一阶导数光谱法测定丙吡胺尿药浓度及其缓释片的相对生物利用度

本文报道了用导数光谱法测定磷酸丙吡胺的尿药浓度,本方法能消除尿中杂质干扰,测定结果准确。6名受试者交叉口服磷酸丙吡胺缓释片和普通片,测得尿药浓度计算消除速度常数K,排泄速率(Δx/Δt)_(max) 所需时间,证明缓稀片药物排泄慢,药效维持时间长,且缓释片的相对生物利用度与普通片基本相同。     

活性金属单环165的临床研究

不锈钢环型节育器(金单环)在中国广为应用。为提高金单环的避孕效果,进行了金单环支撑力与脱落关系的研究,对200,165,135g不同支撑力进行比较性研究筛选出较为合理的支撑力为165g,其外形和金单环相似,分大、中、小三种型号,大号外径22mm,中号21mm,小号为20mm。外层为不锈钢丝螺旋簧,在螺旋环内相间置入纯铜丝(200mm2)和消炎痛硅橡胶各二段(消炎痛总含量5mg左右,现已改为10mg)。于1988年10月～1989年6月全国南北方7省市11所医院共放置1000例,经3年定期随访,12,24,36个月继续存放率各为92.5,88.99及85.94/100妇女年,36月累积带器妊娠率仅1.61/100妇女,脱落率比原金单环明显降低近40％,因症取出率为3.12。于放置前后进行月经血量测量24例,放置后3、6月各增加24.4％和27.4％。行子宫内膜“含铜含药组”和“有铜无药”组对照检查各11例,含药组炎症细胞略少。作宫颈粘液中铜离子含量测定,以6月内含量较高,6月后趋向平稳。消炎痛释放测定,1月内释放较快,一年后残留20％左右。经1249例临床观察,活性金单环165是一种不需特殊培训易于推广的、安全、经济并能长期放置的IUD。     

广西武鸣华侨农场心血管病危险因素的调查研究

对广西武鸣华侨农场4158人进行基线普查,410人进行膳食调查和作8小时夜尿电解质测定,并将高血压低发区广西的资料与高发区的北京作对比.结果显示,体重指数高是高血压一个重要的危险因素,而体重过重又与膳食中摄入碳水化合物和总热量大有关.另一主要的危险因素是钠,膳食中摄入钠高,尿Na和Na/K比值高者,血压水平和高血压的患病率亦高.     

Orthogonal solid-phase synthesis of a monobiotinylated analog of Neuropeptide Y

Analogs of Neuropeptide Y (NPY) were synthesized with conventional Boc/benzyl protective group strategy. Instead of Asn⁷ in the native scquence, Boc-Lys(Alloc)-OH was incorporated. At the end of the synthesis the Alloc group was selectively removed by palladium-catalyzed hydrostannolysis and biotin coupled to the e-amino group of Lys⁷. After cleavage and characterization with plasma desorption mass spectrometry the N^e-7-biotinyl-[Lys⁷]-NPY and the nonbiotinylated analog [Lys⁷]-NPY were investigated as ligands to the NPY receptor from rat cerebral cortex. Both analogs were found to be high affinity ligands to the NPY receptor and bound with essentially the same affinity as unmodified NPY.     

高压液相色谱纯化肾综合征出血热病毒血凝素及其性状分析

用吐温８０－乙醚（ＴＥ）法、蔗糖－丙酮（ＳＡ）法、丙酮－乙醚（ＡＥ）法分别从肾综合征出血热病毒（ＨＦＲＳＶ）感染的Ｖｅｒｏ－Ｅ６细胞培养和乳小白鼠脑组织中制备病毒血凝素（ＨＡＮ），定量对比证明其制备效果，结果无明显差异。粗制ＨＡＮ经高压液相色谱（ＥＰＬＣ）纯化，有４个洗脱峰，血凝活性物质存在于峰１。纯化ＨＡＮ在ＳＤＳ－ＰＡＧＥ中呈单一区带，分子量５６．６ＫＤ，ＨＡＮ相对含量７９．６％。纯化ＨＡＮ在蔗糖密度梯度液中有一条１．１５～１．１６ｇ／ｃｍ３的沉淀，粗制ＨＡＮ有３条沉淀。电镜观察纯化ＨＡＮ中为大小相等的球状颗粒。粗制ＨＡＮ的高密度沉淀中可见到病样颗粒。对几种常用消毒剂、氧化剂、去垢剂对ＨＡＮ的灭活作用做了实验对比观察。     

PHA RMA COKINETICS OF CUPRIC－BIS（SALICYLALDEHYDE－2－FURA NTHIOCA RBOXY－HYDRAZONATE） DICHLORIDE（CSFTCH） IN RABBITS

ＰＨＡＲＭＡＣＯＫＩＮＥＴＩＣＳＯＦＣＵＰＲＩＣ－ＢＩＳ（ＳＡＬＩＣＹＬＡＬＤＥＨＹＤＥ－２－ＦＵＲＡＮＴＨＩＯＣＡＲＢＯＸＹ－ＨＹＤＲＡＺＯＮＡＴＥ）ＤＩＣＨＬＯＲＩＤＥ（ＣＳＦＴＣＨ）ＩＮＲＡＢＢＩＴＳ￥ＧａｏＹｕｎｓｈｅｎｇ；ＺｈｕＹｕｙｕｎ（...     

