口服香叶木甙治疗老年性急性痔发作的临床研究（附82例分析）

目的研究应用口服微粒化的香叶木甙(爱脉朗Alvenor)治疗老年性急性痔发作.方法本组82例患者,年龄68～92岁,中位年龄78岁.随机分为两组,研究组应用香叶木甙42例,对照组应用安慰剂40例,疗程10天.结果在安全性方面两组均未出现全身不良反应,也未出现血液系统、肝、肾等脏器功能损害.用药10天后复查发现(1)疼痛症状消失的患者,研究组为70.2%,对照组为38.6%,两组之间有显著差别(P＜0.01).(2)水肿体征消失和明显改善的患者,研究组为96.7%,对照组为67.5%,两组之间有显著差别(P＜0.01).(3)出血症状完全消失的患者,研究组为92.5%,对照组为63.2%,两组之间有显著差别(P＜0.01).结论香叶木甙与安慰剂相比,对于老年性痔疼痛、水肿、出血等的疗效有显著差别,口服香叶木甙治疗老年性急性痔发作较安全、有效.     

香叶木甙止血作用的实验研究

香叶木甙止血作用的实验研究杨军王静陈澍禾（安徽省医学科学研究所药理研究室，合肥２３００６１）中国图书分类号Ｒ９７３．１；２８２．７１香叶木甙（Ｄｉｏｓｍｉｎ）为３′，５，７－三羟基－４′－甲氧黄酮－７－芸香糖。文献报道：本品具有维生素Ｐ样作用，能增强...     

肢体淋巴水肿诊断治疗进展

<正>肢体淋巴水肿系由于淋巴管先天性发育不全或后天的原因发生狭窄、闭塞,使四肢远端淋巴回流受阻,瘀积在皮下组织间隙内,继而发生纤维结缔组织增生、脂肪硬化、筋膜增     

香叶木素通过抑制破骨细胞分化治疗早期骨关节炎的可行性研究

目的验证香叶木素治疗早期骨关节炎(OA)的可行性。方法收集人体骨关节炎软骨下骨标本,通过ACLT法手术建立小鼠骨关节炎模型,通过组织染色检测破骨细胞数量,通过显微CT检测小鼠软骨下骨结构变化。通过CCK-8法检测香叶木素对BMMs细胞的细胞毒性;通过细胞因子诱导骨髓来源巨噬细胞(BMMs)分化成破骨细胞,建立破骨细胞分化模型,并将其分为单纯诱导组及不同浓度的香叶木素诱导组;通过TRAP染色检测香叶木素对破骨细胞分化的影响;PCR法检测破骨细胞分化标记基因(TRAP,CTSK)的表达情况。结果在人体标本中,患侧软骨下骨标本中的破骨细胞数量明显少于健侧(P<0.05)。在小鼠骨关节炎模型中,术后小鼠的胫骨平台软骨下骨TRAP染色阳性的破骨细胞数量明显多于假手术组(P<0.05),小鼠膝关节软骨下骨显微CT扫描结果显示,术后的软骨下骨呈现明显的骨质疏松表现;通过CCK-8法对BMMs的活性检测,在香叶木素浓度为20μmol/L以上的处理组细胞数量较空白对照组明显减少(P<0.05),其余浓度的处理组培养至5 d仍未见明显细胞毒性;TRAP染色结果显示,成破骨细胞分化诱导7～9 d后,香叶木素(5μmol/L)诱导组TRAP染色阳性的多核细胞数量较空白对照组明显减少(P<0.05);PCR检测显示,破骨细胞分化相关基因在香叶木素(2.5μmol/L)诱导组表达水平已经明显降低(P<0.05)。结论①小鼠模型中,早期OA的软骨下骨成骨质疏松样改变,人体晚期骨关节炎软骨下骨中的破骨细胞数量明显降低;②香叶木素可以抑制破骨细胞分化。因此,推测香叶木素有望通过抑制破骨细胞分化,降低早期骨关节炎软骨下骨丢失,进而对早期骨关节炎具有一定的治疗作用。     

