褶合光谱法应用于增效联磺片的定量

本文应用计算机辅助褶合光谱分析法，不经分离，同时分别测定了增效联磺片中ＳＭＺ、ＳＤ和ＴＭＰ三组分的含量，平均回收率和ＲＳＤ分别为９９．２５％，０．４３％；１００．４４％，０．２９％；９９．８１％，０．２０％。     

褶合光谱－PLS法同时测定安痛定注射液3组分含量

通过褶合变换获得褶合光谱，以此为基础，结合应用偏最小二乘（ＰＬＳ）法，同时测定安痛定注射液中氨基比林、安替比林及巴比妥的含量，方法简便，结果满意。平均回收率和ＲＳＤ依次分别为：９９．８４％，０．１５％；９９．８７％，０．２１％及１００．２７％，０．３９％。     

替硝唑片剂的HPLC和UV测定

采用ＨＰＬＣ和ＵＶ法测定替硝唑片剂的含量，其线性范围和平均回收率分别为：ＨＰＬＣ法６０～１００．μｇ／ｍｌ，９９．５６％（ＲＳＤ０．８８％）；ＵＶ法５～２５μｇ／ｍｌ，９９．７０％（ＲＳＤ０．５４％）。方法准确可靠。     

卡尔曼滤波分光光度法同时测定替硝唑含漱液三组分含量

本文研究了卡尔曼滤波分光光度法同时测定替硝唑含漱液中三组分：替硝唑、达克罗宁、地塞米松，结果各组分平均回收率分别为１００．１％，１００．８％和９９．３％，ＲＳＤ分别为０．８３％，０．７７％和１．４７％。     

对乙酰氨基酚溶液的HPLC测定

采用ＨＰＬＣ法以十八烷基硅烷键合硅胶为固定相，甲醇－０．０５ｍｏｌ／Ｌ醋酸铵溶液（１５：８５）为液动相，茶碱为内标，测定对乙酰氨基酚溶液的含量。测得４种处方的回收率分别为９９．６、９９．７、１００．５及１００．１％，ＲＳＤ分别为０．９４、１．１９、０．２３和０．５０％。     

高效液相色谱法测定复方氯霉素酊中氯霉素和水杨酸的含量

本文采用高效液相色谱法同时测定复方氯霉素酊中氯霉素和水杨酸的含量，方法简单、快速、准确。用对乙酰氨基酚为内标物，氯霉素的方法回收率为９９．９％，ＲＳＤ＝０．８９％（ｎ＝５）；水杨酸的方法回收率为１００．０％，ＲＳＤ＝０．５４％（ｎ＝５）。     

扑苯黄片中三组分的HPLC测定

用ＨＰＬＣ同时测定扑苯黄片中三组分的含量。采用Ｓｐｈｅｒｉｓｏｒｂ ＣＮ柱，操作简单，结果准确。对乙酰氨基酚、盐酸伪麻黄碱、盐酸苯海拉明的回收率分别为１００．３％、９９．８％、９９．５％，ＲＳＤ分别为０．２９％、０．５１％、０．４５％。     

反相高效液相色谱法测定复方土槿皮酊中水杨酸和苯甲酸的含量

本文报道了反相高效液相色谱法测定复方土槿皮酊中水杨酸和苯甲酸含量，以对氨基苯甲酸为内标，该法简便、快速，每个样品测试在１０ｍｉｎ内完成。其中水杨酸平均回收率为１００．８５％，变异系数为０．１９％；苯甲酸平均回收率为９９．５０％，变异系数为０．２４％。     

联立方程组的新解法在测定复方利凡诺溶液中的应用

本文报道了分光光度法中联立方程组新解法在复方利凡诺溶液中的应用，用吸收度比值代替吸收系数，不仅简便了测定方法，而且提高了方法的准确度。其中：λ１：２５５ｎｍ，λ２：２７８ｎｍ；αβ：０．１９；两组分回归系数皆为：０．９９９９；方法回收率分别为利凡诺：１００．３２％，ＲＳＤ：０．６３％，间苯二酚：９９．６５％，ＲＳＤ：０．１６％。     

复方环丙沙星栓的系数倍率测定

采用系数倍率法测定复方环丙沙星栓中环丙沙星和甲硝唑的含量。方法简单、快速，结果准确，其平均回收率分别为９９．３３％和１００．７０％，ＲＳＤ分别为０．７７％和０．４５％。     

Accumulation of radiolabelled low molecular peptides and proteins in experimental inflammation

