Solvent-mediated amorphous-to-crystalline transformation of nitrendipine in amorphous particle suspensions containing polymers

The amorphous-to-crystalline transformation of nitrendipine was investigated using Raman spectroscopy and X-ray powder diffraction (XRPD). The nucleation and growth rate of crystalline nitrendipine in a medium containing poly (vinyl alcohol) (PVA) and polyethylene glycol (PEG 200) were quantitatively determined using image analysis based on polarized light microscopy. The findings from the image analysis revealed that the transformation process occurred through the dissolution of amorphous drug precipitate followed by the nucleation and growth of the crystalline phase with the amorphous precipitate acting as a reservoir for maintaining the supersaturation. The rates of nucleation and crystal growth of nitrendipine decreased with an increase in PEG 200 concentration in organic phase from 0% to 75% (v/v). Increasing the PVA concentration in water phase from 0.1% to 1.0% (w/w) also decreased the rates of nucleation and crystal growth, however, an increase in PVA concentration from 1.0% to 2.0% (w/w) did not result in a further decrease in the rates of nucleation and crystal growth. An increase in drug concentrations in the organic phase from 10 mg/ml to 30 mg/ml led to faster nucleation rates. However, a further increase in drug concentration to 100mg/ml decelerated the growth of nitrendipine crystals. Combining image analysis of polarized light micrographs together with Raman spectroscopy and XRPD provided an in-depth insight into solid state transformations in amorphous nitrendipine suspensions.     

The antidepressant effect of Cynanchum auriculatum in mice

Context: Antidepressant effects of various plants are generally attributed to their anti-inflammation and antioxidant activities. Cynanchum auriculatum Royle ex Wight (Asclepiadaceae) is a traditional medicinal plant in China and India used for immunological regulation, anti-inflammation, and antioxidant purposes. However knowledge about its antidepressant activity has been poorly investigated. Objective:To investigate the antidepressant activities of the total glycosides of C. auriculatum (TGC) and its CHCl(3)/MeOH (10:1) fractions (TGC-D and TGC-E) in mice. Materials and methods: TGC, TGC-D and TGC-E (20, 40 and 80 mg/kg) were intragastrically administered to mice twice a day for 5 days. The tail suspension test, forced swimming test, and locomotor activity test in mice were used to evaluate the effect of C. auriculatum. The inhibition of [(3)H]-serotonin reuptake in rat brain synaptosomes was detected to investigate their mechanism. Results:TGC, TGC-D and TGC-E (80 mg/kg) decreased the immobility time by 61.7, 64.5, and 61.9% in tail suspension test. TGC (80 mg/kg), TGC-D (80 mg/kg) and TGC-E (20 mg/kg) decreased the immobility time by 32.6, 47.3, and 48.7% in forced swimming test. TGC (80 mg/kg) and TGC-E (20 and 40 mg/kg) decreased the crossing distances by 28.8, 29.5, and 36.2% in locomotor activity test. TGC, TGC-D and TGC-E (10 mg/L) inhibited serotonin reuptake by 7.4, 4.5, and 71.1% in rat brain synaptosomes, and IC(50) value of TGC-E was 5.2 mg/L. Discussion and Conclusion:TGC, TGC-D and TGC-E have potential antidepressant activities. The antidepressive effect of TGC-E maybe attributed partly by the inhibiting effect on serotonin reuptake.     

细胞分泌活动的实时监测技术

分泌活动是神经元和内分泌细胞进行化学通信的基本模式。各种研究细胞分泌活动的生物物理技术的发展极大地加深了人们对细胞分泌机制的了解。简要介绍了三种新近发展起来的实时监测细胞分泌活动的生物物理技术。     

人参糖肽注射液肽含量测定研究

目的：改进人参糖肽注射液肽含量测定方法。方法：参照《中国药典》（2005年版）一部附录VA＂紫外-可见分光光度法＂,将对照品溶液牛血清白蛋白浓度0.05 mg/mL改为0.1 mg/mL,供试品由＂精密量取本品5 mL,置50 mL量瓶中＂改为＂精密量取本品10 mL,置50 mL量瓶中＂,使供试品溶液的吸光度（A）值在0.3~0.7之间。结果：3批样品的检测结果显示,将供试品的测定浓度及对照品的浓度提高1倍后,供试品溶液的A值均在0.3~0.7之间。结论：改良的测定方法稳定可行,符合药品检验的规定。     

Synthesis of biscoumarin and dihydropyran derivatives as two novel classes of potential anti-bacterial derivatives

A series of bisoumarin (1–4) and dihydropyran (5–8) derivatives were successfully synthesized as new antibacterial agents. The molecular structures of three representative compounds 1, 5 and 7 were confirmed by single crystal X-ray diffraction study. Among these compounds tested toward Staphylococcus aureus (S. aureus ATCC 29213), methicillin-resistant S. aureus (MRSA XJ 75302), vancomycin-intermediate S. aureus (Mu50 ATCC 700699), and USA 300 (Los Angeles County clone, LAC), compounds 1 and 2 displayed the most potent antibacterial activity. Additionally, the HB energy in biscoumarins 1–4 was calculated by density functional theory (DFT) [B3LYP/6-31G*] method.     

