可降解淀粉微球包载盐酸洛美沙星的研究

目的 研究可降解淀粉微球用于包载盐酸洛美沙星药物.方法 以淀粉微球为药物载体,用反相乳液聚合的方法 制备了盐酸洛美沙星淀粉微球,建立了淀粉微球中盐酸洛美沙星的快速测定方法 -紫外分光光度法.用微球的载药量和包封率作为考察指标,通过正交设计实验研究了制备条件对微球载药量和包封率的影响.结果 该方法 快速、准确、操作简单;影响微球载药量和包封率的主要因素是淀粉溶液和盐酸洛美沙星溶液体积比以及淀粉乳浓度.结论 综合考虑了各种情况我们确定的最优实验方案为:淀粉浓度8%、淀粉溶液和盐酸洛美沙星溶液体积比2:1、油相水相体积比8:1、交联剂用量300μL.此时得到的载药量为:19.89μg*mg-1,包封率为:49.75%.     

双水相萃取法分离纯化白芸豆中α-淀粉酶抑制剂的研究

采用PEG/(NH4)2SO4双水相系统萃取α-淀粉酶抑制剂,考察了PEG浓度、(NH4)2SO4浓度和NaCl溶液浓度对α-淀粉酶抑制剂分配系数、相比和活力回收率的影响.确定了白芸豆中α-淀粉酶抑制剂提取的最佳条件,即PEG质量分数为12.O%,(NH4)2SO4的质量分数为13.3%,NaC1质量分数为O.003%时,分配系数、相比和活力回收率分别为4.40,O.57,71.41%.     

十味百合胶囊辅料优选工艺研究

目的 确定十味百合胶囊辅料种类和用量.方法 以颗粒吸湿率和休止角为指标,通过辅料种类、辅料配比筛选试验,优选出最佳辅料后,再对最佳辅料的不同用量进行考察.结果 加入辅料后,颗粒的吸湿率和流动性都有明显改善,其中糊精和可溶性淀粉制粒效果最好.结论 辅料选用糊精和可溶性淀粉,添加比例为干膏粉∶糊精:可溶性淀粉为8:1:1,制得颗粒具有最佳吸湿率和流动性.     

羟乙基淀粉130/0.4的研究进展

羟乙基淀粉130/0.4是一种新型的羟乙基淀粉代血浆产品, 国外已用于临床.重点综述了羟乙基淀粉130/0.4的扩容作用、药动学、安全性评价和临床研究.     

小儿健胃消食颗粒剂的处方优化

目的筛选小儿健胃消食颗粒剂的最佳处方.方法考察乳糖、淀粉、糊精及蔗糖对小儿健胃消食颗粒剂质量的影响.结果最佳处方为乳糖∶蔗糖∶可溶性淀粉:稠膏比为3∶1∶8∶6.颗粒中熊果酸的含量为0.2167mg/g.结论本法处方合理,工艺简单,所制备的小儿健胃消食颗粒质量稳定.     

高梁淀粉作片剂崩解剂和粘合剂的评价

本文介绍了用高粱淀粉作为含有无机和有机药物片剂的粘合剂和崩解剂的实用性实验,且与阿拉伯胶作粘合剂、玉米淀粉作粘合剂或崩解剂制备的片剂的物理性质进行了比较.可溶的和不可溶的无机药物以硫酸镁和碳酸钙为例,有机药物以磷酸氯喹和磺胺二甲基嘧啶为例.高粱淀粉由高粱种子中制得.高粱种子洗净后立     

TOC检测法测定羟乙基淀粉200/0.5残留量

目的通过对羟乙基淀粉200/0.5残留量TOC检验方法的验证,确定羟乙基淀粉200/0.5残留量用该检验方法检测的定量限、线性、灵敏度和回收率(准确度),确保该方法对羟乙基淀粉200/0.5残留量浓度检测结果的准确性.方法总有机碳法.结果该检测方法的线性范围为0.200～2.000 ppm;检测方法的回收率为100.7%;擦拭法的回收率为73.0%;精密度与重复性良好;定量限为:0.002 ppm.确定了凡残留量0.002～2.000 ppm范围内均可采用此方法检测.结论此方法操作简单,精密度、准确度、重复性较好.     

