苦参素注射液的人体药动学

目的：建立测定苦参素血药浓度的HPLC法并研究苦参素注射液在健康人体内的药物动力学。方法：18名健康男性受试者，肌注300mg药物后，采用HPLC法测定血药浓度，用3p87软件经微机处理药－时数据。结果：苦参素注射液的体内过程符合二室模型。结论：此法提供了苦参素注射液在健康人体中的药动学数据。     

口服抗病毒新药——缬更昔洛韦

缬更昔洛韦 (valganciclovir)是抗病毒药更昔洛韦的前体药物 ,用于治疗AIDS病人发生的巨细胞病毒 (CMV)视网膜炎。缬更昔洛韦口服后迅速吸收 ,并水解为更昔洛韦 ,其口服给药的生物利用度较高 (60 % )。试验表明 ,口服缬更昔洛韦 (90 0mg)与静脉注射更昔洛韦 (5mg·kg-1) ,bid,3wk后改为 qd ,治疗 1 60例AIDS病人发生的CMV视网膜炎有相同疗效 ,且耐受性相似。缬更昔洛韦维持治疗中最常见的不良反应为中性粒细胞减少症、贫血、胃肠道反应 (腹泻、恶心、呕吐 )、发热、头痛和失眠等     

Involvement of adenosine A1 and A2A receptors in the motor effects of caffeine after its acute and chronic administration.

The involvement of adenosine A(1) and A(2A) receptors in the motor effects of caffeine is still a matter of debate. In the present study, counteraction of the motor-depressant effects of the selective A(1) receptor agonist CPA and the A(2A) receptor agonist CGS 21680 by caffeine, the selective A(1) receptor antagonist CPT, and the A(2A) receptor antagonist MSX-3 was compared. CPT and MSX-3 produced motor activation at the same doses that selectively counteracted motor depression induced by CPA and CGS 21680, respectively. Caffeine also counteracted motor depression induced by CPA and CGS 21680 at doses that produced motor activation. However, caffeine was less effective than CPT at counteracting CPA and even less effective than MSX-3 at counteracting CGS 21680. On the other hand, when administered alone in habituated animals, caffeine produced stronger motor activation than CPT or MSX-3. An additive effect on motor activation was obtained when CPT and MSX-3 were coadministered. Altogether, these results suggest that the motor-activating effects of acutely administered caffeine in rats involve the central blockade of both A(1) and A(2A) receptors. Chronic exposure to caffeine in the drinking water (1.0 mg/ml) resulted in tolerance to the motor effects of an acute administration of caffeine, lack of tolerance to amphetamine, apparent tolerance to MSX-3 (shift to the left of its 'bell-shaped' dose-response curve), and true cross-tolerance to CPT. The present results suggest that development of tolerance to the effects of A(1) receptor blockade might be mostly responsible for the tolerance to the motor-activating effects of caffeine and that the residual motor-activating effects of caffeine in tolerant individuals might be mostly because of A(2A) receptor blockade.     

茯苓萜类的高效液相色谱指纹图谱研究

目的 建立茯苓三萜化合物的指纹图谱。方法 反相高效液相色谱法。结果 道地药材茯苓及不同地区收集的市场商品具有相当稳定的、相似程度很高的指纹图谱。结论 可利用液相色谱的特征峰控制茯苓及其制剂的质量。     

宫颈癌盆腔淋巴结转移相关因素分析

目的 :了解子宫颈癌盆腔淋巴结转移的相关因素。方法 :对 3 0 5例ⅠA～ⅡB期宫颈癌行根治术的临床资料进行回顾性分析。结果 :ⅠA期宫颈癌盆腔淋巴结转移率 0 ,ⅠB期为 9 8% ,ⅡA期为 18 5 2 % ,ⅡB期为 5 7 14 % ;宫颈鳞癌盆腔淋巴结转移率为 8 2 % ,宫颈腺癌为42 2 7% ;宫颈癌高分化组盆腔淋巴结转移率为 0 ,中分化组为 11 16% ,低分化组为 40 62 % ;宫颈间质浸润深度 <1/ 2组盆腔淋巴结转移率为 1 2 3 % ,≥ 1/ 2组为2 1 88% ;宫颈癌糜烂型盆腔淋巴结转移率为 17 0 2 % ,外生型为 13 95 % ,内生型为 18 5 2 % ,溃疡型为 41 67% ;宫颈肿瘤≥ 4cm者盆腔淋巴结转移率为 2 0 0 % ,<4cm者为 12 14 % ;手术前予化疗者盆腔淋巴结转移率为 7 4% ,未行化疗者为19 5 6% ;手术前行放疗者盆腔淋巴结转移率为 4 76% ,未行放疗者为 19 5 6%。结论 :宫颈癌患者的临床分期、病理分级、组织类型、宫颈间质浸润深度、生长方式及术前化疗或放疗与盆腔淋巴结转移有直接关系 ,而肿瘤大小与盆腔淋巴结转移关系不明显。     

