奥沙利铂-碘油乳剂制备比例的试验研究

目的:研究肝动脉导管注射使用的奥沙利铂-碘油乳剂中溶媒(5%葡萄糖注射液)与碘油的较佳用量比例。方法:取50mg奥沙利铂分别溶解于0.5、1、2、2.5mL的5%葡萄糖注射液中,再分别与5mL的碘油混合后置于注射器中,用"单泵法"制备乳剂;采用普通显微镜观察乳滴分布情况,37℃观察油水分层情况,透析法进行体外释放试验,用高效液相色谱法测定透析液中奥沙利铂的浓度并计算累积释放度。结果:随着奥沙利铂-碘油乳剂中5%葡萄糖注射液比例的降低,乳滴分布趋向均匀,油水分层时间延长,缓释作用延长。二者比例为0.5∶5时,乳剂乳滴分布均匀,乳剂在放置时间超过24h时未见分层,释放慢,具有良好的物理化学稳定性。结论:奥沙利铂在葡萄糖注射液-碘油(0.5∶5)乳剂中具有稳定的物理化学性质和优良的缓释作用。     

乳剂型大蒜素妇炎栓制备工艺研究

妇科炎症是妇科常见疾病,是由霉菌、白假丝酵母菌、衣原体等病原体单一或混合感染引发的疾病。研究表明大蒜素对霉菌、白假丝酵母菌、衣原体等病原体有着很好的抑制作用,并有增强人体免疫力的作用[1-3],目前市场在售的外用药如甲硝唑栓剂、双唑泰栓等,多对细菌或真菌感染引起的妇科炎症有效,但其     

维通静脉注射乳安全性研究

目的：对维通静脉注射乳（WIE）进行安全性检查。方法用豚鼠进行过敏性实验,用小鼠进异常毒性实验,用家兔进行刺激性和溶血性实验研究维通静脉注射乳安全性。结果 WIE未引起豚鼠的变态反应,未引起家兔血红细胞溶血性反应,未引起小鼠异常毒性反应。结论本方法生产的维通静脉注射液性质安全,具有一定的应用价值。     

Preparation of microcapsules and control of their morphology

For the preparation of microcapsules using the W/O/W (water in oil in water) emulsion system, it is essential to control various factors such as the dispersed state of the organic phase in the W/O/W emulsion, the difference in the solute concentration between the inner and outer aqueous phases and the volume fraction of the dispersed phase. In this study, cross-linked microcapsules were prepared by the in-situ polymerization of styrene and divinylbenzene and biodegradable microcapsules were prepared by the solvent evaporation method. The effects of the preparation conditions on the capsule morphology and entrapment efficiency of water-soluble materials were investigated. The average diameter of the surface pores and internal hollows were controlled on a sub-micron order by changing the preparation conditions such as diluent concentration, volume fraction of the dispersed droplets in the W/O (water in oil) emulsion, surfactant concentration monomer ratio and salt concentration in the outer aqueous phase. Furthermore, the water-soluble materials were completely entrapped in the biodegradable microcapsule by changing the preparation conditions such as volume fraction of the dispersed droplets in the W/O emulsion, salt concentration in the inner and outer aqueous phases, polymer concentration and supersonic irradiation of the W/O droplets.     

Concanavalin-A Conjugated Fine-Multiple Emulsion Loaded with 6-Mercaptopurine

Fine-multiple (water-in-oil-in-water) emulsions were prepared by two-step emulsification using sonication. They were coated with concanavalin-A (Con-A) by three methods. The one involving covalent coupling of Con-A to the multiple emulsion incorporated anchor was better compared with lipid derivatized Con-A anchoring or the glutaraldehyde-based cross-linking method, as shown by the faster rate of dextran-induced aggregation. The selected multiple emulsions were characterized by physical properties such as droplet size, encapsulation efficiency, and zeta potential. Stability parameters such as droplet size, creaming, leakage, and aggregation as a function of relative turbidity were monitored over a 1-month period, which revealed good stability of the formulations. The release profile of 6-mercaptopurine followed zero-order kinetics. Pharmacokinetic studies showed an increase in half-life and bioavailability from multiple emulsion formulations administered intravenously. There was prolonged retention of drug in various tissues of rats when treated with Con-A-coated multiple emulsion as compared with uncoated one. Our study demonstrates the suitability of fine-multiple emulsion for intravenous administration and the potential for prolonged retention of drugs and targeting in biological systems.     

