盐酸二甲双胍缓释片处方筛选及工艺研究

对盐酸二甲双胍缓释片的处方及工艺进行筛选和研究。方法：根据释放度作为判断原则，对缓释骨架材料、填充剂、粘合剂、润滑剂及包衣材料的种类、规格、用量及工艺等进行了考察，并在此基础上采用正交试验1．9(3^4)方案对处方进行筛选。结果：以HPMC K100M及HPMC K15M作为盐酸二甲双胍缓释片的基本骨架材料，微晶纤维素作为填充剂，硬脂酸镁为润滑剂，4％HPMCE5的70％乙醇溶液适量作为粘合剂制成片芯，采用薄膜包衣法，以欧巴代的70％乙醇溶液作为薄膜包衣材料，制得盐酸二甲双胍缓释骨架片。结论：本制剂工艺简单，所用各种辅料均为国产化，成本低，制得盐酸二甲双胍缓释片释放度符合规定。     

静脉与硬膜外PCA用于剖宫产术后镇痛的对比观察

目的：比较自控静脉镇痛（PCIA）和自控硬膜外镇痛（PCEA）用于剖宫产术后镇痛的有效性、安全性及不良反应。方法：选择剖宫产术后病人90例，随机分为PCIA组、PCEA组和对照组，每组30例。PCIA组和PCEA组术后立即使用自控镇痛（PCA）泵．对照组则不用任何药物镇痛。采用视觉模拟评分法（VAS）对术后1、4、8、24、48h各时间段进行镇痛效果评价和镇静评分并同时观察病人术后肠蠕动恢复情况、拔尿管后排尿情况、子宫复旧情况及产后出血、恶心呕吐、皮肤瘙痒、呼吸抑制等不良反应。结果：同一时间段PCIA组与PCEA组VAS评分比较无显著差异（P〉0．05）．但均小于对照组（P〈0．01）；术后肠蠕动恢复时间、子宫复旧情况、产后出血及恶心、呕吐、皮肤瘙痒、嗜睡等不良反应发生率三组比较无显著差异（P〉0．05）；拔尿管后排尿困难发生率PCIA组明显低于PCEA组（P〈0．05）；呼吸循环抑制PCEA组多于PCIA组，但差异不显著（P〉0．05）。结论：PCIA组与PCEA组均有良好的术后镇痛效果．但PCIA组拔尿管后排尿困难的发生率低．对呼吸循环影响小，镇痛质量优于PCEA组。     

紫外分光光度法测定黄芩苷脂质体的包封率与渗漏率

目的测定黄芩苷脂质体的包封率与渗漏率。方法采用Sephadex G-50凝胶柱分离游离药物，紫外分光光度法测定黄芩苷脂质体的含量。结果黄芩苷线性范围4～20 μg·mL^-1，r＝0.999 4，加样回收率98.83%，RSD＝2.26%。结论该方法简便易行，准确性高，可用于测定脂质体的包封率与渗漏率。     

不同型号聚羧乙烯对口腔粘附缓释膜质量的比较

目的　比较不同型号生物粘附剂———聚羧乙烯对口腔粘附缓释膜质量的影响。方法　以中药复方溃宁为模型药,通过对给药系统的粘附力、体外释放速率等的测定进行评价。结果　3种膜剂的粘附力分别为CP934:6 6. 8±4 .5g/cm2 ;CP971 :5 5 . 9±4 .7g/cm2 ;CP974 :5 2 . 8±4 .4g/cm2 。体外释放速率(T50 )分别为CP934:2 4 0min ;CP971 :30 0min ;CP974 :1 0 0min。结论　不同型号的生物粘附剂聚羧乙烯对口腔粘附缓释膜的质量有显著影响;膜的粘附性CP934最大,CP974最小;释放速率CP974型最快,CP971型最慢。     

加味补肾壮筋汤颗粒剂防治去卵巢大鼠骨质疏松症的实验研究

目的:评价与比较加味补肾壮筋汤传统汤剂与其中药配方颗粒剂对卵巢切除诱发骨质疏松大鼠模型的防治效果.方法:选用6月龄清洁级Wistar雌性大鼠60只,随机分为正常对照组.模型组、汤剂组和颗粒剂组,每组15只.用双侧卵巢切除术进行动物造模,术后1周给药,用药3月后分别进行血清Ca、P、ALP、BGP、PTH、CT、尿H0P含量的测定,并进行全身骨、股骨颈、胫骨干骺端、腰椎等部位的骨密度检测.结果:加味补肾壮筋汤汤剂和其颗粒剂均能明显增加血清BGP、CT的含量,降低血清PTH和尿HOP含量,均能增加全身骨、股骨颈、胫骨干骺端、腰椎等部位的骨密度值,且差异与模型组有统计学意义(P＜0.05),但两者之间差异无统计学意义(P＞0.05).结论:加味补肾壮筋汤颗粒剂进行剂型改革后仍能发挥防治骨质疏松症的作用,且与传统汤剂相比并不会导致疗效上的不同,故该中药配方颗粒剂可以代替传统汤剂使用.     