正交试验法优化藻酸双酯钠片工艺处方的研究

目的:优化藻酸双酯钠片的工艺处方.方法:采用正交试验设计,考察蔗糖、淀粉、滑石粉、糊精的配比和素片硬度、崩解度对藻酸双酯钠片的质量影响.结果:当处方蔗糖为21%、糊精为3%、滑石粉为7%、淀粉为6%时,素片硬度控制在5 kg左右,藻酸双酯钠片不仅有较好的硬度,而且崩解时间短.结论:新处方组方合理,重视性好,适合批量大生产.     

基于碘-淀粉显色的α-淀粉酶抑制剂筛选方法研究及应用

目的 对基于碘-淀粉显色的α-淀粉酶抑制剂筛选方法进行优化,以用于α-淀粉酶抑制剂的初期筛选。方法 本实验对基于碘-淀粉显色的α-淀粉酶抑制剂筛选方法体系中的淀粉浓度、α-淀粉酶浓度、阿卡波糖IC50值进行优化,考察了优化后方法的精密度、稳定性、重复性,并应用该方法测定了海地瓜多肽对α-淀粉酶的抑制作用。结果 优化后基于碘-淀粉显色的α-淀粉酶抑制剂筛选方法体系中淀粉浓度为0.08%、α-淀粉酶浓度为0.02 mg?mL?1、阿卡波糖IC50值为0.8 mg?mL?1,该方法精密度、稳定性及重复性均符合要求。结论 优化后方法可用于小分子化合物和肽类化合物的α-淀粉酶抑制剂筛选,具有广阔的应用前景。     

姜黄素多孔淀粉微球的制备

目的 制备姜黄素多孔淀粉微球.方法 用酶解法在玉米淀粉粒上水解出小孔,利用多孔淀粉的吸附作用制备姜黄素淀粉微球.结果 微球形态圆整,孔隙发育良好,载药量达4.1mg·g-1.结论 本法制备微球简单,方便.     

不同止血药物与妇科手术后深静脉血栓形成关系研究

目的：了解不同止血药物对妇科手术后深静脉血栓形成（LEDVT）的影响。方法：对1105例因妇科良性疾病行经腹盆腔手术的患者进行回顾性研究，所有研究对象按术中止血药物使用情况分为三组：立止血组，止血合剂组，未用止血药组．研究术中、术后止血药物应用对下肢深静脉血栓形成的影响。结果：术后应用氨甲环酸患者血栓发生率明显高于应用止血合剂患者，但明显低于应用白眉蛇毒凝血酶患者，差异有统计学意义（P〈0.01）。术中用止血合剂患者血栓发生率高于未用止血药组，但低于用立止血组。差异有统计学意义（P〈0．01）。结论：术中应用了止血药物的患者较未用止血药物的患者LEVDT发生率增加，并且LEVDT的发生与术中、术后应用止血药物的种类有关。     

我院临床使用抗菌药物存在问题的调查分析

通过对2003年我院住院患者抽查590例,对其抗菌药物使用情况进行调查、统计、分析.结果表明:抗菌药物不合理用药占22.16%.抗菌药物使用频度以头孢菌素类居首位,其次为喹诺酮类.不合理用药的主要表现是:预防应用比例过大,选择用药档次太高,用药剂量偏大,给药次数不恰当等.     

免疫抑制药物在妊娠合并再生障碍性贫血的应用

目的：探讨妊娠合并再生障碍性贫血孕期的免疫治疗。方法收集2003年至2013年我院收治的8例妊娠合并再生障碍性贫血的临床资料,采用回顾性分析的方法对其孕期免疫治疗及妊娠结局进行分析。结果孕期治疗：有1例应用环孢素,1例应用康力龙,2例应用达那唑,3例应用强的松,4例应用地塞米松,1例应用阿赛松,2例应用大剂量丙种球蛋白,均未见明显药物副反应;妊娠结局：1例阴道分娩,7例剖宫产分娩,指征均为产科因素,新生儿均未发现畸形。结论环孢素A及激素在孕期使用是相对安全的,但应密切监护母儿情况及注意防治药物副反应。     

