目的:建立反相高效液相色谱法(RP-HPLC)测定叶黄素脂质体的含量.方法:采用Diamonsil(2)C18 (5μm,250 mm×4.6 mm)色谱柱,以100％纯乙腈为流动相,流速0.6 mL·min-1,检测波长为443 nm,进样量20 μL.结果:叶黄素的线性范围为6.96～69.57 μg·mL-1(r=0.999 8),平均加样回收率(n=9)为98.8％.3批样品的含量分别为98.61％、96.17％、100.51％.结论:本方法适用于叶黄素脂质体的含量测定.

Objective:To investigate the pharmacodynamics of Yuchang granules in the rat model of chronic ulcerative colitis(CUC) induced by 2,4,6-three nitrobenzene sulfonic acid (TNBS).Methods:Yuchang granules were prepared by fluidized granulation technology.A rat model of CUC was set up by TNBS.According to body mass stratification,72 rats were randomly divided into 6 groups:the normal control group,the model group,the Changyanning 10 g/kg group(as a positive control) and the Yuchang granules 5,10,15 g crude drug/kg groups.The drugs were administered by gavage once daily for 10 days.The body mass on days 2,4,6,8,10 and the numbers of the rat with diarrhea and hematochezia on days 1,3,5,7,9,10 were recorded.The visual and histopathological examinations of the colon were performed as well.Results:As compared with that of the normal control group,the weight gain of the model group decreased,hematochezia and diarrhea occurred in all the rats of the model group,and the scores of colon lesion and colon histopathology were all higher than those of the rats in the normal control group.Statistical significance could be seen,when comparisons were made between the 2 groups (P＜0.01).The weight gain at 2,4,6,8,10 days in the rats of the Changyanning group was significantly greater than that of the rats in the model group,the number of the rats with hematochezia at 7,9,10 days was significantly less (P＜0.05),the number of the rats with diarrhea at 7 days significantly decreased (P＜0.05),and the scores of colon lesion and colon histopathology all de creased as compared with those of the model group.Statistical significance could also be noted,when comparisons were made between the 2 groups (P＜0.01).Changes in the body mass of the rats in the Yuchang granules 15 g crude drug/kg group were obviously greater than those of the rats in the model group (P＜0.01),the number of the rats with hematochezia at 7 and 9 days obviously decreased (P＜0.05) and the number of the rats with diarrhea at 7 days also obviously decreased (P＜0.05).The scores of colon lesion and colon histopathology for the rats in the 10 or 15 g crude drug/kg Yuchang granules groups all dropped considerably as compared with those of the model group,with a dose-dependent trend (P＜0.01),and the effect of 15 g crude drug/kg Yuchang granules was equivalent to that of the effect of 10 g crude drug/kg Changyanning granules.Conclusion:Yuchang granules could decrease the rates of hematochezia and diarrhea in the model rats with CUC,and dose-dependently alleviate colon lesion and promote ulcer healing.

Objective To investigate the extraction process of Yuchang granules .Methods The extraction process was optimized by orthogonal experiment based on the content of berberine ,atractylodes lactone Ⅰ and the extraction yield .Results Through the visual analysis of orthogonal experiment ,the analysis of variance and the verification experiments ,the optimum extraction process was obtained as follows :extracting 1 h for twice with 10 times water of medicinal herbs and the 70％ ethanol depositing concentration .Conclusion This process is consistent and feasible .It is a simple and convenient method to extract Yuchang granules .

1999年Ross提出动脉粥样硬化(atherosclerosis,AS)属于炎症性疾病[1].炎症是机体为了减轻细胞损伤而自动采取的防御反应.炎症会在人体内引发一系列的疾病,其中有些疾病患病率较高,并且容易导致死亡,比如AS等.而AS又是心血管疾病的重要诱因,全球每年因病死亡的人数有一半是心血管疾病患者[2]. 炎症小体(inflammasome)是天然免疫系统的组成部分,大量的研究证实了炎症小体与AS、心肌病、痛风等疾病的发展存在着关联.炎症小体响应于广泛的危险信号促进炎症的发展.NLRP3[nucleotide-binding domain and leucine-rich repeat containing (NLR) family,pyrin domain containing 3]是最常见的炎症小体[3],在AS的形成中起着重要作用,其沉默可促进AS斑块的稳定[4].