This study focuses on evaluating accumulation of the low molecular peptides and proteins labelled with 99mTc in rat inflammatory/infection foci. Peptides (human leukocyte dialysate, HLD; thymosin fraction 5, TF5; aprotinin, APT), and proteins (human IgG, HIG) were labelled with 99mTc using redox polymer. The labelling efficiency was evaluated using paper, TLC and/or column chromatography. Biodistribution of labelled substances was evaluated in rats with Staphylococcus aureus infection or with sterile kaolin suspension inflammation 24 h after abscess induction. Accumulation of 99mTc activity was determinated both by external gamma camera imaging and by counting dissected tissues 4 h after administration. The evaluated peptides and proteins show high labelling efficiency (99mTc-HLD>98%, 99mTc-TF5>95%, 99mTc-APT>98%, 99mTc-HIG>95%). Usage of redox polymer for labelling increases the stability of 99mTc-labelled substances. The labelling efficiency stays nearly the same (95-98%) after 8 h at least. In experimentally induced inflammation the amount of 99mTc-peptides and 99mTc-HIG activity accumulated is 2.5-6.5 and 5.3-10.6 times higher than in a control tissue. When comparing two types of model inflammations (kaolin- and Staphylococcus-induced ones), the values measured with 99mTc-peptides are more than double than those of kaolin suspension inflammation. The studied low molecular peptides labelled with 99mTc allow rapid localisation of infection foci. 99mTc labelled HIG proved useful for detection of infections and inflammatory lesions.     

五价锝标记化合物在缺血性心肌中的摄取与其离解性

目的：研究在机体内具有一定的稳定性而又能离解出可达靶组织的活性形式ＴｃＯ４＾３－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：＾９９ｍＴｃ＾５＋－ｓｕｃｃｉｍｅｒ为０，＾９９ｍＴｃ＾５＋ＧＨ为２８．１％±１．３％，＾９９ｍＴｃ％５＋－ＰＰｉ为４６．０％±２．９％，而缺血３ｈ     

In vitro validation of 99mTc-HFA-FP delivered via pMDI-spacer.

The purpose of the study was to label Flixotide (fluticasone propionate [FP] with HFA propellant), with technetium-99m and validate that (99m)Tc acts as a suitable marker for FP when delivered via pMDI-spacer. Sodium pertechnetate was mixed with 5 mL of butanone. (99m)Tc was extracted into butanone and transferred into an empty canister. The (99m)Tc lined canister was heated, and the butanone evaporated to dryness. A supercooled commercial Flixotide canister was decrimped, and the contents transferred to the (99m)Tc lined canister and recrimped. The particle size distribution of FP and (99m)Tc from 10 radiolabeled canisters was measured using an Anderson cascade impactor calibrated to 28.3 L/min, and compared to commercial FP. The drug (FP) content of each particle size fraction was measured using ultraviolet spectrophotometry and the (99m)Tc level in each fraction was measured using an ionization chamber. The percentage of particles in the fine particle fraction (<;4.7 microm) and the percentage of (99m)Tc from commercial and radiolabeled canisters were compared. The mean (SD) % FP in the fine particle fraction, before and after label was 43.2 (1.8) % and 43.9 (2.6) %, respectively. The mean (SD) % (99m)Tc in the fine particle fraction was 42.1 (5.1) %. The mean %FP exiting spacer at (<4.7 microm) before labeling was not significantly different from the mean % FP exiting spacer at (<4.7 microm) after labeling (p > 0.05). The mean % (99m)Tc attached to particles at (<4.7 microm) after radiolabeling was not significantly different from the mean % FP levels (p > 0.05). The validation in this study indicates that (99m)Tc can act as a suitable marker for HFAFP, delivered via pMDI-spacer.     

The Absorption of 99mTc-alendronate Given by Rectal Route in Rabbits

Alendronate sodium (ALD) is a bisphosphonate medication used in the treatment and prevention of osteoporosis. Absorption of ALD as oral formulation is very poor (0.5%–1%). Its bioavailability can decrease with food effect. It has some gastrointestinal adverse effects such as gastritis, gastric ulcer, and esophagitis. The aim of this study was to develop a rectal formulation of ALD as an alternative to oral route and to investigate the absorption of it by using gamma scintigraphy. For this reason, ALD was labeled with Technetium-99m (^99mTc) by direct method. The radiochemical characterization of the ^99mTc-ALD was carried out by paper chromatography, thin layer chromatography, and electrophoresis methods.

The labeling efficiency of ^99mTc-ALD was found 99% without significant changes until 6 h postlabeling at room temperature. The rectal suppositories containing ^99mTc-ALD were prepared by fusion method using polyethylene glycol (PEG) 1500. The ^99mTc-labeled ALD suppositories were administrated to rabbits by rectal route. Serial scintigrams over all bodies of the rabbits were obtained at different time intervals using a gamma camera. We found that the rectal absorption of ^99mTc-ALD from suppository formulation was possible. According to our results, this formulation of ALD can be suggested for the therapy of osteoporosis as an alternative route.     

