优选砂仁油滴丸成型工艺

目的优选砂仁油滴丸的成型工艺。方法采用正交设计法,对滴丸制备过程中基质配比、滴管内径、挥发油与基质的比例、冷却温度等因素进行考察。通过测定滴丸重量差异,溶散时限以及对滴丸进行外观评价,气相色谱法测定砂仁油滴丸中主要有效成分乙酸龙脑酯的含量,综合确定其最佳成型工艺。结果最佳成型工艺条件为：选择PEG6000/PEG4000（1∶1）为基质,滴管内径为2.0mm,挥发油与基质配比为（1∶2）,冷却温度为0～5℃（冰水浴中）。结论此工艺制备的砂仁油滴丸,每丸中乙酸龙脑酯含量高、滴丸重量差异、溶散时限以及外观评价各指标均达到或优于中国药典2005年版一部要求。     

甲地孕酮联合EOF方案治疗晚期胃癌的临床观察

目的观察甲地孕酮在治疗晚期胃癌化疗中的辅助治疗效果。方法将64例晚期胃癌患者随机分为治疗组与对照组：EOF方案＋甲地孕酮组（治疗组）33例,单纯EOF方案组（对照组）31例。两组患者均以21d为1个周期,所有患者至少接受2个周期治疗后评价疗效。观察两组患者的客观疗效、生活质量、化疗毒副反应的变化情况及甲地孕酮的不良反应。结果两组患者客观疗效（CR＋PR）分别为51.52%及48.38%,无显著性差异（P〉0.05）;治疗组患者在食欲改善、体重增加和提高KPS评分,以及在保护骨髓功能和减轻消化道反应方面均优于对照组,有显著性差异（P〈0.01）,未见甲地孕酮引起的不良反应。结论甲地孕酮联合EOF方案和单纯EOF方案治疗晚期胃癌的客观疗效无明显差异,但前者副作用小,可作为化疗期间改善生存质量的有效手段。     

醋酸布舍瑞林纳米粒的制备及体外释放特性研究

目的:制备醋酸布舍瑞林纳米粒并考察其体外释药特性。方法:以复乳法制备纳米粒。采用高效液相色谱法测定其含量并计算制剂包封率及载药量,透析袋法考察制剂体外释药特性。结果:所制制剂外观圆整,醋酸布舍瑞林检测浓度的线性范围为0.1～8.0μg·mL-(1r=0.999 9),平均回收率为105.38%,日内RSD<1.78%,日间RSD<0.93%。制剂包封率为(63.37±0.29)%,载药量为(1.03±0.09)%,在pH 7.4的磷酸盐缓冲液中72 h的累积释药百分率为62.35%。结论:该制剂制备工艺简单可行,具有明显的缓释效果。     

Neuronal cytoskeleton and synaptic densities are altered after a chronic treatment with the cannabinoid receptor agonist WIN 55,212-2

Cannabinoid CB1 receptors are the most abundant G-protein-coupled receptors in the brain. Its presynaptic location suggests a role for cannabinoids in modulating the release of neurotransmitters from axon terminals by retrograde signaling. The neuroprotective effects of cannabinoid agonists in animal models of ischemia, seizures, hypoxia, Multiple Sclerosis, Huntington and Parkinson disease have been demonstrated in several reports. The proposed mechanism for the neuroprotection ranges from antioxidant effects, reduction of microglial activation and anti-inflammatory reaction to receptor-mediated reduction of glutamate release. In the present work, we analyzed the morphological changes induced by a chronic treatment with the synthetic cannabinoid receptor agonist, WIN 55,212-2, in four brain regions where the CB1 cannabinoid receptor is present in high density: the CA1 hippocampal area, corpus striatum, cerebellum and frontal cortex. After a twice-daily treatment for 14 days with the cannabinoid receptor agonist (3 mg/kg sc, each dose) to male Wistar rats (150-170 g), the expression of neurofilaments (Nf-160 and Nf-200), microtubule-associated protein-2 (MAP-2), synaptophysin (Syn) and glial fibrillary acidic protein (GFAP) was studied by immunohistochemistry and digital image analysis. Ultrastructural study of the synapses was done using electron microscopy. After the treatment, a significant increase in the expression of neuronal cytoskeletal proteins (Nf-160, Nf-200, MAP-2) was observed, but we did not find changes in the expression of GFAP, the main astroglial cytoskeletal protein. In cerebellum, there was an increase in Syn expression and in the number of synaptic vesicles, while, in the hippocampus, an increase in the Syn expression and in the thickness of the postsynaptic densities was observed. The results obtained from these studies provide evidences on the absence of astroglial reaction and a sprouting phenomena induced by the WIN treatment that might be a key contributor to the long-term neuroprotective effects observed after cannabinoid treatments in different models of central nervous system (CNS) injury reported in the literature.     

A pilot study of hormone modulation as a new treatment for mania in women with bipolar affective disorder

We tested and compared the use of two adjunctive hormonal agents, tamoxifen and medroxyprogesterone acetate (MPA), for the treatment of acute mania or hypomania. A total of 13 women with acute Bipolar Affective Disorder in the manic or hypomanic phase were recruited from a clinical population to participate in this 28-day, three-arm, double blind, placebo-controlled study. The women who received tamoxifen exhibited significant improvement in symptoms of mania from baseline to final assessment compared with the placebo group. The MPA group improved more than the placebo group. Further exploration of tamoxifen as a useful adjunct in the treatment of acute manic symptoms in women with Bipolar Affective Disorder is warranted.     