目的:为优化社区药学服务(CPC)工作模式和服务内容,发挥社区药师在家庭医生团队中的作用提供借鉴.方法:设计调查问卷,对上海市虹口区8家社区卫生服务中心(CHCC)的家庭医生团队成员(家庭医生-家庭护士-公共卫生人员人数比为3:3:1)进行问卷调查与分析,了解家庭医生团队成员对CPC的认知、评价和需求.结果:共回收有效问卷224份(其中家庭医生96人、家庭护士96人、公共卫生人员32人),问卷有效率100％.77位(34.4％)被调查者"了解"CPC;157位(70.1％)被调查者"非常想"获得关于合理用药方面的帮助和支持;家庭医生团队3种岗位成员在对CPC的了解渠道、对社区药师应掌握临床知识的程度及对社区药师参与治疗方案制定的建议采纳程度上等项目的调查结果有差异.结论:家庭医生团队成员对CPC工作有一定的认知,且有较高的需求;现有的家庭医生团队成员构成仍有必要进行完善,有必要让社区药师参与家庭医生药疗工作.同时,还应进一步加大社区药师队伍的培养,优化知识结构,优化服务能力,使其能提供优质的CPC,满足不同家庭医生团队成员的需求.

目的:观察复方冬虫夏草口服液对载脂蛋白E基因敲除(ApoE-/-)小鼠动脉粥样硬化(AS)的影响,并探讨其作用机制.方法:将45只雄性ApoE-/-小鼠随机分为模型组(生理盐水)、阳性对照组(阿托伐他汀,5 mg/kg)和复方冬虫夏草口服液低、中、高剂量组(0.4、1.2、3.6 g/kg,以生药量计),每组9只;另取9只雄性C57BL/6J小鼠作为空白对照组(生理盐水).除空白对照组小鼠给予普通饲料外,其余各组小鼠均给予高脂饲料以复制AS模型,并于造模同时每天灌胃给药1次,连续8周.末次给药后,分离血清,检测各组小鼠血清中总胆固醇(TC)、三酰甘油(TG)、低密度脂蛋白胆固醇(LDL-C)、高密度脂蛋白胆固醇(HDL-C)水平;分离胸主动脉及主动脉窦,以油红O染色,检测胸主动脉斑块损伤面积比(即胸主动脉斑块面积与胸主动脉总面积的比值)和主动脉窦脂质损伤面积比(即主动脉窦脂质沉积面积与主动脉窦管腔总面积的比值);采用免疫组化法测定主动脉窦巨噬细胞表达量(即巨噬细胞阳性表达面积与斑块面积的比值).结果:与空白对照组比较,模型组小鼠血清TC、TG、LDL-C水平显著升高,HDL-C水平显著下降(P<0.01);胸主动脉斑块形成明显,主动脉窦脂质沉积明显增多,其斑块损伤面积比和脂质损伤面积比均显著升高(P<0.01);主动脉窦巨噬细胞阳性表达明显增加,其表达量显著升高(P<0.01).与模型组比较,各给药组小鼠血清TC、TG、LDL-C水平均显著降低,HDL-C水平均显著升高(P<0.05或P<0.01);胸主动脉斑块面积及主动脉窦脂质沉积明显减少,其斑块损伤面积比和脂质损伤面积比均显著下降(P<0.05或P<0.01);主动脉窦巨噬细胞浸润明显减少,其表达量显著下降(P<0.05或P<0.01).结论:复方冬虫夏草口服液可抑制AS斑块形成,其机制可能与降低血清TC、TG、LDL-C水平,缩小胸主动脉斑块面积,减少主动脉窦脂质沉积和巨噬细胞浸润有关.

