膜控型微丸制剂的研究进展

从膜控型微丸削剂的特点、所用材料及调节药物释放的方法等方面介绍膜控型微丸制剂的研究进展.普通缓释微丸、脉冲微丸、肠溶微丸及结肠靶向微丸等膜控型微丸制剂具有广阔的发展前景,其释药机制仍有待于进一步深入研究.     

胃肠道微生态及微生态制剂在治疗胃肠道疾病中的应用

目的对胃肠道微生态及微生态制剂在治疗胃肠道疾病中的应用进行综述,提示临床医师注意微生态制剂的临床应用。方法采用文献查阅法,对有关胃肠道微生态及有关微生态制剂在治疗胃肠道疾病中的应用的文献进行综合、整理。结果胃肠道内环境微生态正常情况处于动态平衡状态,微生态制剂可以纠正胃肠道微生态失调,治疗胃肠道疾病。结论微生态制剂在治疗胃肠道疾病中具有一定作用。     

微透析技术在体内药物分析中的应用

论述微透析技术在体内药物分析中的应用研究，着重介绍微透析系统的基本结构与操作步骤、微透析技术用于定量分析及影响回收率的因素以及微透析技术与其他技术的联用。     

微生态制剂进展与应用中的药学监护

微生态制剂(probioties,microecologics)亦称微生态调节剂(microecological modulator),包括益生菌(probiotics)、益生元(prebiotics)、合生元(snybiotics),是针对广谱抗生素大量应用后所致的菌群紊乱,在微生态理论指导下,调整胃肠道、阴道微生态菌群失调,保持微生态环境平衡,提高机体健康水平或增     

微生态调节剂在儿科的临床应用

广谱抗菌药物在临床的广泛应用引起了菌群失调与耐药性的出现,从而推动了微生态学的发展。近年来,微生态调节剂在临床的应用范围日益扩大。本文综述了微生态调节剂在儿科的应用。     

微丸压片技术的研究进展

口服缓、控释多单元制剂因其多方面的优点在药剂学领域中的应用日益广泛。其中,由微丸亚单元压制成的微丸型片兼有缓、控释和多单元制剂的优点。本文就近年来国内外微丸压片技术的研究进展进行综述,归纳和总结了微丸压片的机制、辅料和工艺参数对多单元微丸系统压片性能的影响,并展望了膜控微丸压片技术的发展前景。     

自微乳释药系统研究进展

简要介绍了自微乳释药系统的组成、体外释药研究方法及自微乳新型制剂的研究进展.自微乳新型制剂主要包括固体自微乳、过饱和自微乳和正电荷自微乳,新型自微乳制剂可以弥补其不足,更好地发挥自微乳固有特点.     

微透析取样技术及其在药代动力学中的应用

本文综述了近年来国外有关微透析取样技术在药代动力学中的应用，介绍了微透析取样技术的原理、组成以及微透析探针的类型，重点介绍了在体微透析取样技术在动物和人药代动力学中的应用。表明微透析取样技术在药代动力学中的应用具有广阔的前景。     

微乳及自微乳给药系统的药学应用进展

目的介绍微乳及自微乳给药系统的最新进展及在药学研究方面的应用。方法查阅国内外文献资料进行整理和归纳。结果微乳及自微乳给药不仅能改善难溶于水、油溶性药物的溶解性,也可以保护不稳定的药物,控制药物的释放,它可以用于多种给药途径。结论此类给药系统是非常有前景的给药系统。     

葛根素固体自微乳制剂的制备及其质量评价

目的:制备葛根素固体自微乳制剂,并评价其质量。方法:通过改变处方组成、稀释倍数、介质、温度等考察影响自微乳化效率和粒径大小的因素,采用激光粒度分析仪测定成乳后粒径,并通过透射电镜对成乳后的微乳进行形态学观察;通过3个月的加速试验考察葛根素固体自微乳的稳定性。结果:处方组成、温度等因素对自微乳化效率和粒径大小都有影响;稀释倍数、分散介质等在一定范围内影响不大。葛根素固体自微乳成乳后为圆球形,平均粒径为30nm。结论:葛根素固体自微乳粒径小,稳定性好。     

Interindividual variability in metabolic activation in humans in vivo

In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.     