机关工作人员高血压、糖尿病及高脂血症患病情况分析

目的了解机关工作人员高血压、糖尿病和高脂血症现患情况。方法对1462名体检人员的一般资料及血压、血糖和血脂等资料进行分析。结果①高血压现患率为21.8%,新诊断者占31.6%,过去确诊的高血压患者63.4%血压控制不达标;②糖尿病现患率为9.4%,空腹血糖受损和/或糖耐量减低现患率为12.5%,48.9%的糖尿病患者为首次确诊,过去确诊的糖尿病患者78.6%血糖控制不满意;③高脂血症现患率为41.5%,单纯高甘油三酯血症和单纯高胆固醇血症分别是16.6%和12.9%。高血压、糖尿病和高脂血症现患率基本上呈随龄递增趋势;体重指数(BMI)愈大,高血压、糖尿病和高脂血症患病率愈高。结论高血压、糖尿病和高脂血症是影响本组人群健康的常见病,年龄增大和体重增加是高血压、糖尿病和高脂血症的重要危险因素。     

玻璃体切割手术相关医源性视网膜裂孔的临床观察

目的分析玻璃体切割手术过程中医源性视网膜裂孔(iatrogenic retinal breaks,氉IRB)的发生率、危险因素及预防措施。方法回顾分析129例133眼玻璃体手术病例,记录眼别、术前诊断、玻璃体后脱离状态、晶状体状态,分析术中IRB的数目、分布及预防措施。结果 133眼中12眼术中出现13个IRB,总体发生率为9.0%。其中,黄斑裂孔或黄斑前膜33眼中3眼(9.1%)出现IRB,增生性糖尿病视网膜病变52眼中6眼(11.5%)出现IRB,玻璃体积血40眼中3眼(7.5%)出现IRB。8眼(6.0%)出现巩膜切口相关IRB,5眼(3.8%)出现其他区域IRB,其中1眼同时存在巩膜切口相关IRB及其他区域IRB。术中制作玻璃体后脱离组的IRB发生率(12.3%)高于术前存在玻璃体后脱离组(6.6%),但差异无统计学意义(P=0.256);有晶状体组的IRB发生率(10.5%)高于术中联合超声乳化组(4.5%)及人工晶状体或无晶状体组(8.0%),但差异均无统计学意义(均为P>0.05)。术后发生视网膜脱离4眼(3.0%),所有视网膜脱离眼经二次手术后视网膜均达到解剖复位。结论各种疾病行玻璃体切割手术均有发生IRB的可能,没有证据表明术中制作玻璃体后脱离及晶状体状态与IRB的发生具有明显相关性。为避免IRB可能引起的玻璃体术后视网膜脱离,术中仔细排查与处理是非常重要的。     

硅油在外伤性玻璃体视网膜手术中的临床作用

观察硅油在外伤性玻璃体视网膜手术中的作用。 方法：眼外伤患者36例36眼接受经睫状体扁平部玻璃体切除手术治疗,术中使用曲安奈德和激光,眼内填充硅油。术后8mo左右行硅油取出手术。 结果：硅油填充后,观察10mo。及时补充激光治疗。观察期内,视网膜平伏,未见眼内出血和严重增殖性反应,无感染性眼内炎。 结论：硅油在外伤性玻璃体视网膜手术中,可起到长期顶压视网膜,控制炎症反应,抑制增殖和预防感染的作用,并为术后及时补充激光治疗提供有利条件。     

α-晶状体蛋白的结构和功能及基因学研究进展

α-晶状体蛋白包括αA-,αB-晶状体蛋白,是哺乳动物晶状体的主要蛋白,属于小热休克蛋白家族成员,具有分子伴侣功能,可以抑制变性蛋白质的凝聚和酶的失活。α-晶状体蛋白基因突变可导致白内障和肌病。本文对α-晶状体蛋白的分布、结构、功能以及基因学等方面综述。