香叶木素的检测方法与生物活性及其机制研究进展

目的:为香叶木素的研究与开发提供参考。方法:以"香叶木素""生物活性""Diosmetin""Bioactivity"等为关键词,组合查询2000年1月-2016年3月在PubMed、中国知网、万方、维普等数据库中的相关文献,对香叶木素的检测方法和生物活性及其机制进行综述。结果与结论:共检索到相关文献50篇,其中有效文献24篇。香叶木素可采用毛细管电泳-电化学法、化学发光法、高效液相色谱法等方法进行检测,其具有抗氧化、抗菌、抗炎、抗肿瘤及雌激素样作用。在信号通路、基因和相关蛋白酶的调控方面的研究,为香叶木素作为新型高效、低毒的抗癌辅助药物开发提供了可能。建议加强香叶木素提取工艺、体内药效学和提高生物利用度的药剂学研究,并对其用药安全性进行考察。     

香叶木苷联合华法林治疗深静脉血栓机制的网络药理学分析

目的:基于网络药理学探讨香叶木苷联合华法林治疗深静脉血栓的分子机制.方法:以Swiss Target Prediction数据库获取香叶木苷及华法林作用靶点,OMIM和GenCards数据库获取深静脉血栓形成的靶点,通过绘制韦恩图发现香叶木苷及华法林治疗深静脉血栓的潜在作用靶点,并建立靶点蛋白相互作用网络.于Metas...     

下肢淋巴水肿的整复治疗临床研究

目的采用不同的手术方法治疗肢体淋巴水肿患者17例,以研究和探索淋巴水肿的修复效果。方法用脂肪抽吸的方法治疗肢体淋巴水肿6例,采用皮瓣下软组织清除、多余皮肤组织切除法治疗4例;肢体淋巴组织增生肿块切除加自体大张皮肤回植7例。结果1例脂肪抽后效果不理想,1例淋巴水肿增生组织切除后回植皮肤愈合欠佳,其余15例效果满意。结论淋巴水肿Ⅱ期选用脂肪抽吸;Ⅲ期采用皮瓣下修复,Ⅳ期选用增生组织切除自体皮肤回植方法较好。     

香叶木素脂质体的处方优化及其体外释放

为改善香叶木素的水溶性,采用薄膜超声分散法制备其脂质体,并首先以包封率、粒径为指标进行单因素试验初步筛选处方和工艺参数,再通过Box-Behnken设计-响应面法进一步优化.结果表明,所得的香叶木素脂质体优化处方工艺如下:脂药比(即大豆磷脂与香叶木素的质量比)5.26、胆固醇质量6.31 mg、水化后磷脂浓度1.19 ...     

口服地奥司明片治疗肢体水肿临床分析

目的研究应用葛泰（微粒化地奥司明）口服治疗肢体水肿的近期疗效。方法108例肢体水肿患者随机分为2组。治疗组60例,应用葛泰口服治疗;对照组48例,应用小剂量利尿剂氢氯噻嗪口服,均连用2周。结果肢体水肿局部痛症状和局部水肿体征在治疗组中显效、有效和无效的频率分别为71.66%、20%和8.3%,总有效率为91.66%。而对照组分别为16.6%、60.4%和22.9%,总有效率7%。两组比较差异有统计学意义（P〈0.01）。而且治疗组主要表现为显效,而对照组主要表现为有效。结论口服葛泰治疗肢体水肿的近期疗效十分明显,优于口服小剂量利尿氢氯噻嗪,且无明显不良反应,值得推广。     

基于绘画训练的功能锻炼对乳腺癌术后患者淋巴水肿、患侧肢体功能的影响

目的 探讨基于绘画训练的功能锻炼对乳腺癌术后患者淋巴水肿、患侧肢体功能的影响。方法 按照随机数字表法将81例乳腺癌术后患者分为观察组和对照组,对照组40例予以常规护理干预,观察组41例在对照组基础上予以基于绘画训练的功能锻炼,观察两组患者淋巴水肿程度、患侧肢体功能以及功能锻炼依从性。结果 出院时,观察组上臂围、小臂围、腕围、掌围小于对照组（P<0.05）;观察组疼痛、日常生活能力、肩关节活动度、肌力评分高于对照组（P<0.05）;观察组身体锻炼、术后注意事项、主动寻求建议评分以及总分高于对照组（P<0.05）。结论 基于绘画训练的功能锻炼应用于乳腺癌术后患者有助于减轻患侧肢体水肿程度,改善患侧肢体功能,提高功能锻炼依从性。     