Theophylline kinetics in peripheral tissues in vivo in humans

Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (c_max, t_max, AUC) were calculated for plasma and tissue time courses. The mean AUC_tissue /AUC_plasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - t_max Time to peak concentration - c_max Peak concentration     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

纳米材料在止血方面的研究进展

纳米材料因其独特的微观结构优势,已被广泛应用于材料制备、微电子与计算机技术、医学与健康、环境与能源等领域。与传统止血材料相比,纳米材料在一定程度上能提高传统止血药物的生物利用度和稳定性,增强药物的缓控与靶向释放,为现代化新型止血材料的发展奠定了良好的基础。对脂质体、纳米粒、自组装纳米肽、纳米纤维等多种纳米止血材料的前沿设计和应用进展进行了综述,最后简述纳米止血材料存在的问题和发展前景。     

Genotoxic effects of chlorophenoxy herbicide diclofop-methyl in mice in vivo and in human lymphocytes in vitro

Diclofop-methyl (DM) is a chlorophenoxy derivative used in large quantities for the control of annual grasses in grain and vegetable crops. In this study, the genotoxic effects of DM were investigated by measuring chromosomal aberrations (CAs) in mouse bone-marrow cells and CA and the comet assay in human peripheral lymphocytes. Mice were treated with 15.63, 31.25, 62.5, and 125?mg/kg body weight of DM intraperitoneally for 24 hours, and 15.63-, 31.25-, 62.5-, 125-, and 250-µg/mL concentrations were applied to human lymphocytes for both 24 and 48 hours. In in vivo treatments, DM significantly, but not dose dependently, increased the total chromosome aberrations, compared to both negative and solvent controls. Cell proliferation was significantly, but not dose dependently, affected by all doses. In in vitro treatments, DM (except 15.63 µg/mL) significantly and dose dependently increased the frequency of chromosome aberrations. Also, 250 µg/mL of 48-hour treatment was found to be toxic. Cell proliferation was significantly and dose dependently affected by DM applications, when compared to negative control. In in vitro treatments, DM significantly decreased the mitotic index only at the highest concentration for 24 hours, and 62.5- and 125-µg/mL concentrations for 48 hours. In the comet assay, a significant and dose-dependent increase in comet-tail intensity was observed at 62.5-, 125-, and 250-µg/mL concentrations. The mean comet-tail length was significantly increased in all concentrations. Our results demonstrate that DM is genotoxic in mammalian cells in vivo and in vitro.     

Polymorphisms in genes involved in neurotransmission in relation to smoking

Smoking behavior is influenced by both genetic and environmental factors. The genetic contribution to smoking behavior is at least as great as its contribution to alcoholism. Much progress has been achieved in genomic research related to cigarette-smoking within recent years. Linkage studies indicate that there are several loci linked to smoking, and candidate genes that are related to neurotransmission have been examined. Possible associated genes include cytochrome P450 subfamily polypeptide 6 (CYP2A6), dopamine D₁, D₂, and D₄ receptors, dopamine transporter, and serotonin transporter genes. There are other important candidate genes but studies evaluating the link with smoking have not been reported. These include genes encoding the dopamine D₃ and D₅ receptors, serotonin receptors, tyrosine hydroxylase, trytophan 2,3-dioxygenase, opioid receptors, and cannabinoid receptors. Since smoking-related factors are extremely complex, studies of diverse populations and of many aspects of smoking behavior including initiation, maintenance, cessation, relapse, and influence of environmental factors are needed to identify smoking-associated genes. We now review genetic polymorphisms reported to be involved in neurotransmission in relation to smoking.     

