提高芪鹿益肾片稳定性的方法研究

目的 筛选适宜的防潮辅料以提高芪鹿益肾片浸膏粉的临界相对湿度,从而提高芪鹿益肾片的稳定性。方法 以浸膏粉的临界相对湿度为评价指标,采用单因素法考察微晶纤维素、微粉硅胶、无水乳糖及甲壳素4种不同的辅料对芪鹿益肾片浸膏粉吸湿性能的影响,并采用长期稳定性试验研究制剂的稳定性。结果 在芪鹿益肾稠浸膏中加入上述辅料后,可使芪鹿益肾浸膏粉临界相对湿度从原工艺的53%分别提高至63%、65%、62%、71%,以0.5%甲壳素改善效果最佳,且长期稳定性研究表明采用该辅料后芪鹿益肾片的质量稳定。结论 在芪鹿益肾稠浸膏中加入适量的甲壳素,能显著提高芪鹿益肾浸膏粉的临界相对湿度,改善芪鹿益肾片的吸潮性,降低制剂工艺中的环境要求,有效地保证芪鹿益肾片的稳定性。     

非那雄胺胶囊剂的制备及其稳定性研究

目的：开发非那雄胺制剂新品种，满足临床用药需要。方法：采用溶媒分散法制粒后填装硬胶囊制备胶囊剂，高效液相色谱法（HPLC）测定其含量及含量均匀度，同时以进口片剂为对照，用桨板法测定其溶出度，并进行光照、高温、高湿、加速及长期试验等稳定性初步研究。结果：所建立的HPLC法准确、可行、重现性好，3批样品的含量分别为99.95%、100.50%和99.80%，含量均匀度与溶出度均符合规定，稳定性初步考察结果表明，非那雄胺胶囊稳定性良好，可暂定有效期为2年。结论：非那雄胺胶囊是一理想的口服制剂。     

氧氟沙星纳米粒制备工艺的优化及稳定性考察

目的:制备粒径小、形态均匀和包封率高的氧氟沙星纳米粒,并对纳米粒的稳定性进行考察.方法:选用聚氰基丙烯酸丁酯为载体,在单因素实验基础上结合均匀实验设计优化出氧氟沙星纳米粒的制备工艺,并从温度、湿度和光照3个方面对纳米粒的稳定性进行考察.结果:采用此方法制备的纳米粒粒径小,形态均匀,载药量高,包封率可达69.69%,且稳定性好.结论:此氧氟沙星纳米粒的制备工艺切实可行.     

二苯乙烯苷的稳定性研究

目的　考察影响二苯乙烯苷 (THSG)溶液稳定性的因素 ,并计算室温下其晶体粉末的 t0 .9值。方法　采用HPL C法和 HPL C- MS联用法。结果　以 L ichrospher5 - C1 8(2 5 0 m m× 4 .6 m m,5 μm)为固定相 ,甲醇 -水 (4∶ 6 )为流动相 ,检测波长为 310 nm。 THSG进样量在 0 .14～ 2 .80μg与峰面积线性关系良好 ,自制 THSG纯度高达99.94 % ,p H5 .8时 ,THSG与水分子发生加成反应。强酸促使 THSG水解为葡萄糖和苷元 ,并进一步降解为酚类化合物。强碱性条件下 ,THSG氧化为醌类化合物。在中性及弱碱性水溶液中较稳定 ,30 d内含量无明显变化。THSG晶体粉末室温下放置 2 4 0 d含量无明显变化 ,t0 .9值为 10 98d。结论　二苯乙烯苷在一定条件下是稳定的     

荆芥内酯聚乳酸乙醇酸纳米粒的制备及其稳定性研究

目的制备荆芥内酯聚乳酸乙醇酸纳米粒,并优化其制备工艺。方法以粒径、分散度、包封率和载药量为指标,对溶剂挥发法、溶剂扩散法和溶剂-非溶剂法制备荆芥内酯纳米粒进行比较。在单因素考察基础上,采用正交设计法对纳米粒的处方和溶剂-非溶剂法制备工艺进行优化,并考察了4℃和25℃条件下纳米粒溶液的稳定性。结果溶剂-非溶剂法制备的荆芥内酯纳米粒形态圆整,大小均匀,平均粒径(80.3±1.75)nm,分散度0.0144±0.00625,包封率可达52.53%±0.97%,载药量27.56%±0.91%,显著优于溶剂挥发法和溶剂扩散法,且具有良好的稳定性。结论溶剂-非溶剂法制备荆芥内酯纳米粒具有工艺简便,粒径和分散度小,包封率和载药量高,重复性好,质量稳定的优点。     

