宣肺止咳糖浆质量标准研究

本文对分离煎煮醇沉法制备的宣肺止咳糖浆中主药的有效成分作了检测，初步确定了其质量控制标准。利用麻黄碱与氨水碱化的ＣｕＳＯ４－ＣＳ２试液作用在氯仿溶液中显黄色反应的性质和离心沉淀丙酮溶液洗涤法分离黄芩甙作分光光度法测定含量的方法，检测宣肺止咳糖浆样品４批。根据实验结果确立的质量标准为：成品呈棕褐色澄明液体，气香、气香、味甜、微苦、久置有少量沉淀，比重１．２左右，ｐＨ在３．５￣４．０之间，含糖量为７５     

基于药效筛选和正交试验优选小儿牛蒡子止咳糖浆的制备工艺

摘要：目的:通过药效实验优选小儿牛蒡子止咳糖浆的工艺路线,并采用正交试验进行优化,确定最优制备工艺。方法:通过止咳作用的药效实验,筛选拟定的小儿牛蒡子止咳糖浆A（提油+水提+醇沉）、B（水提+醇沉）、C（提油+水提）这3种制备工艺。再以出油量、出膏率和牛蒡苷含量测定结果为指标,通过正交试验优化提取工艺参数。结果:药效实验结果表明,工艺路线A和工艺路线C制得的小儿牛蒡子止咳糖浆对小鼠止咳具有一定作用。综合考虑,工艺A样品药效作用最强,且灌胃服用量较小,故选择工艺A作为本方糖浆剂工艺,并通过正交试验优化工艺A的最合理的工艺参数。结论:小儿牛蒡子止咳糖浆对小鼠模型有明显的止咳作用,优选的制备工艺方法稳定可行,为小儿牛蒡子止咳糖浆的后续研发提供依据。     

陶瓷膜微滤技术精制鼻炎糖浆的效果评价

目的：对陶瓷膜错流微滤技术精制鼻炎糖浆的效果进行评价。方法：采用陶瓷膜错流微滤技术对鼻炎糖浆水提液进行除杂处理，并建立鼻炎糖浆的黄芩苷、盐酸麻黄碱的含量检测方法，以鉴别、含量等指标与原工艺进行对比。结果：用错流微滤法制备的鼻炎糖浆澄明度和口感好于原工艺，两种制法的样品鉴别均合格，盐酸麻黄碱含量一致，黄芩苷含量微滤工艺大大高于原工艺。结论：陶瓷膜错流微滤技术适于鼻炎糖浆的精制。     

宣肺止咳颗粒的水提醇沉工艺考察

摘 要 目的：优选宣肺止咳颗粒的水提醇沉工艺。方法: 以橙皮苷量、射干苷量和干膏得率的综合评分为指标,通过正交试验,考察加水量、煎煮时间、煎煮次数对水提工艺的影响,考察相对密度、醇沉浓度、醇沉时间对醇沉工艺的影响。结果:优选的水提工艺为首次加10倍量水煎煮1.5 h,第2,3次分别加8倍量水煎煮0.5 h;优选的醇沉工艺为水提液浓缩至相对密度1.05（60 ℃）,醇沉至乙醇体积分数80%,冷处静置18 h。结论:优选的提取、 醇沉工艺稳定可行,为宣肺止咳颗粒的规范化生产提供参考。     

不同煎煮方法对半夏泻心汤质量的影响

摘要：目的:探讨不同煎煮方法对半夏泻心汤中盐酸小檗碱、黄芩苷、甘草苷及甘草酸铵的含量的影响。方法:按半夏泻心汤处方量,一法遵循传统的记载,去滓再煎（Ⅰ法）制备标准汤液,另法直接合煎（Ⅱ法）制备成标准汤液。用HPLC法分别测定两种方法制备的汤液的出膏率、浸出物含量,以及黄芩苷、盐酸小檗碱、甘草苷、甘草酸铵等成分含量。结果:Ⅰ法汤液的出膏率、浸出物含量明显低于Ⅱ法汤液（P<0.01）,Ⅰ法汤液黄芩苷、盐酸小檗碱、甘草苷、甘草酸铵含量均明显高于Ⅱ法汤液（P<0.01）。结论:两种煎煮方法所得的半夏泻心汤质量存在差异,但由于出膏率和浸出物含量不完全等同于汤液中有效成分含量的提取程度,故以黄芩苷、盐酸小檗碱、甘草苷、甘草酸铵含量为评价指标,半夏泻心汤原方记载煎煮方法更为科学。     