New Characterization Measures of Pore Shape and Connectivity Applied to Coatings used for Controlled Drug Release

Pore geometry characterization-methods are important tools for understanding how pore structure influences properties such as transport through a porous material. Bottlenecks can have a large influence on transport and related properties. However, existing methods only catch certain types of bottleneck effects caused by variations in pore size. We here introduce a new measure, geodesic channel strength, which captures a different type of bottleneck effect caused by many paths coinciding in the same pore. We further develop new variants of pore size measures and propose a new way of visualizing 3-D characterization results using layered images. The new measures together with existing measures were used to characterize and visualize properties of 3-D FIB-SEM images of three leached ethyl-cellulose/hydroxypropyl-cellulose films. All films were shown to be anisotropic, and the strongest anisotropy was found in the film with lowest porosity. This film had very tortuous paths and strong geodesic channel-bottlenecks, while the paths through the other two films were relatively straight with well-connected pore networks. The geodesic channel strength was shown to give important new visual and quantitative insights about connectivity, and the new pore size measures provided useful information about anisotropies and inhomogeneities in the pore structures. The methods have been implemented in the freely available software MIST.     

Tablet and Capsule Hydrophilic Matrices Based on Heterodisperse Polysaccharides Having Porosity-Independent In Vitro Release Profiles

The purpose of the study was to investigate the release-controlling action of a swellable hydrophilic material based on heterodisperse polysaccharides (HP) in relation to the initial pore structure of the formulations. HP-based granules were produced under carefully controlled conditions and compacted into matrix tablets having equivalent tablet thickness. Quantification of pore structure using mercury porosimetry showed that the tablets had substantially different pore volumes and pore size distributions. Dissolution studies demonstrated that release of a water-soluble model compound, benzamide, from swollen matrices was affected neither by total porosity nor median pore diameter of the initial dry matrix. To extend the concept of porosity-independent release further, HP-based formulations containing either diclofenac sodium or propranolol HCl were contained within hard gelatin capsules in the form of uncompacted granules. This produced a dosage form with a high intraparticulate porosity in the dry state. Equivalent weights of the same formulations were also compacted into tablets. The in vitro release profiles from matrix tablets compacted from any of the formulations did not differ significantly from release profiles obtained when the same materials were contained uncompacted in hard gelatin capsules.     

远程无线镇痛泵常见报警原因分析及对策

目的：针对远程无线镇痛泵常见的报警问题分析原因并提出预防及解决方法。方法统计分析2013年1～3月，应用无线镇痛泵的2732例手术患者在使用中所出现的报警问题。结果2732例共出现报警问题1287次，其中，有镇痛不足、堵塞、气泡或无液、电量报警等，经随访人员及时处理，所有报警问题均得以顺利解决。结论在使用远程无线镇痛系统时，预见性评估并解决可能出现的报警问题，正确掌握处理无线镇痛泵报警问题的方法，可有效减少报警发生率，保证镇痛效果，提高患者使用满意度。     

Pharmacokinetics,biocompatibility and bioavailability of a controlled release monoclonal antibody formulation

The sustained and localized delivery of monoclonal antibodies has become highly relevant, because of the increasing number of investigated local delivery applications in recent years. As the local delivery of antibodies is associated with high technological hurdles, very few successful approaches have been reported in the literature so far. Alginate-based delivery systems were previously described as promising sustained release formulations for monoclonal antibodies (mAbs). In order to further investigate their applicability, a single-dose animal study was conducted to compare the biocompatibility, the pharmacokinetics and the bioavailability of a human monoclonal antibody liquid formulation with two alginate-based sustained delivery systems after subcutaneous administration in rats. 28 days after injection, the depot systems were still found in the subcutis of the animals. A calcium cross-linked alginate formulation, which was injected as a hydrogel, was present as multiple compartments separated by subcutaneous tissue. An in situ forming alginate formulation was recovered as a single compact and cohesive structure. It can be assumed that the multiple compartments of the hydrogel formulation led to almost identical pharmacokinetic profiles for all tested animals, whereas the compact nature of the in situ forming system resulted in large interindividual variations in pharmacokinetics. As compared to the liquid formulation the hydrogel formulations led to lower mAb serum levels, and the in situ forming system to a shift in the time to reach the maximum mAb serum concentration (T_max) from 2 to 4 days. Importantly, it was shown that after 28 days only marginal amounts of residual mAb were present in the alginate matrix and in the tissue at the injection site indicating nearly complete release. In line with this finding, systemic drug bioavailability was not affected by using the controlled release systems. This study successfully demonstrates the suitability and underlines the potential of polyanionic systems for local and controlled mAb delivery.     

Ordered mesoporous silica modified with lanthanum for ibuprofen loading and release behaviour

The ordered mesoporous silicas SBA-15 and KIT-6, modified with lanthanum, have been for the first time applied in investigation of ibuprofen adsorption and release. The materials of hexagonal and regular structure were obtained by the hydrothermal method using a triblock copolymer Pluronic P123 as a template. The mesoporous silicas were impregnated with an aqueous solution of lanthanum(III) chloride in the amount necessary to obtain 1, 3 and 5 wt.% La loading. The physicochemical properties of the modified silicas were characterised by X-ray diffraction, transmission electron microscopy, UV–Vis spectrophotometry and low-temperature nitrogen sorption. The results showed that lanthanum strongly determined structural as well as textural properties of the silicas. The samples of modified silica were checked for the ability to adsorb and release of ibuprofen. The storage capacity of the modified silicas obtained increased with increasing their average pore diameter and percentage content of lanthanum. The amount of ibuprofen adsorbed onto KIT-6 silica modified with La was higher than that adsorbed onto SBA-15 materials. The high coverage of lanthanum on the surface of KIT-6 and SBA-15 solids was found to increase the amount of ibuprofen and the rate of its release.