膀胱肿瘤的导向诊断

目的 探讨＾９９ｍＴｃ标记单克隆抗体用于膀胱癌放射免疫显像诊断的临床价值及意义。方法 采用２－硫基乙醇还原法将＾９９ｍＴｃ与抗人膀胱癌单克隆抗体ＢＤＩ－１进行标记，制备＾９９ｍＴｃ－ＢＤＩ－１，灌注入患者膀胱腔中，进行γ－照相机采集图像。结果４４例患者接受了显像。     

联糖米托蒽醌的趋肝性研究

目的：合成肝靶向药联糖米托蒽醌（ＮＧＡＤＨＡＱ）的趋肝性研究。方法：以合成配体半乳糖基拟糖白蛋白（ｎｅｏｇｌｙｃｏａｌｂｕｍｉｎ,ＮＧＡ）为载体,与抗癌药物米托蒽醌（ｍｉｔｏｘａｎｔｒｏｎｅ,ＤＨＡＱ）偶联得肝靶向抗癌药物ＮＧＡＤＨＡＱ。采用紫外光谱和ＨＰＬＣ确证其偶联的形式及在血液中的稳定性。用９９ｍＴｃ标记后进行家兔放射性显像及小鼠体内的分布实验。结果：ＮＧＡＤＨＡＱ为化学偶联物且在血中很稳定,家兔及小鼠肝中药物的量均在５ｍｉｎ时达最大,分别占全身放射量的６５．１％和６５．４％±４．３％（ｎ＝３）。结论：说明ＮＧＡＤＨＡＱ具肝靶向分布性。     

^99mTc—EHIDA显像在婴儿肝炎综合征的应用

９９ｍＴｃ－ＥＨＩＤＡ显像在婴儿肝炎综合征的应用王伯龄黄永坤黄维丽马婉君李庆云纳志云９９ｍＴｃ－ＥＨＩＤＡ显像已应用多年，但在儿科领域内应用不多，我们对３０例婴儿肝炎综合征进行９９ｍＴｃ－ＥＨＩＤＡ动态及延迟显像，用感兴趣区（ＲＯＩ...     

^99mTc—MIBI显像对乳腺肿块及腑淋巴结的诊断价值

目的：探讨＾９９ｍ锝－甲氧基异丁基异腈（ＭＩＢＩ）显像对乳腺肿块良恶性的鉴别价值及对阳性腋淋巴结的显像。方法住院手术的１９例乳腺肿块及腋淋巴结进行＾９９ｍＴｃ－ＭＩＢＩ显像,并与病理结果相对比。结果１４例恶性肿瘤显像１４例,５例良性肿瘤显像２例;７例腋淋巴结阳性显像６例,７例腋淋巴结阴性显像１例;２例单侧乳腺癌显像双侧腋淋巴结阳性并经病理证实。结论＾９９ｍＴｃ－ＭＩＢＩ显像敏感、方便可作为乳腺肿块     

^99mTc—MIBI心肌断层显像潘生丁介入试验对冠心病诊断价值的观察

报道２７例正常对照者７８例冠心病（ＣＨＤ）患者＾９９ｍＴｃ－ＭＩＢＩ静息心肌显像及潘生丁介入后心肌显像，并与心电图（ＥＣＧ）、平板运动试验作对比，结果表明：＾９９ｍＴｃ－ＭＩＢＩ心肌灌注断层显像对缺血性心脏病诊断的阳性率为９２．３％，高于平板运动试验的８１．８％，ＥＣＧ的７４．３％，有非常显著性差异（Ｐ〈０．０１），特异性为８９．４％。     

肝靶向半乳糖基干扰素的合成及其生物学性质研究

本文采用２－亚氨基－２－甲氧乙基－１－β－硫代－Ｄ－半乳吡喃糖甙与基因工程干扰素（ＩＦＮａ１）相偶联，得到半乳糖基基因工程干扰素ａ１偶物（Ｇａｌ－ＬＦＮａ１）。并分别进行小鼠体内分布实验和家兔显像实验，其趋肝性实验结果表明，肝脏对Ｇａｌ－ＩＦＮａ１和ＩＦＮａ１的最大摄取值分别为２９．１％和１０．０％，并采用细胞致病变效应（ＣＰＥ）抑制微量法测定了偶联物的效价，偶联物Ｇａｌ－ＩＦＮａ１与对照品（ＩＦ     

