Carbon‐14 labeling of hydrochlorothiazide via [14C]formaldehyde production from [14C]carbon dioxide at ambient temperature

[¹⁴C]Formaldehyde was synthesized by reducing ¹⁴CO₂ at ambient temperature with Schwartz's reagent. The [¹⁴C]formaldehyde was then used in the radiosynthesis of high specific activity (2.1 GBq/mmol) [¹⁴C]hydrochlorothiazide via cyclization of 4‐amino‐5‐chloro‐1,3‐benzenedisulfonamide.     

替罗非班对急性心肌梗死急诊冠状动脉介入治疗冠状动脉微循环的影响

目的探讨并评价采用替罗非班对心肌梗死患者急诊实施冠状动脉介入治疗微循环产生的影响。方法将我院收治的ST段抬高性急性心肌梗死患者62例随机分成观察组32例与对照组30例,对比分析两组患者的临床状况、心电图ST段回落幅度、主要心脏不良事件及住院期间出血事件发生率等。结果观察组1.5 h心电图ST段回落幅度大于对照组,治疗前后比较差异具有统计学意义（P〈0.05）;观察组发生牙龈出血4例,对照组3例,两组均未见颅内出血与血小板减少症。术后观察组凝血因子TF与vWF均低于对照组,两组比较差异具有统计学意义（P〈0.05）,两组患者的PT与AFTT之间差异无统计学意义。结论采用替罗非班对心肌梗死患者急诊实施冠状动脉介入手术能够争取更多时间,以防止大量心肌细胞发生永久性坏死,有效解除心肌微循环障碍,明显降低无复流现象。     

Benzydamine hydrochloride buccal bioadhesive gels designed for oral ulcers: Preparation,rheological, textural,mucoadhesive and release properties

This study developed and examined the characterization of Benzidamine hydrochloride (BNZ) bioadhesive gels as platforms for oral ulcer treatments. Bioadhesive gels were prepared with four different hydroxypropylmethylcellulose (HPMC) types (E5, E15, E50 and K100M) with different ratios. Each formulation was characterized in terms of drug release, rheological, mechanical properties and adhesion to a buccal bovine mucosa. Drug release was significantly decreased as the concentration and individual viscosity of each polymeric component increased due to improved viscosity of the gel formulations. The amount of drug released for the formulations ranged from 0.76?±?0.07 and 1.14?±?0.01 (mg/cm²?±?SD). Formulations exhibited pseudoplastic flow and all formulations, increasing the concentration of HPMC content significantly raised storage modulus (G′), loss modulus (G″), dynamic viscosity (?′) at 37°C. Increasing concentration of each polymeric component also significantly improved the hardness, compressibility, adhesiveness, cohesiveness and mucoadhesion but decreased the elasticity of the gel formulations. All formulations showed non-Fickian diffusion due to the relaxation and swelling of the polymers with water. In conclusion, the formulations studied showed a wide range of mechanical and drug diffusion characteristics. On the basis of the obtained data, the bioadhesive gel formulation which was prepared with 2.5% HPMC K 100M was determined as the most appropriate formulation for buccal application in means of possessing suitable mechanical properties, exhibiting high cohesion and bioadhesion.     

Coupling of Metal Containing Homing Devices to Liposomes via a Maleimide Linker: Use of TCEP to Stabilize Thiol-groups without Scavenging Metals

Liposomes for drug delivery are often prepared with maleimide groups on the distal end of PEG to enable coupling of homing devices, such as antibodies, or other proteins. EDTA is used to stabilize the thiol group in the homing device for attachment to the maleimide. However, when using a homing device that contains a metal, EDTA inactivates this by scavenging of the metal. Holo-transferrin (Tf) containing two iron atoms (Fe³⁺), has a much higher affinity for the Tf receptor than apo-Tf (which does not contain any Fe³⁺). To couple Tf to a liposome, the introduction of a thiol group is necessary. During this process, by using N-succinimidyl S-acetylthioacetate (SATA), followed by 2–3 h coupling to the liposomes, Fe³⁺ is scavenged by EDTA. This causes a decreased affinity of Tf for its receptor, resulting in a decreased targeting efficiency of the liposomes.

Tris(2-carboxyethyl)phosphine (TCEP) hydrochloride is a sulfhydryl reductant that is often used in protein biochemistry. We found that TCEP (0.01 mM) does not scavenge Fe³⁺ from Tf and is able to protect thiol groups for the coupling to maleimide. Furthermore, TCEP does not interfere with the maleimide coupling itself.