速碧林联合爱脉朗对下肢静脉曲张患者术后疗效和安全性的临床研究

目的 观察速碧林(低分子肝素钙)联合应用爱脉朗(地奥司明)减轻下肢静脉曲张患者术后症状,预防深静脉血栓的疗效和安全性.方法 对入选的90例下肢静脉曲张患者采用单中心、随机、开放、对照的方法进行采集和统计分析.入选患者随机分为试验组(即速碧林联合爱脉朗组30例)和对照组(速碧林组和爱脉朗组,即对照Ⅰ组和对照Ⅱ组各30例).观察术后肿胀、腿部沉重感及疼痛等各项症状,并行双下肢彩色多普勒超声检查评估下肢深静脉血栓(DVT)形成情况.安全性方面,观察患者术前和术后凝血酶原时间(PT)、血小板计数(PLT)及纤维蛋白原(Fib)等反映凝血功能变化指标及临床表现,比较组间、组内的差异.结果 术后1周试验组患者腿部肿胀、沉重感及疼痛等症状均较治疗前明显好转(P＜0.05);对照Ⅰ组症状与治疗前比较差异无统计学意义(P＞0.05).术后2周对照Ⅰ组、试验组患者无DVT等并发症,对照Ⅱ组则有5例出现肌间静脉血栓形成(P＜0.05).安全性方面,术前试验组和对照组患者PT、PLT及Fib的平均值均在正常值范围内,3组比较差异无统计学意义(P＞0.05).术后对照Ⅱ组患者PT延长,Fib升高,PLT术后第3天降低而术后第7天升高,与术前比较差异有统计学意义(P＜0.05).试验组患者PLT术后第3天降低,与术前比较差异有统计学意义(P＜0.05).术后对照Ⅱ组患者PT较试验组延长,Fib升高,差异有统计学意义(P＜0.05).对照Ⅰ组患者中出现血小板持续降低2例而被剔除.3组在治疗期间和术后均无严重出血,3组比较差异无统计学意义(P＞0.05).结论 预防性使用速碧林及爱脉朗对改善下肢静脉曲张术后患者的临床症状和体征、减少深静脉栓塞有效且安全.     

Nonbiological pharmacotherapies for the treatment of diabetic macular edema

Introduction: During the past decade, there have been significant advances in the pharmacotherapies for the treatment of diabetic macular edema (DME). Among the presently available treatment options, anti-vascular endothelial growth factors (anti-VEGF) agents are the most favored agents due to their efficacy and safety. The index review focuses on nonbiological therapies that have entered in phase 3 clinical trials for DME.

Areas covered: An extensive review of the literature was performed to identify various nonbiological immunotherapies i.e., drugs other than ‘-mAbs’ (monoclonal antibodies including anti-VEGF agents), ‘-mibs’ (proteasome inhibitors), ‘-NAbs’ (nanoparticle albumin-bound), and ‘-nibs’ (small molecule inhibitor/tyrosine kinase inhibitors), among others. Extended-release low-dose corticosteroid devices have been recently approved for the treatment of DME. Other compounds such as non-steroidal anti-inflammatory drugs, antibody mimetic proteins, nonbiological growth factor inhibitors, and inhibitors of protein kinase C have been described.

Expert opinion: A number of therapies are under development for the pharmacological management of DME. Due to the rising healthcare costs associated with anti-VEGF agents, a number of alternate treatment options have been explored recently. Some of these agents have reached phase 3 in clinical trials and appear to have a promising role in the management of DME. As further research is conducted, the role of each individual agent will become more defined, alone or in combination therapy.     

Fluocinolone acetonide for the treatment of diabetic macular edema

Introduction: Fluocinolone acetonide intravitreal implant is a non-erodible implant approved for the treatment of diabetic macular edema (DME) insufficiently responsive to available therapies.

Areas covered: The injectable intravitreal implant releases fluocinolone acetonide at an average rate of 0.2 µg/day for at least 36 months. The two pooled pivotal FAME trials showed that, in patients with DME previously treated with laser photocoagulation, fluocinolone acetonide intravitreal implant was more beneficial than sham injection when looking at the proportion of patients with an improvement from baseline in visual acuity of more than 15 letters at 24 months and at 36 months. Cataract (82%) and intraocular pressure (IOP) elevation (37%) were the most common adverse events. Raised IOP was mostly treated with IOP-lowering medications, with <5% of eyes requiring incisional IOP-lowering surgery. FAME trial program results are confirmed by a series of real-world studies in eyes with chronic/recalcitrant DME.