HPLC法测定桉叶止咳糖浆中黄芩苷与麻黄碱的含量

目的建立HPLC法测定桉叶止咳糖浆中黄芩苷与麻黄碱的含量。方法黄芩苷采用PE-Rack C18（5umm,150mm×4.6mm）色谱柱,以0.1%磷酸溶液-甲醇（58：42）为流动相,流速为1.0ml.min-1,检测波长为277nm,柱温为30℃。麻黄碱采用Diamonsil C18（5μm,250×4.6mm）色谱柱,以0.1%磷酸溶液（含0.1%三乙胺）-乙腈（97：3）为流动相,流速为1.0mL.min-1,检测波长为205nm,柱温为25℃。结果黄芩苷在2.8～90μg.ml-1范围内呈良好的线性关系（R2=0.9998）,平均回收率为99.1%,RSD=1.72%（n=6）;麻黄碱在0.1513～2.0716μg范围内线性关系良好（R2=1.0000）,平均回收率为99.43%,RSD=1.10%（n=6）。结论结果表明本方法测定桉叶止咳糖浆中黄芩苷与麻黄碱的含量灵敏度高,操作简便、准确,重现性好。     

醒脑益智颗粒水提醇沉制备工艺研究

目的：研究醒脑益智颗粒的水提醇沉制备工艺。方法：以阿魏酸含量为考察指标，通过L9（3^4）正交试验设计优选水提醇沉的制备工艺条件，确定醒脑益智颗粒的最佳制备工艺。结果：水提醇沉制备工艺影响因素依次为：加水量（A）〉煎煮次数（C）〉醇沉质量分数（D）〉煎煮时间（B），最佳制备工艺条件为A3B1C3D2，即处方药材加10倍量水，煎煮3次，每次0．5h，醇沉质量分数为50％。结论：该制备工艺合理，有效成分提取率高。     

正交试验优选重连口服液的提取工艺

目的优选重连口服液最佳提取工艺。方法水提取工艺以浸膏得率、重楼皂苷、Ⅰ和连翘苷的含量为考察指标,醇沉工艺以重楼皂苷Ⅰ和连翘苷的含量为考察指标,分别采用正交试验法对其提取工艺条件进行优选。结果重连口服液水提最佳工艺条件为加水煎煮3次,每次10倍量水,煎煮1h,醇沉最佳工艺条件为浓缩至相对密度1．10（80℃热测）,加乙醇使药液乙醇浓度达到80％,静置24h。结论优选的提取工艺合理,稳定性好,可为工业生产提供理论依据。     

HPLC法同时测定宣肺止咳糖浆中盐酸麻黄碱和苦杏仁苷的含量

目的：建立高效液相色谱法同时测定宣肺止咳糖浆中盐酸麻黄碱和苦杏仁苷含量的方法.方法：采用Luna C18柱（250 mm×4.6 mm,5 μn）,乙腈-0.1%磷酸溶液（加入0.1%三乙胺）（10：90）为流动相,流速1.0 ml·min-1,检测波长210 nm,柱温30℃.结果：盐酸麻黄碱在2.2～111.5μg·ml-1的范围内有良好的线性关系,r=0.999 6,平均回收率为96.4%,RSD为1.34%（n=9） 苦杏仁苷在20.4～1 020.0μg·ml-1范围内有良好线性关系,r=0.999 9,平均回收率为99.0%,RSD为0.50%（n=9）.结论：方法可同时测定盐酸麻黄碱和苦杏仁苷的含量,简便,准确,重复性好,可作为宣肺止咳糖浆的质量控制.     