肝靶向抗疟药NGA－PQ的合成及其抗疟作用

以肝细胞表面的无唾液酸糖蛋白受体的特异性配基──半乳糖基拟糖白蛋白（Ｎｅｏｇｌｙｃｏａｌｂｕｍｉｎ．ＮＧＡ）作为载体，通过丁二酰胺桥，成功地与抗疟药伯氨喹（ＰＱ）偶联，制备了肝靶向抗疟药ＮＧＡ－ＰＱ，药密度达到１６．８±０．８５，糖密度达到２１．７±１．７３．经药效学试验，ＮＧＡ－ＰＱ的抗疟作用明显优于同剂量的ＰＱ。     

肝靶向抗病毒药NGA－ACV的制备及其趋肝性

以无唾液酸糖蛋白受体（ａｓｉａｌｏｇｌｙｃｏｐｒｏｔｅｉｎｒｅｃｅｐｔｏｒ，ＡＳＧＰＲ）的特异性配体半乳糖基拟糖白蛋白（ｎｅｏｇｌｙｃｏａｌｂｕｍｉｎ，ＮＧＡ）为载体，通过丁二酰基桥将抗病毒药无环鸟苷（ａｃｙｃｌｏｖｉｒ，ＡＣＶ）与ＮＧＡ偶联，得到肝靶向抗病毒药ＮＧＡＡＣＶ。差热分析和高效液相色谱分析结果表明，ＮＧＡＡＣＶ是共价键偶联物，且在血液中稳定性很好。将偶联物用１３１Ｉ标记后进行家兔放射性显像比较研究。结果，高、低药密度ＮＧＡＡＣＶ的肝脏放射性分别是全身放射性的８１．６％和８６．６％，其趋肝性无明显差别。研究小鼠体内高药密度１３１ＩＮＧＡＡＣＶ的分布，在５ｍｉｎ时肝脏放射性达到峰值，为注入量的８１．７±１０．４％。受体竞争抑制实验表明ＮＧＡＡＣＶ的肝靶向机理为受体介导的主动靶向过程。初步体外抗乙肝病毒比较研究表明，ＮＧＡＡＣＶ较ＡＣＶ的抗病毒剂量有明显降低。     

半乳糖抗小鼠CD3单克隆抗体的制备及其结合TIL后的趋肝性研究

报道以半乳糖为原料制得２－亚氨基－２－甲氧乙基－１－硫代－β－Ｄ－半乳糖苷（ＩＭＥ）后,与抗小鼠ＣＤ３单克隆抗体共价偶联制得半乳糖抗小鼠ＣＤ３单克隆抗体,再与标记３Ｈ－ＴｄＲ的肿瘤浸润性淋巴细胞（ＴＩＬ）结合。经动物试验表明,复合物较单纯ＴＩＬ具有明显的趋肝性,且能较长时间地浓集于小鼠肝脏内,说明半乳糖抗小鼠ＣＤ３单克隆抗体可作为肝靶向载体将抗肿瘤药选择性地导向肝脏,可能为肝癌的生物导向治疗开辟了新的途径。     

Uptake of ~(99m)Tc~(5 )-complexes in ischemic myocardial slices and theirdisociable ability

目的：研究在机体内具有一定的稳定性而又能离解出可到达靶组织的活性形式ＴｃＯ３－４的多核锝标记化合物．方法：模仿锝标记化合物进入血循环后的状况，采用稀释的方法，用硅胶板薄层层析法来测量其离解能力的大小．结果：５００倍稀释液的离解物峰的相对放射性百分数为：９９ｍＴｃ５＋ｓｕｃｉｍｅｒ为０，９９ｍＴｃ５＋ＧＨ为２８１％±１３％，９９ｍＴｃ５＋ＰＰｉ为４６０％±２９％，而缺血３ｈ的心肌中的摄取为：９９ｍＴｃ５＋ｓｕｃｉｍｅｒ是４２０％±１１０％ｄｏｓｅ／ｇｔｉｓｕｅ，９９ｍＴｃ５＋ＧＨ是７１０％±１８０％ｄｏｓｅ／ｇｔｉｓｕｅ，９９ｍＴｃ５＋ＰＰｉ是１２９５％±３９０％ｄｏｓｅ／ｇｔｉｓｕｅ．结论：以上几种多核螯合物的离解性与其在缺血性心肌中的摄取成正相关关系．     