Taxifolin stability: In silico prediction and in vitro degradation with HPLC-UV/UPLC–ESI-MS monitoring

Taxifolin has a plethora of therapeutic activities and is currently isolated from the stem bark of the tree Larix gmelinni (Dahurian larch). It is a flavonoid of high commercial interest for its use in supplements or in antioxidant-rich functional foods. However, its poor stability and low bioavailability hinder the use of flavonoid in nutritional or pharmaceutical formulations. In this work, taxifolin isolated from the seeds of Mimusops balata, was evaluated by in silico stability prediction studies and in vitro forced degradation studies (acid and alkaline hydrolysis, oxidation, visible/UV radiation, dry/humid heating) monitored by high performance liquid chromatography with ultraviolet detection (HPLC-UV) and ultrahigh performance liquid chromatography-electrospray ionization-mass spectrometry (UPLC-ESI-MS). The in silico stability prediction studies indicated the most susceptible regions in the molecule to nucleophilic and electrophilic attacks, as well as the sites susceptible to oxidation. The in vitro forced degradation tests were in agreement with the in silico stability prediction, indicating that taxifolin is extremely unstable (class 1) under alkaline hydrolysis. In addition, taxifolin thermal degradation was increased by humidity. On the other hand, with respect to photosensitivity, taxifolin can be classified as class 4 (stable). Moreover, the alkaline degradation products were characterized by UPLC-ESI-MS/MS as dimers of taxifolin. These results enabled an understanding of the intrinsic lability of taxifolin, contributing to the development of stability-indicating methods, and of appropriate drug release systems, with the aims of preserving its stability and improving its bioavailability.     

pshRNA-survivin脂质体的制备及初步稳定性考察

目的:制备包封率高、粒径均匀、稳定性好的pshRNA-survivin脂质体,并对其质量进行评价.方法:采用逆相蒸发法制备pshRNA-survivin脂质体;正交设计优选制备处方;考察脂质体的粒径分布、zeta电位;用超滤离心法测定脂质体的包封率;离心加速实验与渗漏率的测定考察脂质体的稳定性.结果:所得优化处方为磷脂...     

Interventions to improve chronic cyclosporine A nephrotoxicity through inhibiting renal cell apoptosis: a systematic review

Objective To reveal interventions for chronic cyclosporine A nephrotoxicity （CCN） and provide new targets for further studies,we analyzed all relevant studies about interventions in renal cell apoptosis.Data sources We collected all relevant studies about interventions for cyclosporine A （CsA）-induced renal cell apoptosis in Medline （1966 to July 2010）,Embase （1980 to July 2010） and ISI （1986 to July 2010）,evaluated their quality,extracted data following PICOS principles and synthesized the data.Study selection We included all relevant studies about interventions in CsA-induced renal cell apoptosis no limitation of research design and language） and excluded the duplicated articles,meeting abstracts and reviews without specific data.Results There were three kinds of intervention,include anti-oxidant （sulfated polysaccharides,tea polyphenols,apigenin,curcumin,spirulina,etc）,biologics （recombinant human erythropoietin （rhEPO）,a murine pan-specific transforming growth factor （TGF）-beta-neutralizing monoclonal antibody1D11,cartilage oligomeric matrix protein （COMP）-angiopoietin-1 and hepatocyte growth factor （HGF） gene）,and other drugs （spironolactone,rosiglitazone,pirfenidone and colchicine）.These interventions significantly improved the CCN,renal cell apoptosis and renal dysfunction through intervening in four apoptotic pathways in animals or protected renal cells from apoptosis induced by CsA and increased cell survival through respectively four pathways in vitro.Conclusions There are three group interventions for CCN.Especially anti-oxidant drugs can significantly improve CCN,renal cell apoptosis and renal dysfunction.Many drugs can improve CCN through intervening in Fas/Fas ligand or mitochondrial pathway with sufficient evidences.Angiotensin Ⅱ,nitric oxide （NO） and endoplasmic reticulum （ER） pathways will be new targets for CCN.     

