长效避孕皮下埋植剂体外缓释行为研究

本文对以加成型硅橡胶为基质的左旋18—甲基炔诺酮长效避孕埋植剂的体外释放行为及对可能影响其释放量的诸因素,进行了观察与研究,结果表明:此长效避孕皮下埋植剂的体外释药行为,符合零级释药动力学规律。释药量受控释膜厚度,控释膜交联密度及释药面积的影响。体外释放药物曲线无明显爆破峰。     

Characterisation of pre- and post-synaptic α-adrenoceptors in modulation of the rat ileum longitudinal and circular muscle activities

Previous study has shown that α_2D-adrenoceptors are involved in modulation of peristalsis in the rat ileum. The aim of the present study was to determine the tissue location of α-adrenoceptors in the rat ileum by using a recently devised method. The pre-synaptic α-adrenoceptors were characterised by measuring the potencies of agonists to inhibit transmurally-evoked (1 ms pulses, 10 Hz, 8-10 s trains) contractions of the longitudinal and circular muscles and the affinities of antagonists. Post synaptic α-adrenoceptors were identified by screening agonists and antagonists in carbachol-contracted tissues. In the circular muscle the order of potencies for inhibiting transmurally-induced contraction was: clonidine ≥ oxymetazoline ≥ UK 14,304 ≥ guanfacine > talipexole > phenylephrine > azepexole. The potency ratios relative to clonidine correlated to those previously derived using the rat ileum peristaltic reflex preparation. Most of the α-adrenoceptor agonists, however, caused only small inhibitions of the longitudinal muscle contraction in response to transmural stimulation, except phenylephrine and azepexole. RX 821002, yohimbine, rauwolscine, BRL 44408, phentolamine, idazoxan, ARC 239, and prazosin inhibited the effect of clonidine on the circular muscle response with apparent pK_B values best correlated with pK_B or pK_i values derived from the rat ileum peristaltic reflex preparation and other tissues known to have the α_2D-subtype. The rank order of potencies at inhibiting carbachol-induced responses of both muscle layers was: phenylephrine ≥ oxymetazoline > clonidine ≥ talipexole > azepexole >> guanfacine. UK 14,304 was inactive up to 10 μM. The EC₅₀ value of each agonist on the longitudinal muscle was not significantly different to the corresponding value on the circular muscle. Prazosin was more potent than yohimbine at inhibiting the relaxant effect of phenylephrine in both muscle layers of carbachol-contracted tissues. It is concluded that the recently identified α_2D-adrenoceptors of the rat ileum are located on cholinergic neurons controlling circular muscle contraction. The study also demonstrated the presence of postsynaptic α₁-adrenoceptors involved in mediating relaxation in both muscle layers. Received: 4 November 1996 / Accepted: 10 April 1997     

人晶体上皮细胞的体外培养

目的:提供一种简单可行,易于掌握的体外培养人晶体上皮细胞的方法。方法:用无齿显微镊子将晶体囊膜分离出来,剪碎后直接移至细胞培养瓶中培养,当细胞长出融合后,用胰蛋白酶消化传代。结果:接种培养4天后,可见晶体上皮细胞开始长出,并以贴壁方式生长。结论:用此方法体外培养人晶体上皮细胞,具有简单、快捷、成功率高的优点。眼科学报1997;13:170—172。     

粉被虫草提取物对巨噬细胞吞噬功能及CTL活性的影响

研究粉被虫草菌丝体提取物在体外对小鼠腹腔巨噬细胞吞噬功能和脾细胞免疫功能的影响，结果表明：粉被虫草提取物在正常情况下不仅能够促进小鼠腹腔巨噬细胞的吞噬功能，而在免疫抑制的情况下，一定浓度的粉被虫草菌丝体提取物还能恢复提高吞噬功能；它不仅能促进正常脾活化Ｔ细胞的增殖，而且能恢复环磷酰胺和氢化可的松抑制免疫小鼠脾活化Ｔ细胞的增殖；在较高浓度下能增高小鼠脾细胞毒Ｔ淋巴细胞（ＣＴＬ）活性，同时在一定浓度下能恢复免疫抑制小鼠脾ＣＴＬ活性。     

几种脑积水分流方法的临床评价(附75例报告)

目的总结75例不同病因引起脑积水的3种分流方法，以评价其临床疗效。方法分析75例脑积水形成的病因手术方法、手术结果、术后并发症等。结果除颅内肿瘤（5例）及术后癫痫致颅内出血（2例）共死亡7例外，手术疗效满意。但术后并发症以脑室心房分流术及脑室腹腔分流术后分流管堵塞的发生率较高。结论根据不同手术指征，选择不同分流方法，改进分流管，可减少手术损伤及术后分流管堵塞引流不畅等并发症。     

小儿先天性巨结肠42例手术疗效分析

手术治疗小儿先天性巨结肠４２例，其中Ｄｕｈａｍｅｌ术９例，Ｓｗｅｎｓｏｎ术１１例，Ｓｏａｖｅ术６例，Ｒｅｈｂｅｉｎ术１０例，直肠后壁肌切除４例，直肠肛管纵切心形斜吻合术２例。术后污粪、便秘、小肠结肠炎及肛门狭窄发生率２１％。认为：手术疗效是与术前充分准备，选择适宜术式，术中精细操作，术后加强护理，精心喂养等直接相关     

Pharmacokinetics of Controlled Release and Immediate Release Morphine Sulphate Tablets after a Single Dose and Multiple Doses in Chinese Volunteers

健康志愿者１０名，随机交叉口服硫酸吗啡控释片（ＣＲＭＳ）３０ｍｇ（３０ｍｇ×１）和硫酸吗啡普通片（ＩＲＭＳ）２０ｍｇ（１０ｍｇ×２），分别于服药前后各时点取静脉血，用ＧＣＭＳ测定血浆中吗啡含量。以药代软件程序处理，分别求得ＣＲＭＳ和ＩＲＭＳ的Ｃｍａｘ为１９．３８±３．８０和２１．２７±６．２１ｎｇ／ｍｌ；ｔｍａｘ为２．３６±０．３７ｈ和０．５５±０．１６ｈ；ｔ１／２β为３．５３±０．８７ｈ和３．０３±０．７４ｈ，曲线下面积ＡＵＣ为１４５．１５±１７．６５和９３．０８±１６．６５ｎｇ·ｈ／ｍｌ。癌症病人多次口服硫酸吗啡至稳态，ＣＲＭＳ和ＩＲＭＳ的峰浓度分别为２７．４３±０．３３ｎｇ／ｍｌ，２２．６８±０．１６ｎｇ／ｍｌ；谷浓度分别为１９．４５±１．４４ｎｇ／ｍｌ；１８．１４±０．４９ｎｇ／ｍｌ。     

氮唑取代苯基醚类衍生物的合成及其抗真菌活性

通过取代溴苄与１－（２，４－二取代苯基）－２－（１Ｈ－吲哚和苯并咪唑－１－基）乙醇反应，合成了一系列１－｛２－「（取代苯基）甲基」－２－（取代苯基）乙基－１－吲哚和苯并咪唑类新化合物，并用二倍体稀释法对化合物进行了体外抗真菌试验。