5%声振人血白蛋白空气微球蛋白含量测定

采用高效液相凝胶色谱法（ＧＣ－ＨＰＬＣ）、醋酸纤维膜电泳和半微量定氮法测定５０％声振人血白蛋白空气微球制剂中球壁蛋白的含量。ＧＣ－ＨＰＬＣ确证了球壁蛋白主要成分为人血白蛋白;醋酸纤维膜电泳测定空气人血白蛋白微球制剂中人血白蛋白纯度＞９０％;半微量定氮法测出球壁蛋白含量平均值为３．５６％左右,９９％正常值范围为２．５２％－４．６０％。     

白及微球的研制及其肝动脉栓塞实验研究

用乳化－冷凝技术首次制备出白及微球,并通过正交实验,确定了制备特定粒径微球的最佳工艺条件。对微球的外观、粒径与分布、溶胀度及血液相容性等进行了研究。微球平均粒径为５４．３６μｍ,粒径范围５０～９０μｍ,占总数的７８．３７％;微球在ｐＨ＝７．４的缓冲液中有一定的溶胀性;血液相溶性良好。实验小猪微球栓塞后的肝动脉造影表明白及微球可致肝右动脉一级、二级分支完全栓塞;病理检查表明梗死区可见肝组织呈肝硬化改变,大量的假小叶形成。微球栓塞后,ＧＰＴ有一过性升高,３周后恢复正常。实验结果表明,以白及胶为材料制备的微球将为癌症的治疗提供一种新型的栓塞治疗剂     

Effects of dihydroergotamine (DHE) on blood flow and metabolism in the underperfused myocardium in anaesthetized dogs

Summary The study was carried out in 13 mongrel dogs. Regional myocardial blood flow was measured using radiolabelled microspheres. Lactate, H⁺-ions, and O₂ content were measured in arterial and local venous blood. Partial occlusion of the ramus circumflexus (LCX) led to a decrease in left ventricular dp/dt max, systemic arterial pressure, and a marked release of lactate from the underperfused myocardium. With DHE (2 g/kg infused within 5 min, 8 dogs), a slight decrease in heart rate, left ventricular dp/dt max, LCX-resistance and a small increase in femoral and total peripheral resistance as well as in arterial and left and right atrial pressure was observed. In the normally perfused and in the underperfused part of the left ventricle microsphere assessed blood flow was unchanged or slightly elevated with DHE. Lactate release from the underperfused myocardium was markedly reduced. None of the DHE-induced effects on hemodynamic and metabolic parameters were observed in control experiments with infusion of 0.9% NaCl (5 ml). The results indicate that DHE leads to an amelioration of impaired metabolism in the underperfused myocardium and exerts no vasoconstriction in this area.This work was supported by the Fonds zur Förderung der wissenschaftlichen Forschung.     

Optimized Formulation of Magnetic Chitosan Microspheres Containing the Anticancer Agent,Oxantrazole

A combined emulsion/polymer cross-linking/solvent evaporation technique was used to prepare magnetic chitosan microspheres (MCM) containing the anticancer drug, oxantrazole. A central composite experimental design was used to simultaneously evaluate a variety of formulation factors on a number of response variables, such as the percentage of oxantrazole entrapped in the MCM. In association with the study design, statistical optimization procedures indicated the factors that significantly influence MCM preparation and what levels of the factors are needed to produce optimum MCM. Entrapment of anticancer agents into biodegradable microspheres is difficult because of low aqueous drug solubility and porosity of the particles. The latter effect was circumvented by a chitosan cross-linking step that resulted in 3% (w/w) oxantrazole entrapment in the MCM via the optimization procedures. The combined formulation and statistical optimization strategy provide a basis to develop other microparticulate systems and led to a dosage form that can be used for future in vivo investigations.     

水溶性药物聚丙交酯微球的研究

目的考察内相乙醇加入量及其他制备因素对聚丙交酯微球性质的影响。方法以水略溶性药物氟尿嘧啶和水溶性药物地基米松磷酸钠为模型药物，乳化／溶剂挥发法制备微球。维持其他制备条件不变，改变内相乙醇加入量、理论载药量、聚丙交酯浓度、溶剂挥发时间及聚丙交酯分子质量，考察微球载药量、包封率、粒径和释放的影响。结果随着内相乙醇加入量的增多，微球形成加快，微球的粒径减小，模型药物的载药量及包封率略有升高，但乙醇加入量太多时载药量及包封率均明显降低。内相聚丙交酯浓度越大，形成的微球粒径越大，载药量及包封率也愈大。理论载药量对微球粒径影响不大，地基米松磷酸钠的包封率随理论载药量的增加而减小，而氟尿嘧啶为理论载药量为15％时，包封率最大。溶剂挥发时间在0．5～3h，微球的性质无明显变化。分子质量愈小，微球的粒径愈小，载药量及包封率亦随之减小。结论内相中加入一定量乙醇可以提高药物的包封率，并减少有毒含氯溶剂的用量。     