Effects of Sodium Taurocholate on the Absorption of Inhaled 99mTc-DTPA

Purpose The effects of a natural surface-active agent, sodium taurocholate (NaTC), on the absorption of a hydrophilic solute, technetium-99m-labelled diethylene triamine pentaacetic acid (^99mTc-DTPA), deposited at various sites within the airways were evaluated in this open, cross-over, and single-dose study.Methods Nine healthy non-smokers received ^99mTc-DTPA with or without the addition of NaTC, administered as an oropharyngeal aerosol and as nebulized large and fine droplet-sized pulmonary aerosols delivered by Pari and UltraVent nebulizers inhaled at fairly rapid and slow flows, respectively. Plasma concentration versus time profiles and 24-h urinary excretion of radioactivity were assessed. Further, ^99mTc-labelled human serum albumin nanocolloidal particles (^99mTc-Nanocoll) were administered with or without NaTC by Pari and followed by repeated chest γ-imaging.Results NaTC changed no pharmacokinetic parameters for oropharyngeal ^99mTc-DTPA. Independent of intrapulmonary ^99mTc-DTPA deposition pattern, NaTC reduced T _max (Pari: −0.8 h; UltraVent: −1.5 h) and mean absorption time (MAT) (−0.4 h; −0.7 h), and increased bioavailability (+13%; +44%) and dose-adjusted C _max (+54%; +103%). NaTC decreased the pulmonary ^99mTc-Nanocoll disappearance half-life from 8 h and 45 min to 4 h and 19 min.Conclusions Our findings suggest that NaTC increases both rate and extent of ^99mTc-DTPA absorption throughout the lower airways, without changing ^99mTc-DTPA absorption in the oral cavity.     

99mTc-HL91和Tl-201双核素心肌显像在冠心病中的初步临床研究

目的 探索^99mTc-HL9乏氧心肌显像在冠心病中的可行性及临床应用价值。方法3例急性心肌梗塞,1例不稳定性心绞痛连续病例行Tl-201和^99mTc-HL9双核素心肌显像，比较两种核素心肌显像、阳性节段数以及匹配方式。结果 ^99mTc-HL9可以提供较清晰的乏氧心肌图像并用于心肌节段分析；3例急性心肌梗塞，1例不稳定性心绞痛患共68个节段。Tl-201判断为阳性节段23个，占34％；^99mTc-HL9判断为阳性节段36个，占53％；24小时Tl-201延迟显像显示为可逆性分布7个节段，^99mTc-HL91均呈阳性显像；^99mTc-HL9比Tl-201多判断出13个阳性节段，占19％。双核素心肌显像有4种匹配方式：Tl-201正常^99mTc-HL9无显像，25个节段；Tl-201正常^99mTc-HL9显像。20个节段；Tl-201异常^99mTc-HL9显像，16个节段；Tl-201异常／99mTc-HL91无显像，7个节段。即刻Tl-201显像示23个异常节段。其中16个节段呈^99mTc-HL9阳性显像，占70％，24小时Tl-201延迟显像显示有7个(部分)可逆性节段。占30％，^99mTc-HL9检测缺血，存活心肌的能力显高于Tl-201(P=0．008)。结论^99mTc-HL9可以用于冠心病的心肌乏氧成像并用于心肌节段分析．乏氧显像为研究冠心病提供了新的手段。尚需大样本的临床研究。     

Synthesis,Characterization, and Preclinical Evaluation of 99mTc‐Labeled Macrobicyclic and Tricyclic Chelators as Single Photon Emission Computed Tomography Tracer

The novel tetraaza macrobicyclic chelator 3,6,9,15‐tetraazabicyclo[9.3.1]pentadeca‐1(15),11,13‐triene‐2,10‐dione (TBPD) and pentaaza macrotricyclic chelator 9‐oxa‐3,6,12,15,21‐pentaazatricyclo[15,3,2,1]trieicos‐1(21),17,19‐triene‐2,7,11,16‐tetradione (OPTT) were synthesized, characterized, and radiolabeled with ^99mTc to produce ^99mTc‐TBPD and ^99mTc‐OPTT. These radiolabeled complexes were prepared with high radiolabeling yield, radiochemical purity, and good in vitro stability up to 24 h. The labeling efficiency of ^99mTc‐TBPD and ^99mTc‐OPTT was found 98% and 97%. In vitro serum stability of ^99mTc‐TBPD was found to be 95.2%, while that of ^99mTc‐OPTT 94.2% up to 24 h. Blood kinetics experiments of ^99mTc‐labeled complexes showed biphasic pattern of blood clearance. About 99.57 ± 0.89% activity of ^99mTc‐TBPD and 99.42 ± 0.88% activity of ^9mTc‐OPTT were cleared off blood stream at 24 h postadministration. The biological half‐life of ^99mTc‐TBPD was observed: t_1/2(F) 1 h 5 min and t_1/2(S) 12 h and biological half‐life of ^99mTc‐OPTT was observed: t_1/2(F) 1 h 10 min and t_1/2(S) 9 h 50 min, respectively. The biodistribution studies revealed that maximum uptake of ^99mTc‐TBPD was found in liver, concluded that excretory pathway is hepatobiliary, while that of ^99mTc‐OPTT was renal as well as hepatobiliary. The negligible activity observed in stomach confirming the stability of radiolabeled complex in biological milieu. In vitro cytotoxicity study of TBPD and OPTT did not show any considerable antiproliferative activity against cancer cells of human cervical SW756, HeLa, and glioblastoma U‐87, U373 cell lines.     