Expert opinion: data indicate that fluocinolone acetonide intravitreal implant is a useful second-line option for the treatment of DME.     

Fluocinolone acetonide for the treatment of diabetic macular edema

In addition to VEGF inhibitors such as ranibizumab, aflibercept or bevacizumab, clinical and experimental investigations have revealed the great potential of steroids in the treatment of DME. At present two intravitreal steroid inserts are approved for the treatment of DME containing either dexamethasone or fluocinolone acetat (FA) as a pharmacological compound. The non degradable intravitreal FA insert releases 0.2 µg FA per day (Iluvien, Alimera Sciences). Clinical phase III studies have demonstrated the beneficial effect of the FA insert to last up to three years, especially in patients with a prolonged history of DME of at least three years at the initiation of therapy. While the treatment appears to be well tolerated over all, side effects such as cataract formation in nearly all treated phakic patients and raise of intraocular pressure need to be discussed with the patients as potential complications of the treatment.     

2018年7月美国、欧盟和日本新批准药物概述

2018年7月,美国、欧盟和日本共批准36个新药,包括新分子实体、新有效成分、新生物制品、新增适应证及新剂型药物。对全球首次获得批准的新分子实体、新有效成分、新生物制品进行分析,重点介绍这些药物的临床研究结果和研发历史进程。

     

Pharmacokinetics of triamcinolone acetonide for the treatment of macular edema

INTRODUCTION: The use of intravitreal triamcinolone acetonide (TA) for the treatment of various types of macular edema has been widespread, particularly for the last decade. Currently, there is a scant amount of evidence-based literature evaluating the pharmacokinetic profile of TA despite clinical data showing the efficacy of intravitreal TA for multiple forms of macular edema. AREAS COVERED: This paper is an extensive review of human and experimental studies published on the pharmacokinetics of TA for the treatment of macular edema. The literature search was conducted via OVID, TRIP Database and EMBASE, up to April 2011. EXPERT OPINION: The pharmacokinetic profile of TA is unpredictable and the agent has a time-limited therapeutic action due to its relatively short half-life. This has led to the need for repeated injections. Future research should investigate the pharmacokinetic profiles of TA when administered intravitreally, as well as through alternate routes in more robust studies.     

灯盏花素注射液对肢端感觉异常症的循证治疗

目的从循证医学的角度,介绍灯盏花素注射液对肢端感觉异常症循证治疗方案的确立方法。方法以一位难治性肢端感觉异常症患者为例,介绍如何提出临床问题,怎样检索文献,如何对文献进行评价,怎样结合病例的具体情况和临床医生的个人经验,应用得到的证据拟定治疗方案。结果按照循证医学方法确立的以灯盏花素注射液为主治疗肢端感觉异常症患者22次后,患者症状得到明显改善。结论通过临床提出问题、寻找证据、分析证据、循证决策、循证实践过程,不但患者对疗效满意,医生也提高了理论水平和临床能力。     

Corticorelin acetate injections for the treatment of peritumoral brain edema

Background: The use of corticosteroids has been shown to be effective in the management of vasogenic edema caused by brain tumors, and is currently the standard of care. The associated systemic side effects, however, can be even more debilitating than the primary disease process, ultimately warranting premature discontinuation of steroids in some patients. In response, corticorelin acetate, a synthetic targeted human corticotropin-releasing factor (hCRF) analogue, has been developed to simulate the benefits of corticosteroids in treating peritumoral brain edema (PBE), while sparing the systemic toxicity. Objective: This article reviews the development of corticorelin acetate and its potential role in treating PBE as an alternative to standard corticosteroid therapy. Methods: Relevant articles and abstracts were obtained from searches of the medical and chemical literature databases, as well as from the references from published articles. Results/conclusion: Animal studies and a Phase I randomized trial have demonstrated that hCRF is well tolerated and effective in reducing PBE and its associated signs and symptoms. In addition, the effectiveness of this drug may be helpful in sparing the use of corticosteroid therapy in patients with brain tumors, with the results from several multicenter, randomized, placebo-controlled, Phase III clinical trials currently pending.