布比卡因白蛋白微球的制备及药理学研究

目的制备盐酸布比卡因人血清白蛋白微球(Bupi-HSA-MS),并对其体内药动学、药效学及生物相容性进行评价。方法采用高压电场法制备布比卡因人血清白蛋白微球,采用改良的反相高效液相色谱法测定体内布比卡因血药浓度,以家兔为实验对象,以针刺疼痛反应圈直径大小评价其麻醉效果。结果药动学实验结果表明,注射剂组血药浓度达峰值时间短,浓度高,药物驻留时间短。微球组峰值浓度显著低于注射剂组并长时间维持低浓度。微球组MRT较对照组明显延长(P<0.01)。微球组皮下给药最大麻醉圈直径明显小于注射剂对照组(P<0.01),而微球组局麻持续时间较对照组明显延长(P<0.01)。结论高压电场法是一种简单、易行的白蛋白微球制备新方法。Bupi-HSA-MS兔皮下给药,药物扩散少,局部麻醉作用持续时间长,是一种安全长效的局部麻醉止痛新方法。     

尼索地平微球的制备

采用溶剂挥发法制备了尼索地平微球 ,考察了制备工艺中影响微球质量的 5个主要因素 ,筛选出较理想的处方和工艺。所得微球形态圆整 ,表面光滑 ,粒径 (18.2± 3.8) μm,载药量 2 1.2 % ,包封率 85 .4 %。     

口蹄疫DNA疫苗海藻酸钠微球的制备及体外释放的研究

目的：研制DNA疫苗海藻酸钠微球，并对其体外释药特性进行考察。方法：以口蹄疫DNA疫苗为DNA疫苗的模型药物，采用喷雾干燥一离子交联法制备DNA疫苗海藻酸钠微球；考察粒径大小、外观、载药量等理化特性；考察微球的体外释药特性及其影响因素。结果：微球球形圆整，分散性好，平均粒径为11．9μm，载药量为5％，产率为53．2％。微球的体外释放速率受载药量影响较小，而壳聚糖的交联固化度增高，微球的体外释放速率变慢。结论：以生物降解材料海藻酸钠、壳聚糖，用喷雾干燥法制备DNA疫苗微球，不需要超声和有机溶剂，因而有利于DNA疫苗结构和功能的稳定性；工艺简便，易于工业化生产。     

区域注射磷—32玻璃微球对裸鼠移植性人肝细胞癌的形态学影响

目的：研究－３２玻璃微球（３２Ｐ－ＧＭＳ）区域注射对裸鼠移植性人肝细胞癌的形态学影响及其意义。方法：应用光镜、免疫组织化学及电镜观察对照组及治疗组的肿瘤组织学和超微结构特征。结果：对照组中，瘤体长径约３ｃｍ，瘤细胞排列紧密，呈小梁状，富于血窦，约５％瘤细胞坏死。治疗组中，瘤体长径为０．４～２ｃｍ，其中少部分瘤体边缘细胞排列紧密，大部分瘤细胞排列松散，呈网状或假腺样且被纤维血管束分割成巢。４０％～８０％的瘤细胞呈凝固性坏死。７５％以上排列紧密的瘤细胞ＰＣＮＡ阳性，而排列松散的ＰＣＮＡ阳性瘤细胞不足２５％。松散排列的瘤细胞较紧密排列的瘤细胞，桥粒显著减少、细胞变性坏死增多。结论：本研究提示局部内放射３２Ｐ－ＧＭＳ明显具有杀伤癌细胞和抑制肿瘤生长的作用。这为３２Ｐ－ＧＭＳ对肝癌治疗的实验研究和临床应用提供形态学依据。     

骨炎一号微球的制备及其体外释药性能的研究

目的:制备骨炎一号微球,并考察其体外释药性能。方法:采用复乳-溶剂挥发法制备骨炎一号微球,用电子扫描显微镜观察微球表面形态,并测定微球的平均粒径、粒度分布、载药量、包封率,采用小杯法测定骨炎一号微球的体外释药情况,并计算其累积释药量。结果:制得的骨炎一号聚乳酸微球的形态圆整,微球的平均粒径为8.59μm,粒径在1-12μm的占总数的90%以上,载药量为48.39%,包封率为19.32%。骨炎一号微球在108h的累积释药量约为78.4%,t_1/2为40.8h,Higuchi方程为Y=0.1326 X-0.4782,r=0.9951。结论:得到了比较满意的骨炎一号微球制备工艺,且其体外释药性能符合长效制剂特征。