无定型药物活性成分(active pharmaceutical ingredients,APIs)比晶型APIs具有更高的表观溶解度,但其热稳定性极差,贮藏中易转变为稳定的结晶型.将晶型APIs无定型化,制备成无定型固体分散体(amorphous solid dispersion,ASD),使无定型APIs长期稳定,为药物制剂开发尤其是BCS(biopharmaceuticalclassification system,BCS)Ⅱ类或Ⅳ类的难溶性APIs制剂的开发,提供了一种新方法.本文主要对无定型态的APIs热力学特征,制备无定型固体分散体的制备技术及载体进行综述,其中对新型纳米无机载体和适用于工业化生产的无定型固体分散体制备技术进行详细叙述和评价.

Objective To study the physicochemical properties of aqueous solution of surface active drug montelukast so-dium (MS) ,which could provide experimental basis for further development of micelle or mixed micelle preparations .Methods Critical micelle concentration (CMC) of MS at different temperatures were determined by conductivity measurements .The absorbance and transmittance of MS aqueous solution were measured by UV at different sodium chloride concentration levels . The micelle stability was evaluated via high speed centrifugal .Results The CMC of MS aqueous solution at 25℃ ,30℃ ,35℃were 0 .75 ,0 .82 ,0 .90 mmol/L .The absorbance and transmittance of MS aqueous solution were affected by the sodium chlo-ride concentration and the concentration of MS itself .It was observed that a clear solution was obtained when MS concentration>7 .5 mmol/L and no precipitation was noticed even after high speed centrifugal .Conclusion Montelukast sodium is a surface active drug .Its solubility is related to MS concentration .The solubility is also sensitive to the temperature and the electrolyte concentration .These unique physicochemical properties could be used to develop micelle or mixed micelle pharmaceutical prepa-rations .

OBJECTIVE:To improve community pharmaceutical care so as to promote the rational drug use of community resi-dent and improve the quality of life. METHODS:By analyzing the situation of community pharmaceutical care,the pharmaceutical care of community pharmacists was improved by changing pharmaceutical care mode,actively developing the propaganda of ratio-nal drug use,strengthening retraining of clinical pharmacists. RESULTS:With the help of Hongkou district quality control group, many hospitals of the district signed the"pharmaceutical linkage assistance agreement". Through the efforts of Hongkou district quality control group and many hospitals,community pharmaceutical care was improved and the propaganda of rational drug use has achieved certain results. CONCLUSIONS:Through exploration and practice,the pharmaceutical care levels of community phar-macists have been improved and the rational drug use of community residents has been promoted.

Objective To study the influence of Sargassum thunbergii and fucoidan on the blood lipid level in experimental hyperlipoidemic mice.Methods Mice were randomly divided into normal control group,hyperlipoidemic model group,positive group,petroleum ether group,ethyl acetate group,butanol group,fucoidan group.Each group was fed respectively with common forage or high cholesterol forage.2 weeks later,each group was fed respectively with corresponding drug.2 weeks later,the level of total cholesterol (TC),triglyceride (TG),low density lipoprotein cholesterol (LDL-C) and high density lipoprotein cholesterol (HDL-C) were determined.Results The level of TC and LDL-C were 2.94±-0.34,0.69±0.12 mmol · L-1 in butanol group,lower than those in hyperlipoidemic model group;The TC and LDL-C were 2.42±0.62,0.52±0.08 mmol · L-1 in fucoidan group,lower than those in hyperlipoidemic model group also.The two group could also improve the liver index and fat index.Conclusion Fucoidan group and butanol group could reduce the blood lipid level in experimental hyperlipoidemic mice.

OBJECTIVE:To establish a method for the content determination of loxoprofen silver in Loxoprofen silver cream, and provide reference for the quality control of the preparation. METHODS:HPLC was performed on the column of Diamonsil C18 with mobile phase of methanol-water-glacial acetic acid-triethylamine(55:45:0.1:0.1,V/V/V/V)at a flow rate of 1.0 mL/min,de-tection wavelength was 223 nm,column temperature was 30 ℃,and the injection volume was 20 μL. RESULTS:The linear range of loxoprofen silver was 6.53-130.7μg/mL(r=0.9999);the limit of quantitation was 0.253μg/mL,limit of detection was 0.076μg/mL;RSDs of precision,stability and reproducibility tests were lower than 2%;recovery was 96.79%-103.68%(RSD=2.23%, n=9). CONCLUSIONS:The method is simple,accurate and reproducible,and can be used for the content determination of Loxo-profen silver cream.