An alkylpolyglucoside surfactant as a prospective pharmaceutical excipient for topical formulations: The influence of oil polarity on the colloidal structure and hydrocortisone in vitro/in vivo permeation

There is a growing need for research into new skin- and environment-friendly surfactants. This paper focuses on a natural surfactant of an alkylpolyglucoside type, which can form both thermotropic and lyotropic liquid-crystalline phases. The aim of this study was to relate some physicochemical properties (characterised by polarisation and transmission electron microscopy, thermal analysis and rheology) of the three formulations based on cetearyl glucoside and cetearyl alcohol, to the results of in vitro and in vivo bioavailability of hydrocortisone (HC). The three formulations contained oils of different polarity (medium chain triglycerides: MG, isopropyl myristate: IPM and light liquid paraffin: LP), respectively. In vitro permeation was followed through the artificial skin constructs (ASC), while the parameters measured in vivo were erythema index: EI (using instrumental human skin blanching assay), transepidermal water loss (TEWL) and stratum corneum hydration (SCH). The vehicles based on cetearyl glucoside and cetearyl alcohol showed a complex colloidal structure of lamellar liquid-crystalline and lamellar gel-crystalline type, depending on oil polarity. Rheological profile of the vehicle was directly related to the in vitro profile of the HC permeation. In vivo results suggested that the vehicle with MG retarded the HC permeation, whereas less polar IPM and non-polar LP enhanced it. It is suggested that the enhancement is achieved either by a direct interaction with lipid lamellae of the SC or indirectly by improving skin hydration.

There were no adverse effects during in vivo study, which indicates a good safety profile of this alkylpolyglucoside surfactant.     

颈椎侧块钢板在脊髓型颈椎病治疗中应用

目的 对15例脊髓型颈椎病患者行后入路椎管减压、椎板成型术的同时使用颈椎侧块钢板固定，探讨和分析该手术方法的优点和手术治疗效果。方法 从自2000年3月—2002年12月，对15例脊髓型颈椎病患者(术前颈椎MR显示有三个节段颈椎椎间盘水平病变并有黄韧带增厚突入椎管)，行颈椎后入路双开门椎板成型术加双侧颈椎侧块钢板固定。按JOA评分法评定患者手术前后恢复情况。结果 本组患者男10例，女5例，随访5个月—1年2个月，平均9个月，术后2—7天(平均3．5天)可戴颈围坐起，颈围外固定时间12周，融合时间3—5个月，(平均为3．5个月)，术后JOA评分明显提高，所有病人无术中血管、神经根损伤，无植骨不愈合，无内固定断裂。结论 行颈椎后入路双开门椎板成型术联合应用颈椎侧块钢板固定，从后方扩大椎管容积，对脊髓进行减压，辅助以侧块钢板对减压后的颈椎行即时的稳定的固定，增加后方所植髂骨的融合成功率，大大地减少颈椎术后后突畸形发生和术后卧床并发症的发生率。     

城市污灌废水的致突变性检测及色谱/质谱分析

应用Ames致突变试验,对比研究了武汉市易家墩、黄孝河污灌区污灌废水与土壤的致突变性。同时应用色谱/质谱(GC/MS)分析技术。测定了主要污水中有机污染物的化学组成。结果表明:罗家渠废水的致突变活性最强;受各条污水灌溉的土壤的致突变活性顺序与相应废水的强弱顺序一致;罗家渠废水中致突变致癌物主要是萘、联苯等。     

Combined treatment with a 5HT1A receptor agonist and a muscarinic acetylcholine receptor antagonist disrupts water maze navigation behavior

The present study was designed to investigate the effects of combined treatment with a serotonin (5-HT)_1A receptor agonist, 8-hydroxy-2-(dipropylamino)-tetralin (8-OH-DPAT), and a muscarinic acetylcholine receptor antagonist, scopolamine, on water maze (WM) navigation. Treatment with either 8-OH-DPAT or scopolamine before daily behavioral training disrupted spatial navigation at medium doses and cue navigation at high doses. Pretraining treatment with a combination of subthreshold doses of 8-OH-DPAT and scopolamine impaired WM spatial and cue navigation, but did not impair the WM performance if the drugs were injected post-training. In trained rats, combined injections of subthreshold doses of 8-OH-DPAT and scopolamine given pretraining did not impair the rats' ability to find the platform in a familiar or in a novel position. The combination of 8-OH-DPAT and scopolamine also disrupted WM navigation in rats with central 5-HT depletion. A combination of a peripheral muscarinic acetylcholine receptor antagonist and 8-OH-DPAT had no effect on WM navigation. These data suggest that combined treatment with drugs blocking muscarinic acetylcholine receptors and activating 5-HT_1A receptors greatly impairs WM learning/performance, but does not impair spatial memory per se.