5-Fu、MTX、VP16-213联合方案治疗恶性妊娠滋养细胞肿瘤的研究

目的 探讨5-Fu、MTX、VP16—213联合化学治疗恶性妊娠滋养细胞肿瘤患者的疗效。方法 对1992年4月至2003年4月11年本院91例恶性妊娠滋养细胞肿瘤(包括侵蚀性葡萄胎和绒癌)患者采用5-Fu、MTX、VP16—213三联化疗方案治疗，其中绒癌36例，有2例为复发性绒癌；侵蚀性葡萄胎(侵葡)55例。Ⅰ期16例，Ⅱ期26例，Ⅲ期56例。结果 91例患者中，采用此三联化疗方案治疗有86例获治愈，总治愈率高达94．51％。此三联化疗方案的主要毒副反应是骨髓抑制和胃肠道反应，其中Ⅲ～Ⅳ度粒细胞减少占27．3％，Ⅲ～Ⅳ度血小板减少占7．4％，Ⅲ度恶心呕吐占19．80%，Ⅲ度腹泻占2．4％，Ⅰ度肝功损害占2．1％，在19．69％的疗程中发生口腔溃疡，其中Ⅲ度占8．36％。结论 5-Fu、MTX、VP16—213联合方案治疗恶性妊娠滋养细胞肿瘤可达满意的临床效果，对其他药物耐药或复发病例也可获得满意的疗效。     

Efficacy of preoperative intracavitary brachytherapy and surgery in patients with stage ⅠB2 and ⅡA bulky cervical cancer

Objective To analyze the outcomes of preoperative intracavitary brachytherapy plus sur-gery in patients with stage ⅠB2 and ⅡA bulky cervical cancer. Methods From January 2001 to January 2007, 77 patients with stage ⅠB2 and ⅡA bulky cervical cancer were included. The diameter of primary tumor was greater than 4 cm. Preoperative intracavitary brachytherapy with the total dose of 20-30 Gy (0.5 cm below the vaginal mucosa) was delivered by 2-3 fractions, one fraction per week. After an interval of 10-14 days, the efficacies of radiotherapy were evaluated and radical hysterectomy with pelvic lymphade-nectomy was performed. Then the treatment complications, clinicopathological characteristics, survival and recurrence were analyzed. Results The tumor shrinkage was observed in all the patients after intracavitary brachytherapy. The CR, PR and SD were 5% (4/77), 36% (28/77) and 58% (45/77), respectively. Radical hysterectomy was successfully performed in all patients. The complications of the combined therapy were mild and only 5 patients had grade Ⅱ or less hematological or gastrointestinal toxicities. The 5-year o-verall survival rate and pelvic recurrence rate were 83% and 12%, respectively. Conclusions Preoperative intracavitary brachytherapy of 20-30 Gy plus surgery is effective in the treatment of stage ⅠB2 and ⅡA bulky cervical cancer without increasing the treatment complications.     

趋化因子受体CCR5在食管上皮癌变过程中作用的初步探讨

目的　探讨 CC趋化因子受体 5 (CCR5 )是否介导食管上皮炎性病变与其癌变过程的关系。方法　用免疫组化检测 40例食管鳞状细胞癌 (SCC)、癌旁炎症、不典型增生组织及 10例正常食管黏膜的 CCR5表达情况。结果　食管 SCC的 CCR5表达阳性率高于正常黏膜、慢性炎症及不典型增生的表达率 (P<0 .0 5 )。在 CCR5表达阳性的食管 SCC中 ,癌间质的单核淋巴细胞 CCR5阳性表达率分别低于癌旁炎症的单核淋巴细胞 CCR5阳性表达率(P<0 .0 5 )。结论　 CCR5在食管癌变进程中表达呈升高趋势 ,提示食管 SCC细胞可能通过表达 CCR5受体与间质浸润的单核细胞、淋巴细胞共同竞争趋化因子配体 ,从而实现了食管 SCC发生进程的免疫逃逸现象     

99mTcN(NOEt)2与99mTc-MIBI在肿瘤模型显像中的对比研究

目的　探讨99mTc 氮 二 (N 乙基 N 乙氧基二硫代氨基甲酸盐 ) [99mTcN (NOEt) 2 ]应用于肿瘤诊断的可能性并与99mTc 甲氧基异丁基异腈(99mTc MIBI)肿瘤模型显像进行比较。方法　制备99mTcN (NOEt) 2 ,用上行薄层色谱法测定放化纯。各取 4只移植性艾氏腹水癌小鼠分别尾静脉注射99mTc MIBI或99mTcN(NOEt) 2 ,30min、2h、4h后进行全身后位静态显像。利用感兴趣区技术 ,分别计算不同时相肿瘤与头部 (T/H)、胸部 (T/C)、及健侧肢体对称部位 (T/L)的放射性比值。 4h后处死99mTcN (NOEt) 2 显像组小鼠 4只 ,取血并剥离脏器组织及肿瘤组织 ,称重 ,测量放射性计数 ,计算肿瘤与各脏器放射性比值。结果　99mTcN (NOEt) 2 室温下 4h保持稳定。99mTcN (NOEt) 2 选择性地有效的聚集于肿瘤组织。除腹部外其它组织靶 /非靶比值较高 ,注射2h后T/L比值达最高 ,为 4.87。99mTcN (NOEt) 2 显像组与99mTc MIBI显像组比较T/L比值差异有显著性 (P <0 .0 1)。体外测量肿瘤与血、肌肉、肺等脏器的单位重量放射性比值较高 ,与肝、小肠等腹部脏器的单位重量放射性比值较低。结论　在移植性艾氏腹水癌小鼠模型中99mTcN (NOEt) 2 从血液中清除很快 ,肿瘤摄取率高 ,有一定的滞留量 ,靶与非靶比值高 ,图像质量明显优于99mTc MIBI肿瘤     

Superselective microcoil embolization of a traumatic pseudoaneurysm of the cavernosal artery

According to the literature, straddle injuries of the perineum may result in arteriosinusoidal fistula and secondary high-flow priapism. We report a case of a 23-year-old man who developed a traumatic pseudoaneurysm of the cavernosal artery, secondary to straddle injury, and presented with painless priapism. It was treated successfully with superselective microcoil embolization and the priapism resolved.