In this communication, we describe the preparation of liposomes, focussing on the coupling of Tf to the maleimide linker at the distal end of PEG, without loosing Fe³⁺ from Tf. This method can be applied to other metal-containing homing devices as well.     

硝酸甘油注射液复合盐酸艾司洛尔注射液用于妊高征心衰的控制

目的寻找更有效控制妊高征产妇心衰的药物，为妊高征产妇心衰麻醉手术处理提供新方法。方法随机抽取广州市重症孕产妇救治中心妊高征心衰紧急剖宫产的产妇100例，采用双盲法随机分为A、B两组，每组50例。两组均进入手术室后先控制心衰后麻醉；A组硝酸甘油注射液5mg／ml以0．9％的氯化钠注射液稀释成10ml以0．05mg／kg快速单次静脉注射，同时复合盐酸艾司洛尔注射液1mg／kg快速单次静脉注射；B组单纯硝酸甘油注射液5mg／ml以0．9％的氯化钠注射液稀释10ml以0．05mg／kg快速单次静脉注射；4分钟、8分钟后观察各指标及相关症状并评判其有效性。结果A组产妇比B组控制心衰效果明显更好，用药后4分钟及8分钟A组SBP／DBP、HR、SPO2、RR、CVP、ECG等指标较B组明显改善俨〈0．05），端坐呼吸者可平卧接受气管插管麻醉。结论硝酸甘油注射液复合盐酸艾司洛尔注射液用于妊高征心衰比使用单纯硝酸甘油注射液更好，值得推广应用，硝酸甘油注射液与盐酸艾司洛尔注射液复合使用确能药效互补完全控制好心衰。     

来得时联合拜唐平治疗初发Ⅱ型糖尿病疗效观察

目的观察来得时联合拜唐平治疗初发Ⅱ型糖尿病的临床疗效，并作安全性评价。方法将符合初发Ⅱ型糖尿病纳入标准病例90例，按入院顺序随机分为治疗组45例与对照组45例，对照组予以诺和灵30R治疗，治疗组给予来得时联合拜唐平治疗，比较两组的疗效，以及两组治疗前后各项实验室指标的变化情况。结果治疗组总有效率明显优于对照组（P〈O．05），且治疗组在降低空服血糖、餐后2小时血糖及糖化血红蛋白水平方面均明显优于对照组（P〈0．05或P〈0．01）。治疗组低血糖发生率明显低于对照组，差异有统计学意义（P〈0．05）。结论来得时联合拜唐平治疗初发Ⅱ型糖尿病疗效确切，安全有效，低血糖发生率低，值得临床推广应用。     

盐酸环丙沙星壳聚糖纳米粒原位凝胶的制备与评价

目的 制备盐酸环丙沙星壳聚糖纳米粒原位凝胶，并评价其抑菌及创面愈合效果。方法 采用复乳法制备盐酸环丙沙星壳聚糖纳米粒，采用2因素2水平全因子析因实验设计考察了壳聚糖相对分子质量（X₁）和壳聚糖质量浓度（X₂）对壳聚糖纳米粒的药物包封率（Y₁）、粒径分布（Y₂）、多分散系数（Y₃）和Zeta电位（Y₄）的影响；并以泊洛沙姆407作为凝胶基质制备盐酸环丙沙星壳聚糖纳米粒原位凝胶。通过抑菌圈实验比较盐酸环丙沙星乳膏和盐酸环丙沙星壳聚糖纳米粒原位凝胶对金黄色葡萄球菌和铜绿假单胞菌的抑菌活性；使用无菌活检穿刺针在大鼠背部造成直径为5 mm的皮肤全切除的圆形人工创面，并使用金黄色葡萄球菌和铜绿假单胞菌的培养基感染24 h，建立大鼠创面模型，将模型大鼠随机分为模型组、盐酸环丙沙星乳膏组和盐酸环丙沙星壳聚糖纳米粒原位凝胶组，模型组大鼠创面未接受任何处理，给药组大鼠每2天给药1次，每次给药量均约为1 mg，观察并记录每组大鼠创面脱痂时间和愈合时间。结果 选择低相对分子质量壳聚糖、壳聚糖质量浓度为2.0 mg·mL^-1制备盐酸环丙沙星壳聚糖纳米粒，其中盐酸环丙沙星质量浓度为50.0 mg·mL^-1，其包封率为（85.3±0.9）%，平均粒径为（354.7±15.7）nm，PDI为0.357±0.014，Zeta电位为（22.2±0.5）mV，呈球状分布；盐酸环丙沙星壳聚糖纳米粒原位凝胶和盐酸环丙沙星乳膏对金黄色葡萄球菌的抑菌圈直径分别为（38.4±0.2）、（29.2±0.3）mm，对铜绿假单胞菌抗菌圈直径分别为（41.3±0.6）、（32.1±0.1）mm；大鼠创面给予盐酸环丙沙星壳聚糖纳米粒原位凝胶后，其脱痂时间和愈合时间均较模型组和盐酸环丙沙星乳膏组显著缩短（P<0.05）。结论 成功制备盐酸环丙沙星壳聚糖纳米粒原位凝胶，其可以抑制创面细菌繁殖、加速伤口愈合。     

