哺乳妇女单次注射迪波盖司通~长效避孕针后血清和乳液中MPA浓度变化

目的:探讨中国妇女哺乳期使用迪波盖司通后血清和乳液醋酸甲羟孕酮(MPA)浓度变化。方法:10名产后哺乳妇女单次注射迪波盖司通(含MPA150mg),在注射后的第1、2、4、6、8、10和12周采集血样和乳液样本,用放射免疫方法测定MPA。结果:血清MPA浓度于注射后第1周最高,到第2、4周时下降明显,第4周后浓度下降趋势逐渐缓慢。乳液MPA浓度在第1周为最高,第2周比第1周降低了约1/2,之后10周平均浓度变化波动在5.09-8.15ng/ml之间。观察期间乳液/血清MPA浓度比值和曲线下浓度面积比值均为0.55。对象之间和同一对象不同时间点乳液/血清MPA浓度存在明显个体差异。结论:哺乳期使用迪波盖司通,将导致血液和乳液中含有一定量的MPA。     

大气细菌粒子浓度的时间分布特征及最佳采样时间的研究

用ＭＦ－４５型和ＨＴＫ－２０１型空气微生物采样器分别在北京、天津和沈阳三地观测了不同季节和一天中大气细菌粒子的浓度及其变化。结果表明：京、津二地春季大气细菌粒子浓度高，分别为２０５３个／ｍ３和２５５６个／ｍ３；夏季低，分别为９９５个／ｍ３和１０６４个／ｍ３。沈阳秋季大气细菌粒子浓度高，为１０１０８个／ｍ３；冬季低，为１２９４个／ｍ３。一天中，大气细菌粒子浓度呈双峰型变化，６：００～７：００和１８：００时大气细菌粒子浓度高，１１：００～１３：００和１：００～２：００时大气细菌粒子浓度低。根据大气细菌粒子浓度的季节变化和一天中大气细菌粒子浓度的时间分布特征，经过京、津、沈三地一天中分别１２次、８次、６次和４次不同采样时间组合的大气细菌粒子浓度的数理统计分析，大气细菌粒子浓度的监测拟集中在一年冬、春、夏、秋四季的中间月份，即１月、４月、７月、１０月进行；一天中采样８次的时间序列可为７：００、１０：００、１３：００、１６：００、１９：００、２２：００、１：００、４：００一天采样４次的时间序列可为５：００、１１：００、１７：００、２３：００。白天采样４次的时间序列可为春、秋季６：００、９：００、１２：００、１５：００?     

RP—HPLC测定人血浆中洛伐他汀浓度及药动学研究

用ＲＰ－ＨＰＬＣ测定人血浆中洛伐他汀浓度。以甲醇－水（８３∶１７，Ｖ／Ｖ）为流动相，色谱柱采用ＨＹＰＥＲＳＩＬＢＤＳ－Ｃ１８（５μｍ）不锈钢柱，紫外２３７ｎｍ波长检测。血浆样品经环己烷－异丙醇（９５∶５）萃取浓缩后进样测定。洛伐他汀浓度在２．５～８０ｎｇ／ｍｌ范围内线性良好，ｒ＝０．９９６８。测定含洛伐他汀２０．０ｎｇ／ｍｌ的血浆样品，其日内（ｎ＝７）及日间（ｎ＝７）的ＲＳＤ分别为９．８％和８．５％。回收率平均为（１０１．３±５．５）％。测定了１０名健康志愿者单次ｐｏ洛伐他汀片剂８０ｍｇ后不同时间的血药浓度，计算了相应的药动学参数。     

氧化胆固醇对动脉毒性作用的研究

将Wistar大鼠随机分成氧化胆固醇组(Och)、纯胆固醇组(Pch)和对照组,分别用氧化胆固醇混合物(250mg/kg bw/d)、纯胆固醇(250mg/kg bw/d)以及悬浮固醇用的明胶液体给大鼠灌胃,连续二天。于第二次灌胃后18小时,从大鼠尾静脉注射伊文思兰溶液,并于注射后2小时处死;取出主动脉用荧光显微分光光度术测定主动脉内膜的通透性。此外,另一部分动物在第二次灌胃后24小时处死,取出主动脉作扫描电镜的内膜观察。结果表明,Och大鼠主动脉内膜的通透性显著高于Pch组与对照组大鼠(P<0.01),而Pch组大鼠主动脉内膜的通透性和对照组无显著差异(P>0.05)。     

利培酮对氯氮平血浓度影响的研究

目的　了解利培酮对氯氮平血浓度的影响及二药合用的疗效与不良反应。方法　对 5 0例原服用氯氮平治疗的难治性精神分裂症患者合并利培酮治疗 ,分别于合并治疗前及后 1月、2月、3月测定氯氮平血浓度 ,同时评定PANSS ,TESS量表。结果　合用利培酮后 ,氯氮平血浓度无明显升高 ,PANSS评分明显降低(P <0 .0 1) ,TESS评分有所增加。结论　利培酮对氯氮平血浓度无明显影响 ,二药合用能增加疗效 ,不良反应有所增加。     