补肾壮骨胶囊提取工艺的优选

目的：优选补肾壮骨胶囊提取工艺的最佳条件。方法：用正交设计法以方中君药淫羊藿药材的主要成分淫羊藿苷的总量为指标，对其水煎工艺及醇沉工艺进行筛选。结果：优选出补肾壮骨胶囊水煎醇沉工艺，重复试验结果满意。结论：补肾壮骨胶囊水煎工艺的最佳条件为A2B3C2D2，即加12倍量水先浸泡40min，再煎煮2次，每次煎煮90min。醇沉工艺的最佳条件为A282Dl，即浓缩药液比例至1：1(药液：药材量)后醇沉(55％乙醇醇沉)12h。     

Synthesis,Cytotoxicity and Antileishmanial Activity of Some N-(2-(indol-3-yl)ethyl)-7-chloroquinolin-4-amines

We report herein the condensation of 4,7-dichloroquinoline (1) with tryptamine (2) and D-tryptophan methyl ester (3) . Hydrolysis of the methyl ester adduct (5) yielded the free acid (6) . The compounds were evaluated in vitro for activity against four different species of Leishmania promastigote forms and for cytotoxic activity against Kb and Vero cells. Compound (5) showed good activity against the Leishmania species tested, while all three compounds displayed moderate activity in both Kb and Vero cells.     

Efficacy of gut lavage,hemodialysis, and hemoperfusion in the therapy of paraquat or diquat intoxication

Clinical and in vitro investigations were carried out to test the efficacy of gut lavage, hemodialysis, and hemoperfusion in the treatment of poisoning with paraquat or diquat. In a patient suffering from diquat intoxication 130 times more diquat was removed by gut lavage 30 h after ingestion than was removed by complete aspiration of the gastric contents.Determination of in vitro clearances for paraquat and diquat by hemodialysis showed that, at serum concentrations of 1–2 ppm, such as are frequently encountered in poisoning in man, toxicologically relevant quantities of herbicide cannot be removed from the body. At a concentration of 20 ppm, on the other hand, hemodialysis proved to be effective, the clearance being 70 ml/min at a blood flow rate of 100 ml/min. The efficacy of hemoperfusion with coated activated charcoal was on the whole better. Especially at concentrations around 1–2 ppm, the clearance values for hemoperfusion were some 5–7 times higher than those for hemodialysis.In a patient suffering from paraquat poisoning, both hemodialysis as well as hemoperfusion were carried out. The in vitro results could be confirmed: At serum concentrations of paraquat less than 1 ppm no clearance could be obtained by hemodialysis while by hemoperfusion with activated charcoal quite high clearance values were measured and the serum level dropped down to zero.

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Zusammenfassung Klinische Untersuchungen und Laboratoriumsversuche wurden durchgeführt, um die Wirksamkeit von Darmspülung, Hämodialyse und Hämoperfusion bei Paraquat- und Deiquat-Vergiftungen zu prüfen.Bei einem Patienten wurde 30 Std nach Deiquat-Aufnahme durch Darmspülung 130mal mehr Deiquat entfernt als durch vollständige Aspiration des Mageninhaltes. In vitro-Versuche ergaben, daß bei Blutserumkonzentrationen von 1–2 ppm, die bei Vergiftungen oft gemessen werden, durch Hämodialyse keine toxikologisch relevanten Paraquat- oder Deiquat-Mengen entfernt werden können. Dagegen erwies sich die Hämodialyse bei 20 ppm und einer Blutumlaufgeschwindigkeit von 100 ml/min mit einer Clearance von 70 ml/min als wirksam. Die Hämoperfusion mit beschicheter Aktivkohle war in diesen Versuchen aber eindeutig überlegen, denn insbesondere bei Konzentrationen um 1–2 ppm waren die Clearance-Werte 5–7mal höher als bei der Hämodialyse.Die in vitro-Ergebnisse wurden bei einem Patienten mit einer Paraquat-Vergiftung bestätigt: Bei Konzentrationen unter 1 ppm war die Hämodialyse wirkungslos, während durch Hämoperfusion relativ hohe Clearance-Werte erreicht wurden, so daß der Serumspiegel rasch unter die Nachweisgrenze abfiel.