目的：为叶黄素的制剂研究提供参考。方法：以“叶黄素”“药理作用”“剂型”“应用”“Lutein”“Antioxidant”等为关键词，组合查询2006年1月－2016年7月在PubMed、Elsevier、中国知网、万方、维普等数据库中的相关文献，对叶黄素的理化性质、体内过程、抗氧化活性、生物学作用、剂型研究及应用现状等方面进行综述。结果与结论：共检索到相关文献696篇，其中有效文献47篇。叶黄素含有独特的紫罗酮环二羟基结构，可作为强抗氧化剂淬灭单线态氧和蓝光过滤器，具有抗氧化、抗癌、保护视网膜、预防心血管疾病等生物学作用。但叶黄素的理化性质不稳定，在制剂过程中存在水溶性差、性质不稳定和生物利用度低等问题；叶黄素在体内只能与脂类结合吸收，这一特点大大制约了其药效的发挥。通过物理包埋和化学改性（如酯化反应）等方法改变剂型，并利用超微粉碎和微囊化等技术将叶黄素制备成油悬浮液、水分散性干粉、微胶囊和脂质体，能较好地解决这些问题。但如何进一步提高叶黄素的生物利用度、减小对胃肠道作用的影响、改善传统制剂粒径过大等问题还有待进一步研究。

Objective To prepare paeoniflorin gastric floating tablets and to optimize the formulation.Methods Gastric floating tablets were prepared by wet granulation,with floating performance and in vitro cumulative release rate as evaluat indi-cators,single factor tests and orthogonal design test were adopted for the optimal formulation.Results With HPMC K4M 20% as reinforcing materials,NaHCO315% as gas agent,PVPP 7% as the release of accelerator,lactose as a filler,the ob-tained gastric floating tablet can immediately play bleaching,continued to float more than 12 hours,and the cumulative release rate was more than 90%.Conclusion The optimal formulation of paeconiflorin floating tablet has achieved a sustained and slow release request floating,the operability is good.

目的 研究瑞巴派特在体胃肠道吸收动力学的特征.方法 采用大鼠胃部定时取样和单向肠灌流技术,HPLC法测定瑞巴派特的含量,对瑞巴派特在大鼠胃部和不同肠段吸收进行研究.结果 在0～120 min,大鼠胃部吸收呈线性吸收规律,120 min后胃中平均吸收率为28.47％;瑞巴派特在不同肠段的净累计吸收量为十二指肠＞空肠＞回肠＞结肠,并与瑞巴派特吸收速率常数Ka顺序保持一致;瑞巴派特在20～100 μg ·ml-1对小肠吸收速率常数Ka无影响.结论 瑞巴派特为全胃肠道吸收药物,以胃和十二指肠为主要吸收部位,提示瑞巴派特可以设计制成缓控释制剂.

Celastrus orbiculatus Thunb .(Celastraceae) was widely distributed in China and more in the south area of the Yangtze River .Research showed the main chemical components including terpenoids ,lipids ,glycosides and flavonoids .Its pharmacological effects were extensive ,which were including antitumor ,anti-inflammatory ,immunomodulatory ,anti-fibrosis and anti-fertility etc .The separation of active compositions and advances in the pharmacological effects were reviewed in recent years ,which would be helpful in providing reference and thinking for the research and development of Celastrus orbiculatus .

