中药提取物产业化初探

对以国际市场为主要目标市场的中药提取物产业化的背景、生产经营现状、有关政策法规、技术基础、市场前景以及中药提取物产业化的意义等方面进行探讨。     

2-异丁基苹果酸葡萄糖氧基苄酯类对照提取物在白及质量控制中的应用研究

目的 建立以2-异丁基苹果酸葡萄糖氧基苄酯类对照提取物为对照的白及质量控制方法。方法 采用ZORBAX Eclipse Plus C₁₈(100 mm×2.1 mm,1.8μm)色谱柱,流动相为0.05%磷酸水溶液(A)-乙腈(B),梯度洗脱,柱温35℃,体积流量0.15 mL/min,进样体积为2μL,检测波长为220 nm。分别采用对照品法和对照提取物法测定17批白及饮片中1,4-二[4-(葡萄糖氧)苄基]-2-异丁基苹果酸酯-2-葡萄糖苷(2-O-葡萄糖基白及苷)、1-[4-(葡萄糖氧)苄基]-2-异丁基苹果酸酯(手参苷Ⅰ)、1,4-二[4-(葡萄糖氧)苄基]-2-异丁基苹果酸-2-(6-O-乙酰基)葡萄糖苷(手参苷Ⅲ)、1,4-二[4-(葡萄糖氧)苄基]-2-异丁基苹果酸酯(白及苷)4个成分的含量,并进行比较。结果 2-异丁基苹果酸葡萄糖氧基苄酯类对照提取物中2-O-葡萄糖基白及苷、手参苷Ⅰ、手参苷Ⅲ、白及苷线性关系良好(r≥0.999 9),进样精密度RSD值在0.001%～0.58%,重复性RSD值在0.27%～0.53%,4种成分的加样回收率在98....     

表面改性与致孔对干姜醇提物压片关键性能改善的研究

目的 以干姜Zingiberis Rhizoma醇提物为研究对象,研究表面改性、聚集与致孔相结合的共处理方式改善干姜醇提物的压片关键性能。方法 以共聚维酮（plasdone S-630,PVP/VA）和碳酸氢铵分别为改性剂和致孔剂,采用喷雾干燥共处理方法制备不同比例的干姜醇提物改性复合粉体,测定并比较各粉体的密度、流动性、粒径、孔隙率和压缩性等粉体学性质和抗张强度、屈服压、功和能等相关压片性质,并采用扫描电子显微镜（SEM）对各粒子表面形态进行表征。结果 仅加入共聚维酮或碳酸氢铵制备的复合粒子的孔隙率、抗张强度（TS）、有效功（Esp）和能（E2）均优于原粉粒子。此外,相比于碳酸氢铵或共聚维酮单独制备的复合粒子,碳酸氢铵-共聚维酮（7.0%、14.0%、21.0%）共喷雾制备的复合粒子所压制片剂的抗张强度进一步提升：分别为（1）3.8～9.7、4.0～12.5、4.2～13.7倍和（2）1.5～2.1、1.3～2.2、1.2～1.8倍。即同时加入共聚维酮和碳酸氢铵制备的多孔复合粒子使上述性质得到进一步改善。另外,崩解时间会随共聚维酮加入而有所延长（9～14 min）,碳酸氢铵的致孔作用...     

基于网络药理学与动物实验探究桂花醇提物对慢性脑缺血神经损伤的保护作用及机制

目的 基于磷脂酰肌醇3-激酶（phosphatidylinositol 3-kinase,PI3K）/蛋白激酶B(protein kinase B,Akt)通路探究桂花醇提物抗慢性脑缺血性神经损伤的保护作用与机制。方法 借助文献检索、TCMSP、BATMAN数据库筛选桂花活性成分及靶点;OMIM、GeneCards疾病数据库检索疾病靶点。取交集靶点构建蛋白质-蛋白质相互作用（protein-protein interaction,PPI）网络。借助DAVID数据库进行基因本体（gene ontology,GO）功能和京都基因和基因组百科全书（Kyoto encyclopedia of genes and genomes,KEGG）通路富集分析,并建立“成分-靶点-通路”网络。采用右侧颈总动脉结扎法建立慢性脑缺血小鼠模型,随机分为假手术组、模型组、脑络通（195 mg/kg）组和桂花醇提物低、高剂量（125、375 mg/kg）组。采用旷场实验评价各组小鼠自发能力及探索行为;检测各组小鼠海马组织胆碱乙酰化酶（choline acetylase,ChAC）和胆碱酯酶（cholinester...     

Immune adjuvants for chemotherapy or radiotherapy in the 9L rat brain tumor model

Summary The therapeutic efficacy and toxicity of three biological response modifiers,Corynebacterium parvum (Cp), Chinese blister beetle extract (CBBE), recombinant human IL-1 (rhIL-1), used alone or in combination with chemotherapy or radiotherapy, were investigated in the intracerebral (ic) rat 9L brain tumor model. Used alone, Cp (2mg/rat, ip plus 70g/rat, ic), CBBE (5l of an ethanol extract, ic), or IL-1 (lg/rat, ic or 1g/rat × 3, q 3 d, ic), had no effect on animal survival compared to the untreated or saline treated controls. When combined with chemotherapy or radiotherapy, the three immunotherapeutic agents did not show any additive effects on survival compared to that observed with systemic BCNU (12mg/kg), local ic bleomycin (0.25 unit), or local radiotherapy (16 Gy). While ic IL-1 did not produce evident toxicity, there was fatal toxicity caused by ic Cp or CBBE treatment in a few animals. The combination of Cp and bleomycin produced severe neurotoxicity, resulting in the early death of animals. This study demonstrates a lack of efficacy of the nonspecific immune adjuvants IL-1, Cp or CBBE, used either alone or combined with cytotoxic chemotherapy or radiotherapy, in this rat brain tumor model.     