CYP2C19基因多态性对癫痫患者丙戊酸血药浓度的影响

目的：研究癫痫患者CYP2C19基因多态性与丙戊酸稳态血药浓度的关系。方法：运用PCR-RFLP方法对99例癫痫病人的CYP2C19＊2（681G→A）和CYP2C19＊3（636G→A）位点进行基因型分析,选择其中临床资料较全的88名,对其丙戊酸血药浓度检测结果与基因型结果进行统计学分析。结果：在99例患者中,同时分析两个位点共5种双位点基因型组合：681GG-636GG、681GA-636GG、681GG-636GA、681AA-636GG和681GA-636GA,分布频率为37.4%、42.4%、6.1%、9.1%和5.1%。其中681AA-636GG基因型患者的丙戊酸血药浓度与体重剂量的比值明显高于野生基因型（681GG-636GG）（P〈0.05）,其他基因型与野生型相比无统计学差异。结论：本研究结果证实CYP2C19基因多态性影响了丙戊酸血药浓度,说明药物遗传学研究对丙戊酸临床合理用药有指导意义。     

水解明胶霜治疗皲裂的临床疗效观察

本文报告自1984年以来应用水解明胶霜治疗龟裂30例,皲裂333例,取得满意效果。皲裂的有效率达99％,治愈率为78.7％。在治愈的262例皲裂中平均12.3d治愈。61％在10d内治愈。疗效明显优于常用治皲裂的尿素脂及硫黄水杨酸软膏,统计学处理p<0.01。其疗效机理可能由于水解明胶与尿素相似有较强的水合作用,可防止皮肤干燥,且可加速细胞生长,从而修复和促进裂口的愈合。     

In vivo evaluation of time and site of disintegration of polysaccharide tablet prepared for colon-specific drug delivery

Compression coating has been found to be useful for colonic drug delivery. The aim of the present investigation was to evaluate a formulation with a considerably reduced coat weight and gum concentration for colonic drug delivery in vivo using gamma scintigraphy. In vitro studies have found this formulation to be useful for delivery of 5-fluorouracil to the colon. Rapidly disintegrating core tablets containing (99m)Tc-DTPA were prepared and compression coating with 150 mg of granules containing a mixture of xanthan (XG), guar gum (GG) and starch. The ratios of the two gums XG:GG in the coat was kept 10:20. In vitro dissolution studies on XG:GG::10:20 tablets containing (99m)Tc-DTPA were carried out in simulated upper GIT conditions and also in presence of colonic contents. Cumulative percent release of technetium in the upper GIT conditions and transit time amounted to 4%. The total amount of technetium released in the 24 h of the dissolution study was 53+/-3.23%. Upon introduction of cecal content into the dissolution medium (4%), the release of technetium from the compression-coated tablet increased to 78.34+/-5.34%. Gamma scintigraphy studies carried out in six healthy human volunteers showed that the tablet remained intact during its transit through the upper GIT. The anatomical site of disintegration was found to be the ascending colon/hepatic flexure and the disintegration of the tablet started between 4 and 6 h post-dose in all the volunteers with a further spread of tracer into the ascending, transverse, descending and sigmoidal colon.     

褪黑激素明胶微球的鼻腔给药

目的　制备经鼻粘膜给药的褪黑激素明胶微球,以提高其生物利用度。方法　用乳化交联技术制备褪黑激素明胶微球,用放射性核素^99mTc标记,用γ射线闪烁显像技术考察微球在鼻粘膜滞留时间,用HPLC法测定药物的体内吸收。结果　褪黑激素明胶微球粒径在30～70 μm,平均粒径为50.2 μm,褪黑激素含量为13.48%。与滴鼻液相比,明胶微球在鼻粘膜滞留时间明显延长。褪黑激素明胶微球的绝对生物利用度为87.47%。结论　鼻粘膜给药明胶微球,能避免肝脏首过作用,延长药物在鼻粘膜滞留时间,提高药物吸收,有很好的应用前景。     

复方黄连凝胶剂体内抗菌活性研究

将药理学研究的基础方法与组织学技术相结合,以细菌和真菌感染皮肤的日本大白兔模型为研究对象,研究了复方黄连凝胶剂对细菌和真菌皮肤感染的治疗效果。并通过皮肤组织学实验,以皮肤细胞修复状况和炎性细胞浸润为主要指标,从组织学角度进一步阐述复方黄连凝胶剂促进皮肤愈合的疗效。结果显示,治疗组愈合率均高于对照组。研究表明复方黄连凝胶剂抗菌作用强,是一种较好的外用抗菌药。     

A scintigraphic investigation of the disintegration behaviour of capsules in fasting subjects: a comparison of hypromellose capsules containing carrageenan as a gelling agent and standard gelatin capsules.