吲达帕胺胶囊的研制与质量控制

目的 :研究吲达帕胺胶囊的制备及其质量控制方法。方法 :含量测定采用紫外分光光度法 ;有关物质检查采用高效液相色谱法。结果 :吲达帕胺在3 7～11 1μg/ml浓度范围内线性关系良好 ,r=0 9997,回收率为99 50% ,精密度为0 43% ;有关物质检查精密度为0 1%。考察3批样品 ,相对百分含量分别为99 07%、99 34%、99 58 % ;每批样品随机取10粒 ,所测得的含量均匀度A +1 80S值均小于15;有关物质均小于1 %。结论 :以本方法制备的吲达帕胺胶囊 ,主药和辅料混合均匀 ,含量及有关物质符合相关规定 ,质控方法可靠。     

Synthesis and biological characterization of 99mTc(I) tricarbonyl cysteine complex,a potential diagnostic for assessment of renal function

Cysteine containing three functional groups, i.e. a carboxyl, sulfhydryl, and amino group, has been labelled with ^99mTc(I) tricarbonyl precursor ( 2 ) in order to study the renal characteristics of the resulting ^99mTc(I) tricarbonyl cysteine ( 3 ) versus the reference ^99mTc‐MAG₃ ( 1 ). The ^99mTc(I) tricarbonyl cysteine ( 3 ) was prepared in good yields and characterized by HPLC, eletrophoresis, and eletrospray mass spectrometry. The plasma protein binding rate of ^99mTc(I) tricarbonyl cysteine ( 3 ) was about 70 to 80%, and similar to that of ¹³¹I‐OIH (70%) but lower than that of ^99mTc‐MAG₃ (90%). The T_1/2 of ^99mTc(I) tricarbonyl cysteine (4.30±0.79 min) in the kidney was higher than the one of ^99mTc‐MAG₃ (2.43±0.70 min). The static image of ^99mTc(I) tricarbonyl cysteine at 5 min post injection showed high concentrated activity in the kidney. And in the 15, 30 min post injection images, most activity appeared in the bladder without a residue in other organs. The ^99mTc(I) tricarbonyl cysteine exhibited biological behavior comparable to ^99mTc‐MAG₃ and it is expected to have diagnostic potential for imaging renal function in nuclear medicine. Copyright © 2004 John Wiley & Sons, Ltd.     

A study of 99mtechnetium-labelled beclomethasone dipropionate dilauroylphosphatidylcholine liposome aerosol in normal volunteers

^99mTechnetium (^99mTc) was bound to preformed beclomethasone dipropionate (Bec) dilauroylphosphatidylcholine (DLPC) liposomes (Bec-DLPC) in the presence of the reducing agent, stannous chloride. Labelling efficiency was 96–99% as determined by micropartition and chromatographic analysis. Andersen cascade impactor analysis showed close correlation of the distribution of ^99mTc, DLPC, and Bec over the full range of particle sizes sampled. In mouse biodistribution studies, approximately one-half of ^99mTc activity delivered to the lungs was retained at 24 h. ^99mTc clearance was almost exclusively via the gastrointestinal tract. In contrast, free ^99mTc (administered unbound to Bec-DLPC) liposomes was cleared from mouse lungs within a few minutes. Six normal volunteers inhaled 20 breaths of the labelled Bec-DLPC liposome aerosol from each of two nebulizers (Aerotech II, MMAD 1.5μ, GSD 2.4) (Spira, MMAD 3.6μ, GSD 2.5). Immediately following inhalation, the gamma camera analysis showed 17% pulmonary deposition of inhaled ^99mTc-Bec-DLPC with the Aerotech II and 14% with the Spira nebulizer. At 3 h after Aerotech II exposure, 93% of deposited activity was retained in the lung and 82% was retained from the Spira nebulizer. These findings suggest that there is a stable association of ^99mTc with the Bec-DLPC liposomes and that inhaled liposomes were cleared slowly from the lungs of normal volunteers. The smaller particles produced by the Aerotech II nebulizer are presumably responsible for the somewhat larger deposition and longer persistence of pulmonary activity. These findings encourage further study of this modality of treatment for asthma and related conditions.