Enteroviral meningitis in children in Turkey

In the indexed medical literature, there have been a very limited number of studies to investigate the epidemiologic and clinical features of enteroviral meningitis in Turkey. The aim of the present retrospective study is to update the actual situation to recognize the spectrum and magnitude of this important clinical entity. Between June 1999 and December 2004, 612 cases of aseptic meningitis were followed up at our hospital. Enteroviral meningitis was defined by isolation of enteroviruses from cerebrospinal fluid (CSF) and/or stool samples. Mumps virus was detected in 310 cases (50.7%) and enteroviruses were the etiologic agents in 104 (17%) of the patients with aseptic meningitis. Most of the enteroviral meningitis cases (36 cases, 34.6%) were diagnosed in August and 70 (67.3%) of them were male. The mean age was 5.6 ± 3.4 years. The most common initial symptoms were fever (81.7%), vomiting (77.9%) and headache (57.7%). In the physical examination, 46.2% of the cases had neck stiffness and 38.5% had pharyngitis. Echovirus 30 was the most frequently (38 cases, 36.5%) isolated enterovirus with peaks in 1999, 2002 and 2004. The other frequently isolated enteroviruses were Coxsackie virus type B (17 cases, 16.3%), echovirus 6 (11 cases, 10.6%), echovirus 11 (6 cases, 5.8%), and echovirus 13 (4 cases, 3.8 %). Mean hospitalization time was 6.2 ± 2.4 days. All patients recovered without any sequelae. Enteroviruses have an important role in childhood aseptic meningitis cases in Turkey too, and the predominant serotypes vary according to years.     

我院2004年门急诊处方及抗菌药物合理应用分析

目的了解我院抗菌药物使用状况,为临床合理用药提供参考依据。方法随机抽取2004年门急诊处方样本2444份,依据统计学方法归纳制表并进行综合分析。结果2004年门急诊每张处方药品数平均为3.24种;注射给药处方数占西药总处方数的33.43%,高于北京三甲医院水平(约10%);抗菌药物使用率为43.54%,高于上海、武汉等城市水平(约35%);一线抗菌药物使用率为70.56%,二线抗菌药物使用率为29.37%,抗菌药物分级使用状况总体符合规定;抗菌药物联合用药比率为26.22%,单一用药比率达73.78%,属基本合理范围。结论我院抗菌药用药以一线抗菌药物为主,合理用药是主流,但也存在一定问题,宜制定相应措施,提高用药合理性和安全性。     

2010调脂治疗领域进展

2010年在调脂治疗领域针对他汀治疗心血管病的防治又进行了许多探索。本文通过综述他汀类药物的国际大规模临床试验结果,重新评价了他汀类药物在冠心病一级预防和冠心病二级预防中的地位,阐明了强化他汀治疗的意义;对他汀的心肾保护作用和安全性新证据进行了说明。     

Disease control in asthmatic children seen in private practice in Switzerland

ABSTRACT

Background: Asthma is the most common chronic childhood disease in Switzerland with a prevalence of 10%. Asthma has a high economic burden accounting for high medical costs. Assessment of disease control is likely to be of help in the implementation of strategies to improve asthma. Therefore, we aimed to evaluate asthma control and therapy regimens among children in private practice.

Methods: We assessed asthma control as well as therapy regimens in 575 asthmatic children in an experience programme in Switzerland by using an abbreviated questionnaire based on the asthma control questionnaire and the child health questionnaire on Visit 1 and Visit 2.

Results: Good asthma control at Visit 1 was only present in 25.7% of asthmatic children. Occasional asthma symptoms, limitation of physical activity, nocturnal awakening and anxiety of the parent was present in 80.5%, 41.2%, 46.8% and 57% of the children, respectively. After adjustment of therapy regimens at Visit 1, mainly by adding a leukotriene receptor antagonist, asthma control was reported to be much better in 53.4% of the children at Visit 2.

Conclusions: As asthma control is inadequately achieved within a major portion of asthmatic children, it is imperative to find measures to improve asthma control and hence, to reduce the burden of disease.