总序葱臭木茎干的化学成分研究

从总序葱臭木Dysoxylum laxiracemosum茎干分离得到12个化合物,通过波谱分析,化合物结构分别鉴定为sho-reic acid(1),cabraleahydroxylactone(2),cabralealactone(3),cinchonain(4),aurantiamide acetate(5),儿茶素(6),莨菪亭(7),香草酸(8),对羟基苯甲酸(9),1-二十二醇(10),β-谷甾醇(11),胡萝卜苷(12)。其中,化合物1～6,8～12首次从总序葱臭木中分离得到,化合物4～6首次从该属中分离得到。     

达英-35和雌孕激素联合应用治疗青春期功血60例的临床分析

目的：对比达英-35和雌孕激素联合应用治疗青春期功血的临床疗效及再次出血、不良反应情况。方法：对青春期功血患者60例,分两组分别用达英-35和雌孕激素联合应用止血,对比两组止血效果及再次出血、不良反应情况。结果：两组患者治疗效果,完全控制出血的时间差别无统计学意义。止血后两组再次发生出血的情况,达英-35组无此现象,雌孕激素联合应用组6例,经t检验,P〈0.05,差别有统计学意义,不良反应及第一次停药后阴道流血情况达英-35组亦明显少于雌孕激素联合应用治疗组。结论：达英-35治疗青春期功血优于传统的雌孕激素联合应用,此外达英-35服用简单,依从性好,值得临床推广应用。     

反相高效液相梯度洗脱法测定地松磺胺麻黄碱滴鼻液中有效成分含量

 目的 建立同时测定地松磺胺麻黄碱滴鼻液中有效成分含量的反相高效液相梯度洗脱法（reverse-phase high performance liquid chromatography,RP-HPLC）。方法 采用Agilent Eclipse XDB-C18（250 mm×4.6 mm,5 μm）色谱柱,以甲醇（A）-0.1%磷酸水溶液（B）为流动相进行梯度洗脱,梯度洗脱程序为：进样0~10 min,调节流动相A∶B（30∶70,V/V）;10~18 min,流动相A∶B（70∶30,V/V）;18~20 min,流动相A∶B（30∶70,V/V）;流速：1.0 mL/min,检测波长为梯度波长：0~5 min,220 nm;5~8 min,310 nm;8~20 min,240 nm;柱温：30℃,进样量：10 μL。结果 盐酸麻黄碱、磺胺甲噁唑和醋酸地塞米松分别在0.083~0.667 g /L、0.417~3.333 g/L和0.003~0.027 g/ L范围内与峰面积呈良好的线性关系;相关系数分别为：0.999 7、0.999 8和0.999 5;平均回收率分别为：（100.2±1.6）%时RSD为1.61%,（100.4±1.3）%时RSD为1.29%,（99.8±1.4）%时RSD为1.74%。样品中3者平均含量分别为（97.2±3.1）%时RSD为3.06%,（98.6±1.1）%时RSD为1.13%,以及（97.8±1.2）%时RSD为1.23%。结论 该方法简便、快速、专属性强,可用于地松磺胺麻黄碱滴鼻液的质量控制。     

Therapy of multiple sclerosis in children and adolescents

Background

Paediatric multiple sclerosis accounts for up to 10% of all MS cases. The initial course of the disease is relapsing-remitting in most children, with a relapse rate generally higher than that observed in adult patients. There is published experience on the use of first-line disease modifying therapies in children with MS. However, about 1/3 of paediatric MS cases do not respond to IFN-β or glatiramer acetate and continue to develop relapses and disease progression. These patients could be proposed to a second-line treatment.

Methods

A comprehensive review of the published literature related to pharmacologic treatment of MS in adults and paediatric patients was performed. The recent literature has been extracted for new evidence from controlled trials in adult patients, and open treatment studies and reported expert opinion in paediatric patients.

Results

No disease modifying drug has been approved for the treatment of children and adolescents with MS, although the currently available first-line therapies for adults seem to be safe and well tolerated in this population. Further studies are required to assess the safety and efficacy of second-line treatments in children with MS.

Conclusion

The present article constitutes an update of the existing publications regarding treatment of acute events of CNS demyelination in children and adolescents as well as considerations for the use of immunomodulatory therapies.     

Overlapping and distinct mechanisms of action of multiple sclerosis therapies

In the last two decades MS has changed from an idiopathic condition with only symptomatic treatments to a disease with better characterized pathophysiologic underpinnings and several treatments that modify its long-term course based on specific mechanisms of action. There are now several FDA approved options for therapy at the onset of disease, and discussions have begun on choosing the best treatment in individual patients and what option to choose next in patients who are failing their current treatment. Numerous studies have begun to highlight that the underlying pathology of CNS damage may be different in subsets of patients, raising the possibility that some may respond to a treatment with a mechanism of action that is targeted to ‘their’ MS. Trials are ongoing of numerous new agents with different mechanisms of action and some combination therapies. A better understanding of how each therapy works may guide decisions on initiating, combining or changing therapy in a more rational way to improve patient outcomes. Further knowledge of underlying mechanisms of disease in different patients with ‘the same’ disease may lead to more targeted therapies, as will biomarkers that predict clinical response to therapy. Studies of the effects of various agents used in MS reveal both overlapping and distinct mechanisms of actions that may be relevant to their efficacy and side effects in individual patients. However, it is important to remember that most agents are approved based on their reduction of MRI lesions and relapse rates over a short time frame. These measures only partially correlate with long-term disability, which may be the most relevant clinical outcome for people with MS. Fixed disability requires years to become apparent, and there is a lack of large studies of biomarkers for chronic outcomes. In addition, few large studies correlate response to therapy with cognitive outcomes, which are a major cause of chronic disability.