阿尔茨海默病（ Alzheimer′s disease， AD）是中枢神经系统的一种退行性病变，其临床主要表现为记忆力的下降及其认知功能的减退，尤以近事遗忘为主的一种大脑器质性精神病。近年AD发病率呈逐年上升趋势，我国65岁以上人群中患病率约占5％，85岁以上人群中约占20％。 AD除年龄、遗传和环境等因素外，脑内多种神经递质紊乱，脑血管病变至神经细胞死亡或减少为重要因素。目前预防和治疗AD主要以受损伤的脑神经的修复，活血通淤，改善脑循环为主要手段。人参是我国传统名贵中药，具有补血、生血、活血、安神等多种功效，对机体神经、免疫和心脑血管等多个系统均有显著的保护和治疗作用［1-3］。人参中的主要有效成分为人参皂苷Rg1，它是促进和改善AD学习和记忆的组织形态学基础。本文主要从人参皂苷Rg1的纯化工艺和药理机制等方面探讨其预防和治疗AD的可能性。

目的 建立HPLC法测定舒肝灵茶中特女贞苷含量的方法.方法 采用Diamonsil C18色谱柱(250 mm × 4.6mm,5μm);流动相:乙腈-水(18∶82);流速:1.0 ml ·min-1;检测波长:224 nm;柱温:25 ℃.结果 特女贞苷在8.064 ～403.2μg ·ml-范围内线性关系良好(r =0.9999),平均加样回收率为100.9％,RSD为1.93％,n=9.结论 该方法简便,快速准确,可用于舒肝灵茶中特女贞苷的质量控制.

Objective To researcb tbe pbarmacological effect of antifatigue and immunopotentiation of Compound Ganoderma Lucidum Spore Oil Soft Capsule. Methods Kunming mice were radomly devided into five groups:tbe low,middle and bigb FFLZB doses groups [ 385,770,1 540 mg/ ( kg·d)] ,control red gingseng etbanol extract group and blank control group. Tbe pole-climbing time,serum cre-atinine kinase(CK)and adenosine tripbospbate(ATP)contents on 14 d after medication gavage were detected. At tbe same time tbe immune organ index metbod,cleaning carbon particle metbod and digits tbickening metbod were adopted to detect delayed type bep-ersensitivity(DTH)for investigating tbe influence of CGOC on mice′s immune function. Results Tbe bigb,middle and low doses FFLZB groups could prolong tbe pole-climbing time in different degrees,tbe middle and bigb doses groups could significantly increase tbe serum ATP level after pole-climbing,only tbe low dose group could significantly increase serum CK level after pole-climbing;com-pared witb tbe blank control group,tbe bigb,middle and low FFLZB doses groups could inbibit tbe decrease of mice immune organ in-dex in different degrees,increased tbe level of leaning carbon particles and 24,48 b DTH degree. Conclusion FFLZB bas tbe an-tifatigue and immunopotentiation effect and is a compound Cbinese medicine preparation for effective antifatigue.

Objective To investigate the chemical constituents of Ulva fasciata and identify the material base of the efficacy.Methods The constituents of Ulva fasciata were separated and purified on chromatography of silicon gel,and then their structures were identified based on their physical and chemical nature and the specula.DPPH method was used to evaluate free radical scavenging activity of the compounds.Results Five compounds were isolated from Ulva fasciata and identified as 5-hydroxy-3,6,7,3',4'-pentamethoxyflavone,5-hydroxy-6,7,3',4'-tetramethoxyflavone,2,5-keto-pyrrolepiperazidine,p-hydroxybenzcic acid,succinic acid.Conclusions All the compounds were isolated from Ulva fasciata for the first time,of which compound 1 and 2 showed relatively strong antioxidant activity.

目的:为复发性口腔溃疡(ROU)的临床治疗提供参考.方法:查阅近年国内相关文献,对ROU的化学药治疗、中西医结合治疗以及中医药治疗的进展情况进行归纳和总结.结果:ROU的化学药治疗药理作用明确,使用方便,患者易于接受;中西医结合治疗能提高疗效,降低毒副作用,优于传统西医治疗;中医药治疗刺激性小、无明显不良反应,但缺乏统一的中医辨证标准和有效的中药制剂.结论:化学药治疗在ROU治疗中具有重要作用,中西医结合是ROU治疗的主要导向,中医药治疗需统一中医辨证标准.相关学者需加强有效制剂的研究,结合ROU的发生机制和目标药物的药理药效,探索出更合理的ROU治疗方案.