犬组织匀浆中乌头碱的高效液相色谱-质谱测定法及体外稳定性研究(英文)

目的建立了犬组织匀浆中有毒生物碱乌头碱的高效液相色谱-质谱测定法,并应用该方法考察了乌头碱在犬主要组织匀浆中的代谢稳定性。方法色谱柱为C18柱,流动相为含有5 mmol/L甲酸铵和0.2%甲酸的乙腈和水,梯度洗脱。三重四级杆串联质谱配备电喷雾电离源(ESI),正离子模式下以选择离子监测进行检测。乌头碱分别与犬的肝、小肠、胃和肾的组织匀浆温孵,温孵后不同时间点取出,加入内标西酞普兰,乙腈沉淀后取上清液直接进样测定。结果乌头碱浓度在5～500 ng/ml峰面积和内标的比值与浓度呈良好的线性关系;方法的回收率为85.73%～92.12%,其日内、日间的RSD值分别为5.32%～8.95%和5.45%～8.86%。体外孵育2 h后,在犬肝、小肠匀浆中有约20%的乌头碱进行了代谢转化,其t1/2分别为460.6和521.3 min。但在胃和肾中几乎无变化。结论研究提示犬体内的乌头碱主要在小肠、肝脏中代谢转化,但其代谢和清除较慢。     

后踝骨折研究进展与争论

目的：总结后踝骨折研究进展 数据源：主要使用Pubmed数据库资源 文献选择：选取与后踝骨折或三踝骨折有关的文献 结果：对于多大后踝骨折块影响踝关节稳定并需要手术尚无一致结论。X线评估后踝骨折不可靠,CT推荐使用,特别是胫骨干骨折合并隐匿性后踝骨折,其发生率以往被低估。通过后外侧入路直视下钢板固定后踝骨折块临床效果良好。固定后踝相较于下胫腓螺钉更适用于下胫腓损伤。手术指征和功能锻炼时机仍有争议。 结论：踝关节稳定性判断、选择适宜的诊断评估手段和手术方法有利于后踝骨折处理。需要更多的踝关节稳定性和不同治疗方式对比等方面的基础临床研究。     

移动图书馆理论与应用研究综述

简述了国内外移动图书馆的发展背景,归纳了国内外移动图书馆的服务模式、服务功能和服务内容,对比了国内外移动图书馆的应用现状,并对服务功能进行了比较分析,探讨了国内移动图书馆的发展方向。     

Educational and organizational interventions to improve the management of depression in primary care: a systematic review

Context  Depression is commonly encountered in primary care settings yet is often missed or suboptimally managed. A number of organizational and educational strategies to improve management of depression have been proposed. The clinical effectiveness and cost-effectiveness of these strategies have not yet been subjected to systematic review. Objective  To systematically evaluate the effectiveness of organizational and educational interventions to improve the management of depression in primary care settings. Data Sources  We searched electronic medical and psychological databases from inception to March 2003 (MEDLINE, PsycLIT, EMBASE, CINAHL, Cochrane Controlled Trials Register, United Kingdom National Health Service Economic Evaluations Database, Cochrane Depression Anxiety and Neurosis Group register, and Cochrane Effective Professional and Organisational Change Group specialist register); conducted correspondence with authors; and used reference lists. Search terms were related to depression, primary care, and all guidelines and organizational and educational interventions. Study Selection  We selected 36 studies, including 29 randomized controlled trials and nonrandomized controlled clinical trials, 5 controlled before-and-after studies, and 2 interrupted time-series studies. Outcomes relating to management and outcome of depression were sought. Data Extraction  Methodological details and outcomes were extracted and checked by 2 reviewers. Summary relative risks were, where possible, calculated from original data and attempts were made to correct for unit of analysis error. Data Synthesis  A narrative synthesis was conducted. Twenty-one studies with positive results were found. Strategies effective in improving patient outcome generally were those with complex interventions that incorporated clinician education, an enhanced role of the nurse (nurse case management), and a greater degree of integration between primary and secondary care (consultation-liaison). Telephone medication counseling delivered by practice nurses or trained counselors was also effective. Simple guideline implementation and educational strategies were generally ineffective. Conclusions  There is substantial potential to improve the management of depression in primary care. Commonly used guidelines and educational strategies are likely to be ineffective. The implementation of the findings from this research will require substantial investment in primary care services and a major shift in the organization and provision of care.      

Induction of labour: a continuous quality improvement and peer review program to improve the quality of care

This article describes a program developed to improve the process of planned induction of labour and to reduce the rates of inappropriate induction. The setting is a tertiary-care maternity hospital in urban Vancouver, BC, in which 7000 deliveries take place annually. Approximately 65% of these can be considered primary care; the remainder are secondary- or tertiary-level cases. Continuous quality improvement (CQI) methods were used by a multidisciplinary team, which included nursing staff, physicians, health records personnel and a CQI facilitator. Interventions included the development of a new induction-booking process, clear criteria for induction, feedback to caregivers about changes and a peer review system to oversee and maintain improvement. The overall induction rate for the institution decreased, and this change has been maintained.     