Comparative evaluation of tableting compression behaviors by methods of internal and external lubricant addition: Inhibition of enzymatic activity of trypsin preparation by using external lubricant addition during the tableting compression process

This study evaluated tableting compression by using internal and external lubricant addition. The effect of lubricant addition on the enzymatic activity of trypsin, which was used as a model drug during the tableting compression process, was also investigated. The powder mixture (2% crystalline trypsin, 58% crystalline lactose, and 40% microcrystalline cellulose) was kneaded with 5% hydroxypropyl cellulose aqueous solution and then granulated using an extruding granulator equipped with a 0.5-mm mesh screen at 20 rpm. After drying, the sample granules were passed through a 10-mesh screen (1680 μm). A 200-mg sample was compressed by using 8-mm punches and dies at 49, 98, 196, or 388 MPa (Mega Pascal) at a speed of 25 mm/min. The external lubricant compression was performed using granules without lubricant in the punches and dies. The granules were already dry coated by the lubricant. In contrast, the internal lubricant compression was performed using sample granules (without dry coating) containing 0.5% lubricant. At 98 MPa, for example, the compression level using the external lubricant addition method was about 13% higher than that for internal addition. The significantly higher compressing energy was also observed at other MPas. By comparison, the friction energy for the external addition method calculated based on upper and lower compression forces was only slightly larger. The hardness of tablets prepared using the internal addition method was 34% to 48% lower than that for the external addition method. The total pore volume of the tablet prepared using the external addition method was significantly higher. The maximum ejection pressure using the no-addition method (ie, the tablet was prepared using neither dry-coated granules nor added lubricant) was significantly higher than that of other addition methods. The order was as follows: no addition, external addition, and then internal addition. The ejection energy (EE) for internal addition was the lowest; for no addition, EE was the highest. In the dissolution test, the tablets obtained using external addition immediately disintegrated and showed faster drug release than those prepared using internal addition. This result occurred because the water penetration rate of the tablet using the external addition was much higher. The trypsin activity in tablets prepared using the external addition method was significantly higher than that produced using the internal addition method at the same pressure. All these results suggest that the external addition method might produce a fast-dissolution tablet. Because the drug will be compressed using low pressure only, an unstable bulk drug may be tableted without losing potency.     

我院2006-2008年镇痛药使用情况分析

目的评价医院近年来镇痛药的使用情况。方法采用药历统计软件对北京天坛医院2006—2008年镇痛药的用药品种、销售金额、用药数量进行统计。结果吗啡和芬太尼用药量最大,氨酚羟考酮片（泰勒宁）用药量增长迅速。结论该院镇痛药的使用符合医院特点与镇痛药合理应用原则,用药基本合理。     

质子泵抑制剂预防重型颅脑损伤后与院内获得性肺炎的关系

目的探讨重型颅脑损伤患者应用质子泵抑制剂（PPI）预防应激性溃疡后是否增加院内获得性肺炎的发生率。方法回顾性调查近1年来我院收治的120例住院时间大于7天的重型颅脑损伤患者资料,分析使用PPI与未使用者发生院内获得性肺炎的情况。结果在120例重型颅脑损伤患者中使用PPI者83例,发生院内获得性肺炎29例,感染率为34．94％,尤其持续使用PPI≥7天者感染率为47．05％;未使用者34例,发生院内获得性肺炎4例,感染率为10．81％。结论应用PPI预防应激性溃疡的重型颅脑损伤患者院内获得性肺炎发生率明显高于未使用者,长时间持续使用明显高于短时使用。临床应根据患者具体情况选择用药和控制用药时间,以减少院内获得性肺炎发生率,减轻患者痛苦,减少资源浪费。     

新型毒品所致精神障碍临床特征的比较

目的：了解新型毒品所致精神障碍的临床特征。方法：应用自制吸毒人员一般资料调查表及简明精神病量表（BPRS）对101例新型毒品所致精神障碍患者进行调查和评定。结果：单独使用K粉或冰毒和两者混合使用3组新型毒品所致精神障碍患者的临床特征有所不同,单独使用K粉组的患者出现幻觉的比例明显高于单独使用冰毒或两者混合使用组患者（p均〈0.001）,而出现妄想的比例则低于单独使用冰毒或两者混合使用组患者（p均〈0.05）;BPRS评分显示,两者混合使用组患者思维障碍、激活性、敌对猜疑因子分均高于单独使用K粉或冰毒组患者（p均〈0.05）。结论：不同种类的新型毒品所致精神障碍的临床特征有所不同。     