参麦注射液联合鸦胆子油乳治疗晚期肿瘤恶液质34例

目的探讨参麦注射液联合鸦胆子油乳治疗癌症晚期恶液质的临床疗效。方法将68例晚期癌症恶液质患者随机分为治疗组和对照组,每组34例;治疗组予参麦注射液联合鸦胆子油乳注射液,对照组予氨基酸等胃肠外营养;两组疗程均为1个月,观察生存质量疗效、体质量疗效以及淋巴细胞亚群变化情况。结果治疗组生存质量、体质量总有效率分别为88.2%、85.3%,对照组分别为67.6%、64.7%;治疗组生存质量疗效、体质量疗效均明显优于对照组(P0.05)。治疗前后组内比较,治疗组CD4+、CD4+/CD8+水平明显提高(P0.05),对照组各指标差异均无统计学意义(P0.05);组间治疗后比较,CD4+、CD4+/CD8+差异有统计学意义(P0.05)。结论参麦注射液联合鸦胆子油乳注射液能够改善癌症晚期恶液质患者的生存质量,增加体质量,提高机体免疫功能。     

华蟾素乳剂对小鼠Lewis肺癌的药效学研究

目的：研究华蟾素乳剂对实体肿瘤的疗效及其可能的作用机制。方法：本研究运用Lewis肺癌小鼠模型,观察华蟾素乳剂对小鼠Lewis肺癌的疗效、免疫功能的影响。结果：华蟾素乳剂治疗小鼠Lewis肺癌能抑制肿瘤的生长,抑瘤率高达32.7%,稳定病灶,提高荷瘤小鼠的生存质量,明显提高校正廓清指数α（P〈0.01）以及溶血素水平（P〈0.05）,改善免疫功能。结论：华蟾素乳剂对小鼠Lewis肺癌有明显疗效,其作用机制与其本身对Lewis肺癌实体瘤有抑制作用和提高荷瘤小鼠免疫功能有关。     

鱼油脂肪乳对重症颅脑外伤病人炎性反应的影响

目的:探讨鱼油脂肪乳对重症颅脑外伤病人炎性反应的影响.方法:选择颅脑外伤病人44例,随机分为常规胃肠外营养组(TPN组)和鱼油脂肪乳治疗组(鱼油组),每组各22例.两组病人均接受等氮、等热最的TPN.病人所需热量为83.68 kJ(20 kcal)/(kg·d),氮为0.2 g/(kg·d).鱼油组病人用鱼油脂肪乳,共...     

维生素A棕榈酸酯原料细菌内毒素检查方法研究

目的：建立检查维生素A棕榈酸酯进行细菌内毒素检查法。方法：维生素A棕榈酸酯以无水乙醇为溶剂溶解,再用细菌内毒素检查用水稀释制成乳浊液,依照《中国药典》2020年版(四部)1143细菌内毒素检查法,对维生素A棕榈酸酯细菌内毒素检查法进行干扰试验预试验和干扰试验,同时增加细菌内毒素回收干扰试验预试验和干扰试验。结果：维生素A棕榈酸酯在实验过程中出现的复析、乳浊现象对细菌内毒素检查无影响,维生素A棕榈酸酯在0.015625mg.ml-1^浓度下对细菌内毒素检查无干扰作用。结论：本法可用于维生素A棕榈酸酯细菌内毒素的质量控制。     

大豆油乳剂对胃粘膜保护作用的实验研究

实验研究大豆油乳剂治疗消化性溃疡的疗效及其作用机制。方法：采用阿司匹林、应激性溃疡、幽门结扎及慢性醋酸４种胃溃疡动物模型,对大豆油乳剂治疗胃溃疡的疗效进行了研究,其中慢性醋酸模型和幽门结扎模型选用Ｗｉｓｔａｒ雄性大鼠,应激性溃疡模型和阿司匹林模型选用昆明种雄性小鼠。同时通过对慢性醋酸模型鼠胃粘膜前列腺素Ｅ２（ＰＧＥ２）、超氧化物歧化酶（ＳＯＤ）及丙二醛（ＭＤＡ）的检测,对植物油乳剂治疗消化性溃疡的机制进行了探讨。结果：大豆油乳剂对４种溃疡动物模型均有疗效（Ｐ＜０．０１）。另外,大豆油乳剂可增加鼠胃粘膜的内源性ＰＧＥ２（Ｐ＜０．０１）,降低动物胃粘膜的ＳＯＤ活性（Ｐ＜０．０１）及ＭＤＡ含量（Ｐ＜０．０１）。结论：大豆油乳剂对实验动物的消化性溃疡疗效肯定,其机制主要与增加胃粘膜内源性ＰＧＥ２、减轻氧自由基对胃粘膜的损害有关。