LXT101及其系列结构修饰物在胰酶体系中的稳定性评价研究

目的 探索系列多肽结构修饰物的功能性基团与抑制酶降解能力之间的关系,以期寻找到能有效抑制蛋白酶对多肽降解的功能基.方法 应用反相高效液相色谱法(RP-HPLC)研究新药LXT101及其结构修饰物LZN系列和LMP系列在胰混合酶体系中的体外代谢性质,检测波长均为225 nm.结果 多肽药物的浓度在4.0~400μg/ml范围内与其峰面积呈良好线性关系(r>0.9990),绝对回收率为95.0%~98.7%,日内相对标准偏差(RSD)<1.5%,日间RSD<2.5%.半衰期为LZN系列>LMP系列>LXT101.结论 LZN和LMP系列达到了结构修饰的目的,即具有质子给体或受体的基团如氨甲酰基(Cbm)、乙酰基(Ac)、对氨基苯丙氨酸(Aph)和对脲基苯丙氨酸(Uph)等的修饰可延长此类多肽化合物的代谢半衰期,为研发长效、高活性的肽类药物提供了重要信息.     

复方消积止咳蜜炼膏的质量标准及初步稳定性考察

目的建立复方消积止咳蜜炼膏的质量标准,并对其初步稳定性进行研究。方法采用薄层色谱（TLC）法对方中陈皮、五味子、山楂进行定性鉴别;采用高效液相色谱法（HPLC）对制剂中细叶远志皂苷进行含量测定。结果复方消积止咳蜜炼膏中陈皮、五味子、山楂薄层色谱斑点清晰、分离度好、专属性强;细叶远志皂苷在进样浓度0.02～0.20 mg/mL范围内与峰面积积分值呈良好线性关系,线性方程为Y=4.057×10^3X-6.008×10^4（r=0.999）。平均回收率为100.24%,RSD=2.04%（n=9）。初步稳定性试验表明制剂质量稳定。结论本方法简便易行,适合用于复方消积止咳蜜炼膏的质量控制。     

The effectiveness of interventions using electronic reminders to improve adherence to chronic medication: a systematic review of the literature

Background

Many patients experience difficulties in adhering to long-term treatment. Although patients'' reasons for not being adherent are diverse, one of the most commonly reported barriers is forgetfulness. Reminding patients to take their medication may provide a solution. Electronic reminders (automatically sent reminders without personal contact between the healthcare provider and patient) are now increasingly being used in the effort to improve adherence.

Objective

To examine the effectiveness of interventions using electronic reminders in improving patients'' adherence to chronic medication.

Methods

A comprehensive literature search was conducted in PubMed, Embase, PsycINFO, CINAHL and Cochrane Central Register of Controlled Trials. Electronic searches were supplemented by manual searching of reference lists and reviews. Two reviewers independently screened all citations. Full text was obtained from selected citations and screened for final inclusion. The methodological quality of studies was assessed.

Results

Thirteen studies met the inclusion criteria. Four studies evaluated short message service (SMS) reminders, seven audiovisual reminders from electronic reminder devices (ERD), and two pager messages. Best evidence synthesis revealed evidence for the effectiveness of electronic reminders, provided by eight (four high, four low quality) studies showing significant effects on patients'' adherence, seven of which measured short-term effects (follow-up period <6 months). Improved adherence was found in all but one study using SMS reminders, four studies using ERD and one pager intervention. In addition, one high quality study using an ERD found subgroup effects.

Conclusion

This review provides evidence for the short-term effectiveness of electronic reminders, especially SMS reminders. However, long-term effects remain unclear.     

Progress in studies on the role of gamma-aminobutyric acid type A receptor in convulsion: a short review

Convulsion is the medical condition where body muscles contract and relax rapidly and repeatedly, resulting in an uncontrolled shaking of the body. The impaired inhibition of electrical activity in the brain is one of leading causes of convulsion. γ-aminobutyric acid (GABA) is the chief inhibitory neurotransmitter in the mammalian central nervous system (CNS). GABA acts at inhibitory synapses in the brain by binding to specific transmembrane receptors in the plasma membrane of both pre- and post-synaptic neuronal processes. GABA_A receptor (GABA_AR) is the most important inhibitory receptor, and is the target receptor of anticonvulsant drugs in the clinic. In this review, we describe GABAergic signaling mediated by GABA_AR, the mechanisms of GABA_AR and their expression, and the progress being made on understanding the role of GABA_AR in convulsion with emphasis on the association between GABA_AR mutations or GABA_AR subunit expression and convulsion. We also describe progress of anticonvulsant drugs based on the GABA_AR.