Differential Effects of Anionic,Cationic, Nonionic,and Physiologic Surfactants on the Dissociation, α-Chymotryptic Degradation,and Enteral Absorption of Insulin Hexamers

Various surfactants were investigated to compare their effects on insulin dissociation, -chymotryptic degradation, and rat enteral absorption. With a circular dichroism technique, sodium dodecyl sulfate (SDS) at a 5 mM concentration was found to completely dissociate procine-zinc insulin hexamers (0.5 mg/ml) into monomers. The catalytic activity of -chymotrypsin (0.5 µM) was also abolished by 5 mM SDS. When insulin was injected into the distal jejunum/ proximal ileum segment of the rat, 5 mM SDS greatly enhanced its pharmacological availability, from a negligible value to 2.8%. Being a cationic surfactant, hexadecyl trimethylammonium bromide (CTAB) also efficiently dissociated insulin hexamers at concentrations of 1–5 mM. However, extensive charge–charge interaction was observed below a CTAB concentration of 0.6 mM, leading to insulin precipitation at a molar CTAB:insulin ratio of 1:1 to 2:1. An -chymotryptic degradation study also revealed near-complete dissociation of insulin hexamers at 1 mM CTAB. Above 1 mM, however, CTAB acted as an enzyme inhibitor, most likely by means of charge repulsion. Enteral absorption studies showed a much lower pharmacological availability, only 0.29%. Nonionic surfactants such as Tween 80 and polyoxyethylene 9 lauryl ether were ineffective in dissociating insulin hexamers. Tween 80, at 5 mM, neither significantly altered the -chymotryptic degradation pattern nor enhanced the enteral absorption of insulin. The relative effectiveness of different species of bile salts on insulin hexamer dissociation appeared to be similar. Sodium glycocholate at a 30 mM concentration also significantly increased insulin pharmacological availability, to 2.3%. A morphological study did not reveal any significant alteration of the rat intestinal mucosal integrity after exposure to 5 mM SDS for 30 min. The results further emphasize the importance of the degree of insulin aggregation on its enteral transport.     

水蛭提取物对大鼠脑血栓后脑组织MDA，SOD和NO含量的影响

目的　探讨光化学法诱导大鼠脑血栓形成中丙二醛(MDA) ,NO和 SOD含量的变化及水蛭提取物 (EFH )对其脑组织保护作用的机理 .方法　采用光化学法诱导大鼠大脑中动脉 (MCA)脑血栓形成模型 ,观察脑缺血后及药物作用后 4h,2 4h脑组织匀浆中 MDA,SOD和 NO的含量变化 .结果　大鼠脑缺血后 4h时 MDA的含量增高 ,2 4h明显增高 ;2 4h时 EFH治疗组 MDA含量明显降低 ,由 (4 .77± 0 .2 4) mol·L- 1降为 (2 .5 1± 0 .44 ) mol· L- 1 (P<0 .0 5 ) ,与模型组相比2 4h时 SOD的活性明显增高 (P<0 .0 5 ) . NO含量在脑缺血后 4h降低 ,2 4h时与假手术组相比明显升高 (P<0 .0 1) .结论　光化学诱导大鼠脑血栓形成 ,其脑组织的损伤与 MDA及 NO的神经细胞毒性作用有关 ,EFH可清除 MDA的生成 ,减少 SOD消耗 ,降低 NO的毒性 ,对缺血脑组织有保护作用     

普鲁布考等药物对溶血磷脂酰胆碱引起的牛脑基底动脉条收缩的影响

目的 :研究溶血磷脂酰胆碱 (L PC)对牛脑基底动脉条收缩的影响及普罗布考等药物的保护作用。方法 :通过描记基底动脉条的张力变化 ,测定 L PC对基底动脉条收缩的影响。结果 :L PC能剂量依赖性 (1× 10 - 9～ 1× 10 - 5 mol/ L )促进基底动脉条收缩 ,在 1× 10 - 5 mol/ L时 ,收缩达最大 ,为 (15 1.0± 18.4) %。当用 Triton X- 10 0 (0 .1% )破坏血管内皮层后 ,L PC诱导的血管收缩作用消失。银杏叶提取物 (EGb)、普罗布考 (Pro)和维生素 E(Vit E)能剂量依赖性地减弱 L PC诱导的牛脑基底动脉条收缩。 结论 :药物 EGb,Pro和 Vit E能拮抗 L PC诱导的牛脑基底动脉条收缩。     

正交试验法优选银翘解毒软胶囊的水煮提取工艺

采用Ｌ９（３＾４）正交设计,以浸膏得率,正丁醇浸出率,绿原酸含量为考察指标,优选银翘解毒软胶囊的水煮提取工艺。结果表明：最佳提取工艺为首次加１０倍量水,浸泡３０ｍｉｎ,煎煮２ｈ,第２次加８倍量水,煎煮１．５ｈ。     

石化催化作业工人神经行为功能的调查

（１）目的 探讨石化催化作业对工人神经行为功能的影响。（２）方法 采用ＷＨＯ推荐的神经行为功能测试方法对４０名作业工人（接触组）进行了测定,并与４０名非职业性有害因素作业的工人（对照组）进行了比较。（３）结果 接触组工人情感状态问卷的疲惫－惰性及困惑－迷茫的分数高于对照组,差异有显著性（Ｆ＝４．７８,６．９７,Ｐ〈０．０５）,接触组数字跨度测试的倒序,手提转捷度,数字译码,目标追踪的正确打点数和总