     

Lung disease and PKCs

The lung offers a rich opportunity for development of therapeutic strategies focused on isozymes of protein kinase C (PKCs). PKCs are important in many cellular responses in the lung, and existing therapies for pulmonary disorders are inadequate. The lung poses unique challenges as it interfaces with air and blood, contains a pulmonary and systemic circulation, and consists of many cell types. Key structures are bronchial and pulmonary vessels, branching airways, and distal air sacs defined by alveolar walls containing capillaries and interstitial space. The cellular composition of each vessel, airway, and alveolar wall is heterogeneous. Injurious environmental stimuli signal through PKCs and cause a variety of disorders. Edema formation and pulmonary hypertension (PHTN) result from derangements in endothelial, smooth muscle (SM), and/or adventitial fibroblast cell phenotype. Asthma, chronic obstructive pulmonary disease (COPD), and lung cancer are characterized by distinctive pathological changes in airway epithelial, SM, and mucous-generating cells. Acute and chronic pneumonitis and fibrosis occur in the alveolar space and interstitium with type 2 pneumocytes and interstitial fibroblasts/myofibroblasts playing a prominent role. At each site, inflammatory, immune, and vascular progenitor cells contribute to the injury and repair process. Many strategies have been used to investigate PKCs in lung injury. Isolated organ preparations and whole animal studies are powerful approaches especially when genetically engineered mice are used. More analysis of PKC isozymes in normal and diseased human lung tissue and cells is needed to complement this work. Since opposing or counter-regulatory effects of selected PKCs in the same cell or tissue have been found, it may be desirable to target more than one PKC isozyme and potentially in different directions. Because multiple signaling pathways contribute to the key cellular responses important in lung biology, therapeutic strategies targeting PKCs may be more effective if combined with inhibitors of other pathways for additive or synergistic effect. Mechanisms that regulate PKC activity, including phosphorylation and interaction with isozyme-specific binding proteins, are also potential therapeutic targets. Key isotypes of PKC involved in lung pathophysiology are summarized and current and evolving therapeutic approaches to target them are identified.     

In vitro studies on sterically stabilized liposomes (SL) as enzyme carriers in organophosphorus (OP) antagonism

This study describes a new approach for organophosphorous (OP) antidotal treatment by encapsulating an OP hydrolyzing enzyme, OPA anhydrolase (OPAA), within sterically stabilized liposomes. The recombinant OPAA enzyme was derived from Alteromonas strain JD6. It has broad substrate specificity to a wide range of OP compounds: DFP and the nerve agents, soman and sarin. Liposomes encapsulating OPAA (SL)* were made by mechanical dispersion method. Hydrolysis of DFP by (SL)* was measured by following an increase of fluoride ion concentration using a fluoride ion selective electrode. OPAA entrapped in the carrier liposomes rapidly hydrolyze DFP, with the rate of DFP hydrolysis directly proportional to the amount of (SL)* added to the solution. Liposomal carriers containing no enzyme did not hydrolyze DFP. The reaction was linear and the rate of hydrolysis was first order in the substrate. This enzyme carrier system serves as a biodegradable protective environment for the recombinant OP-metabolizing enzyme, OPAA, resulting in prolongation of enzymatic concentration in the body. These studies suggest that the protection of OP intoxication can be strikingly enhanced by adding OPAA encapsulated within (SL)* to pralidoxime and atropine.     

Gender-related symptoms and correlates of alcohol dependence among men and women with a lifetime diagnosis of alcohol use disorders

This study explored gender-related symptoms and correlates of alcohol dependence in a crosssectional study of 150 men and 150 women with a lifetime diagnosis of alcohol use disorders (AUD). Participants were recruited in equal numbers from treatment settings, correctional centres and the general community. Standardized measures were used to determine participants' use of substances, history of psychiatric disorders and psychosocial stress, their sensation seeking and family history of substance use and mental health disorders. Multivariate analyses were used to detect patterns of variables associated with gender and the lifetime severity of AUD. Men had a longer history of severe AUD than women. Women had similar levels of alcohol dependence and medical and psychological sequelae as men, despite 6 fewer years of AUD. More women than men had a history of severe psychosocial stress, severe dependence on other substances and antecedent mental health problems, especially mood and anxiety disorders. There were differences in family history of alcohol-related problems approximating same-gender aggregation. The severity of a lifetime AUD was predicted by its earlier age at onset and the occurrence of other disorders, especially anxiety, among both men and women. The limitations in the generalizability of these findings due to sample idiosyncrasies are discussed.