Two-piece hard shell capsules made from hypromellose (or hydroxypropyl methylcellulose, HPMC) have been proposed as an alternative to conventional gelatin capsules for oral drug delivery; however, little is known about their in vivo behaviour. The aim of this study was to compare the disintegration of HPMC and gelatin capsules in fasted human subjects using the technique of gamma scintigraphy. HPMC capsules containing carrageenan as a gelling agent (QUALI-V(R), Qualicaps) and gelatin capsules (Qualicaps) of size 0 were filled with a lactose-based mixture. The capsules were separately radiolabelled with indium-111 and technetium-99m. Both capsules were administered simultaneously with 180ml water to eight healthy male subjects following an overnight fast. Each volunteer was positioned in front of the gamma camera and sequential 60s images were acquired in a continuous manner for 30min. No differences in the oesophageal transit of the two types of capsules were noted, with the capsules arriving in the stomach in a matter of seconds. All the capsules disintegrated in the stomach. The mean (+/-S.D.) disintegration time for the HPMC capsules was 9+/-2min (range 6-11min). The corresponding mean time for the gelatin capsules was 7+/-4min (range 3-13min). These disintegration times were not significantly different (P=0.108, paired t-test). In conclusion, HPMC and gelatin capsules show rapid and comparable in vivo disintegration times in the fasted state. HPMC capsules containing carrageenan as a gelling agent therefore offer a practical alternative to gelatin capsules as an oral drug delivery carrier.     

Streptomycin sulphate microspheres: formulation and in vivo distribution

Albumin and gelatin microspheres of streptomycin sulphate were formulated and their potential as a drug delivery system for a tuberculostatic agent in vivo was evaluated. Biodistribution was determined by i.v. administration of a 99mTc-labelled microsphere suspension to mice. The radioactivity of the lungs was compared with the radioactivity of the liver, spleen, kidney and heart at 10 min, 60 min, 4 h and 24 h post-injection. The percentage accumulated was higher in the lungs than in the other organs for both albumin and gelatin microspheres.     

原子吸收分光光度法测定明胶空心胶囊中铬需注意的几个问题

目的归纳总结原子吸收分光光度法测定明胶空心胶囊中铬需注意的问题,为检验人员提供参考。方法从样品的处理及所用试剂的选择、消解程序的选择及样品的制备、检测条件的选择及标准曲线的绘制等方面进行实验和探讨。结果与结论在实验过程中按照应注意的问题进行操作,能够绘制出线性良好的标准曲线,得到准确可靠的检测结果。     

The disintegration behaviour of capsules in fed subjects: a comparison of hypromellose (carrageenan) capsules and standard gelatin capsules

Two-piece hard shell capsules made from hypromellose (or hydroxypropyl methylcellulose, HPMC) containing carrageenan as a gelling agent have been proposed as an alternative to conventional gelatin capsules for oral drug delivery. We have previously compared the disintegration of hypromellose(carrageenan) (Quali-V(?)) and gelatin capsules (Qualicaps) in fasted human subjects using the technique of gamma scintigraphy. This second study used the same technique with both fasted and fed human subjects. Size 0 capsules were filled with powder plugs made from lactose and did not contain croscarmellose as in the original study. The capsules were separately radiolabelled with indium-111 and technetium-99m. Both capsules were administered simultaneously with 180ml water to eight healthy male subjects following an overnight fast. Each volunteer was positioned in front of the gamma camera and sequential 60s images were acquired in a continuous manner for 30min. The mean (±S.D.) disintegration time in the fasted state for the hypromellose(carrageenan) capsules was 8±2min and for gelatin 7±3min. These results were not statistically different from the data in the original study and show that the removal of the croscarmellose had no effect on the results. The mean (±S.D.) disintegration time in the fed state for the hypromellose(carrageenan) capsules was 16±5min and for the gelatin capsules was 12±4min. There was no statistical difference between the hypromellose(carrageenan) and gelatin capsules in either the fed or fasted state.     

Streptomycin sulphate microspheres: formulation and in vivo distribution

Abstract

Albumin and gelatin microspheres of streptomycin sulphate were formulated and their potential as a drug delivery system for a tuberculostatic agent in vivo was evaluated. Biodistribution was determined by i.v. administration of a ^99mTc-labelled microsphere suspension to mice. The radioactivity of the lungs was compared with the radioactivity of the liver, spleen, kidney and heart at 10min, 60min, 4h and 24 h post-injection. The percentage accumulated was higher in the lungs than in the other organs for both albumin and gelatin microspheres.