Predictive Performance of a Semiparametric Method to Estimate Population Pharmacokinetic Parameters Using NONMEM

Routine clinical pharmacokinetic (PK) data collected from patients receiving inulin were analyzed to estimate population PK parameters; 560 plasma concentration determinations for inulin were obtained from 90 patients. The data were analyzed using NONMEM. The population PK parameters were estimated using a Constrained Longitudinal Splines (CLS) semiparametric approach and a first-order conditional method (FOCE). The mean posterior individual clearance values were 7.73 L/hr using both parametric and semiparametric methods. This estimation was compared with clearances estimated using standard nonlinear weighted least squares approach (reference value, 7.64 L/hr). The bias was not statistically different from zero and the precision of the estimates was 0.415 L/hr using parametric method and 0.984 L/hr using semiparametric method. To evaluate the predictive performances of the population parameters, 17 new subjects were used. First, the individual inulin clearance values were estimated from drug concentration–time curve using a nonlinear weighted least-squares method then they were estimated using the NONMEM POSTHOC method obtained using parametric and CLS methods as well as an alternative method based on a Monte Carlo simulation approach. The population parameters combined with two individual inulin plasma concentrations (0.25 and 2 hr) led to an estimation of individual clearances without bias and with a good precision. This paper not only evaluates the relative performance of the parametric and the CLS methods for sparse data but also introduces a new method for individual estimation.     

Encapsulation and in vitro evaluation of amikacin-loaded erythrocytes

The aim of our present work was to establish the effect of the osmolality of the hypotonic buffer on the encapsulated amount and the in vitro properties of Amikacin-loaded erythrocytes. Amikacin was encapsulated in rat erythrocytes using a hypotonic dialysis method with hypotonic buffers of different osmolalities with mean values around 90 and 150 mOsm/kg. Morphological examination of the ghost erythrocytes was accomplished using scanning electron microscopy (SEM). The osmotic fragility of normal and loaded erythrocytes was tested using hypotonic solutions. Evaluation of the hematological parameters of the control and loaded erythrocytes was carried out using a hematology system analyzer. Amikacin release from loaded erythrocytes was tested in autologous plasma at 37°C over a 24-h period. The quantification of Amikacin in loaded erythrocytes and in autologous plasma was performed using an HPLC technique. A higher osmotic fragility of loaded erythrocytes was observed using a low osmolality buffer. Some hematological parameters showed statistically significant differences between the loaded erythrocytes obtained using two buffers of different osmolalities with respect to untreated erythrocytes. According to our results, Amikacin carrier erythrocytes obtained by hypotonic dialysis using a low osmolality buffer (90 mOsm/kg) should afford a good encapsulation yield, appropriate morphological properties, and sustained release in vitro.     

替硝唑片粘合剂的筛选

目的筛选替硝唑片的粘合剂。方法分别采用8%聚乙烯吡咯烷酮(PVP-K30)、10%淀粉浆、40%糖浆和2.0%羟丙基甲基纤维素K4(HPMC-K4),50%乙醇作为替硝唑片的粘合剂,制成不同粘合剂配方的药片,观察素片的外观以及包衣后外观的变化,测定其硬度、脆碎度、崩解时限和溶出度。结果PVP-K30制成的片有光泽,测定脆碎度后有少许崩边缺角现象,包衣后片表面粗糙;淀粉浆制成的片有光泽,测定脆碎度后无崩边缺角现象,包衣后药片完整;糖浆制成的片较脆,测定脆碎度后有崩边、顶裂现象,包衣后片表面粗糙且有顶裂倾向;羟丙基甲基纤维素制成的片有光泽,振摇无崩边缺角现象,包衣后完整,外观好。结论用2.0%HPMC-K4、50%乙醇为粘合剂制备的药片外观好,在包薄膜衣过程中,不易出现崩边、缺角现象,包衣后片面美观,硬度、崩解度和溶出度也优于用其它粘合剂制成的片子。