SEDATION WITH DEXMEDETOMIDINE HYDROCHLORIDE DURING ENDOSCOPIC SUBMUCOSAL DISSECTION OF GASTRIC CANCER

Aim: Although the treatment of early gastric cancer with endoscopic submucosal dissection (ESD) has been widely carried out, a standardized method of sedation for ESD has not been established. The purpose of the present study was to evaluate the efficacy and safety of sedation with dexmedetomidine (DEX). Methods: We conducted a randomized study involving 90 patients with gastric tumors who were intended to be treated with ESD. The patients were sedated either with DEX (i.v. infusion of 3.0 µg/kg per h over 5 min followed by continuous infusion at 0.4 µg/kg per h [n = 30]), propofol (PF [n = 30]), or midazolam (MDZ [n = 30]). In all groups, 1 mg MDZ was added i.v. as needed. Results: En bloc resection of the gastric tumor was achieved in 88 (98%) patients. None of the DEX‐sedated patients showed a significant reduction of the oxygen saturation level. The percentage of patients who showed body movement in the DEX group was significantly lower than those in the PF and MDZ groups, and the mean dose of additional MDZ in the DEX group was significantly smaller than that in the MDZ group. The rate of effective sedation was significantly higher in the DEX group compared with the MDZ or PF group. The mean length of ESD in the DEX group was 65 min, which was significantly shorter than in the other two groups. No DEX‐sedated patient developed major surgical complications. Conclusions: Sedation with DEX is effective and safe for patients with gastric tumors who are undergoing ESD.     

Case Study: An intraoperative finding of black bone disease in a podiatric surgery patient

Black bone disease has been recognised as a potential consequence of long-term treatment with tetracycline antibiotics. Largely documented affecting structures in the head and skull, there are few reported cases of black bone disease in the foot and ankle. The case of a 55 years old patient, who as a teenager, had undergone treatment with minocycline hydrochloride for chronic acne, and was found to have bone discolouration consistent with minocycline induced black bone disease (MIBBD) during the course of hallux valgus corrective surgery some 40 years later, is presented. In spite of the intraoperative findings, the patient’s post-operative recovery and bone healing was uneventful. The literature on minocycline induced black bone disease is reviewed.     

盐酸米诺环素联合翻瓣术辅助治疗慢性牙周炎疗效的Meta分析

目的 系统评价牙周翻瓣术中使用2%盐酸米诺环素处理根面的疗效,为其治疗慢性牙周炎提供循证医学证据。方法 检索中国期刊全文数据库、维普、万方、中国生物医学文献数据库、PubMed、ScienceDirect和Embase等数据库,检索时限为从建库到2017年7月。由2名评价员独立筛选文献、提取资料并评价纳入研究的偏倚风险后,采用RevMan 5.3对数据进行Meta分析。结果 最终纳入7个随机对照实验,共217例受试者。Meta分析结果显示,与单纯翻瓣术（FO）组比较,盐酸米诺环素联合翻瓣术（FM）组患者随访3个月时的探诊深度减少[MD=-0.55,95%CI（-0.84,-0.26）,P=0.000 2],菌斑指数降低[MD=-0.08,95%CI（-0.15,-0.01）,P=0.03],随访6个月时探诊深度减少[MD=-0.62,95%CI（-1.04,-0.21）,P=0.003]方面更加明显,组间比较差异有统计学意义（P<0.05）。FM组患者随访3个月时在临床附着丧失获得[MD=-0.21,95%CI（-0.47,0.04）,P=0.10]方面改变的差异无统计学意义（P>0.05）。结论 在翻瓣下机械清创治疗慢性牙周炎中,使用2%盐酸米诺环素处理根面减少探诊深度和炎症控制方面有明显的效果。