

Comparison of Central Corneal Thickness using Ultrasound Pachymetry during Corneal Collagen Cross-linking

 PURPOSE:To study variation in central corneal thickness (CCT) during corneal collagen cross-linking(CXL) using ultrasound pachymetry． METHODS:Twenty patients (26 eyes) with progressing keratoconus undergoing riboflavin-UVA-induced CXL were involved in this study. Intraoperative CCT measurement using ultrasonic pachymetry was performed during the procedure．Measurements were obtained before operation, after epithelial removal, after riboflavin drop instillation, and after UVA irradiation. RESULTS:Mean CCT was 495±56 and 450±52 μm before and after epithelial removal, respectively. Mean CCT was 443±42 and 411±39 μm after riboflavin drop instillation and after UVA irradiation, respectively. Statistically significant decreases in CCT occurred between the preoperative period and after epithelial removal, after riboflavin drop instillation and after UVA irradiation. Twenty-six eyes from 20 patients undergoing CXL were divided into 2 groups (I with CCT &;gt;or = 400 μm after UVA irradiation and II with CCT &;lt;400 μm after UVA irradiation). No statistically significant difference was noted between I and II in preoperative endothelial cell count, but a statistically greater postoperative endothelial cell count was noted in I compared to II. A statistically significant difference was evident between preoperative and postoperative endothelial cell counts in Group II (P &;lt;0.05). CONCLUSION:Performing CXL with the use of riboflavin and UVA irradiation resulted in a statistically significant decrease in CCT, to a level where the corneal endothelium may be damaged.     

疏血通注射液治疗缺血性脑卒中78例

目的 评价疏血通注射液治疗缺血性脑卒中的疗效。方法 将137例缺血性脑卒中患者分为两组，治疗组78例，对照组59例，均予阿司匹林、银杏叶注射液及基础治疗，治疗组加用疏血通8mL静脉滴注，1次／d，分别于治疗前及治疗后第7，14，21天时对患者进行欧洲卒中量表（ESS）评分、日常生活活动能力评定量表（ADL）及常规检查。结果 治疗后第14，21天时，两组ESS及ADL评分有显著差异（P〈0．05）。结论 疏血通能明显改善缺血性脑卒中的预后，且不增加缺血性卒中后出血的风险。     

Schiff碱型r-氨基丁酸酯类衍生物的合成及其抗惊厥活性

作者设计并合成了9个Schiff碱型取代对羟基本甲醛缩r-氨基丁酸酯类化合物。并用美国NIH提出的“抗癫痫药物开发程序(ADD)对所合成的化合物进行抗惊厥活性筛选。结果表明化合物Ⅲf、Ⅲg、Ⅲh、Ⅲi具有不同程度的抗惊厥活性。     

HPLC测定利福平胶囊含量

应用ＨＰＬＣ法，采用ＬｉｃｈｒｏｓｐｈｅｒＲＰ－８柱，０．０７５ｍｏｌ／ＬＫＨ２ＰＯ４－乙腈－甲醇（１：１：１）为流动相，２５４ｎｍ检测，建立了测定利福平胶囊含量的方法，在４～１２０ｍｇ／Ｌ范围内，峰面积比与浓度呈良好的线性关系，ｒ＝０．９９９８，样品加样回收率为１００．１％，ＲＳＤ为０．７７％，方法较美国药典ＨＰＬＣ法简便，快速，较中国药典方法灵敏，重现性好。     

HPLC法测定乳膏剂中的酮康唑含量

目的：建立高效液相色谱方法测定酮康唑乳膏中酮康唑的含量。方法：采用LC-10ATSPD10A色谱系统。色谱条件：采用Thermo C18（5μm，150×4．6mm）色谱柱；流动相为0．34％四丁基硫酸氢铵溶液-乙腈（75：25）；流速0.9ml／min；检测波长223nm。结果；在建立的色谱条件下，酮康唑进样浓度在18μg／mL～72μg／mL范围内与峰面积呈良好的线性，相关系数为0．9999，平均回收率为100．3％（n=9）。结论：本法测定乳膏剂中的酮康唑含量快速、简捷、准确度高，不受辅料干扰。     

降压治疗对老年高血压及合并脑梗死患者心率变异性的影响

目的研究不同程度降压对老年高血压及合并腔隙性脑梗死患者心率变异性的影响,探讨高血压不同病理状态下HRV变化的差异。方法选择老年原发性高血压(高血压组)及合并腔隙性脑梗死(腔梗组)患者各33例为观察对象;同期健康老年人自愿者(健康对照组)27例,测定降压治疗前后不同血压水平下心率变异性参数的变化。结果降压治疗前高血压并脑梗组和高血压组心率变异性的各时域指标均较正常组明显减小,其中高血压并脑梗组较高血压组减小更明显,但2组比较仅SDNNI和RMSSD差异有统计学意义(P<0.05)。降压治疗后无论高血压组或高血压并脑梗组各时域指标均有不同程度的增高,第2次降压较第1次降压后各组各时域指标增高更明显。第1次降压后和降压前比较,各时域指标仅高血压组SDANNI和PNN50差异有统计学意义(P<0.05);第2次降压后和降压前比较,高血压组SDNN、SDANNI和PNN50差异有统计学意义(P<0.05),高血压并脑梗组SDNN和PNN50亦有显著差异;第2次降压后与第1次降压后比较,仅SDNN有显著差异(P<0.05)。结论高血压及合并腔隙性脑梗死患者心率变异性均有不同程度降低,合理降压治疗可部分提高不同病理阶段高血压患者心率变异性,改善自主神经功能。