Inhibition of N-, P/Q- and other types of Ca channels in rat hippocampal nerve terminals by the adenosine A1 receptor

The effects of the adenosine A₁ receptor agonist, N⁶-cyclopentyladenosine (CPA), on both the increase in intracellular free Ca²⁺ concentration ([Ca²⁺]_i) and on the release of endogenous glutamate in rat hippocampal synaptosomes were studied. The inhibitory effect of CPA on the increase in [Ca²⁺]_i stimulated with 4-aminopyridine was neutralized by the adenosine A₁ receptor antagonist, 8-cyclopentyl-1,3-dipropylxanthine (DPCPX). The inhibitory effect of CPA was greater in synaptosomes from the CA1 subregion than in whole hippocampal synaptosomes. The inhibitory effects of both CPA and of the Ca²⁺ channel blockers, ω-conotoxin GVIA, ω-conotoxin MVIIC or ω-conotoxin GVIA plus ω-conotoxin MVIIC, were greater than those caused by the Ca²⁺ channel blockers. The release of endogenous glutamate was inhibited by 41% by CPA. The inhibition observed when CPA and ω-conotoxin GVIA or CPA and ω-conotoxin MVIIC were present was also greater than the inhibition by the Ca²⁺ channel blockers alone. The presence of both ω-conotoxin GVIA and ω-conotoxin MVIIC did not completely inhibit the release of glutamate, and CPA significantly enhanced this inhibition. The membrane potential and the accumulation of [

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]tetraphenylphosphonium of polarized or depolarized synaptosomes was not affected by CPA, suggesting that adenosine did not increase potassium conductances. The present results suggest that, in hippocampal glutamatergic nerve terminals, adenosine A₁ receptor activation partly inhibits P/Q- and other non-identified types of Ca²⁺ channels.     

高效液相色谱法测定人血清中丙戊酸钠的含量

建立了ＨＰＬＣ方法测定人血清中丙戊酸钠的药物浓度。采用反相柱和乙腈－水（６０∶４０）作为流动相，庚酸作为内标，血样经提取后，用４－溴甲基－６，７－二甲氧基香豆素衍生化，测定波长设在λＳ３２５ｎｍ和λＲ３９８ｎｍ，内标庚酸的保留时间为４．５７ｍｉｎ，丙戊酸钠的保留时间为５．２１ｍｉｎ，线性范围为２～１５０μｇ／ｍｌ。测定了１０名健康受试者单次口服丙戊酸钠片剂后不同时间的血药浓度。     

反相高效液相色谱法测定血浆中氢溴酸右美沙芬浓度

本文报道采用反相高效液相色谱法测定人血浆中氢溴酸右美沙芬的浓度。采用ＹＷＧ－Ｃ１８Ｈ３７分析柱，以乙腈－水－乙酸（５０：４９：１，三乙胺调节ｐＨ至４．３）为流动相，利多卡因作内标，在２７８ｎｍ波长处监测洗提液。本法简便，灵敏，专属性好，适用于氢溴酸右美沙芬血药浓度测定及药代动力学研究 。     

Prostaglandin D2 measurement in nasal secretions is not a reliable marker for mast cell activation in atopic patients

Background Prosia gland in D2 (PGD2) is a very important mast cell product during the early-phase nasal allergic reaction. However, the quantification of PGD2 in nasal secretions has not yet been well established. Objective Quantitative determination of PGD2 in nasal secretions of atopic patients (n=17) after nasal allergen challenge (NAC) and in non-allergic healthy volunteers (n=10). Methods The nasal microsuction sampling technique was used to obtain the nasal secretions with an exactly known and minimally diluted volume. A sensitive and specific enzyme immunoassay was chosen to measure the more stable 11-methoxime derivative of PGD2. which was obtained after extraction in acelone/ethanol and conversion using methoxamine-HCl. The concentrations of PGD2 in nasal secretions obtained from 10 non-allergic healthy volunteers were used as reference values. Results There was no significant difference in the concentrations of PGD2 between men (median: 569pg/mL) and women (median: 407pg/mL), nor between the baseline concentrations from atopic patients (median: 410pg/mL) and non-allergic controls (median: 477 pg/mL). In the atopic patient group, PGD2 did not significantly increase during the entire sampling period after NAC. The absence of PGD2 response contrasted with the nasal symptoms manifested by sneezing, increased nasal airway resistance, and the significant increases of the concentrations of histamine, tryptase, and leukotriene C4 (LTC4) 5min after NAC. Conclusion This observation suggests that the measurement of PGD2 alone in the nasal secretions does not give reliable information on mast cell activation during a nasal allergic reaction.     

33 factorial design-based optimization of the formulation of nitrofurantoin microcapsules

A microcapsule form of nitrofurantoin was prepared by a simple coacervation method with carboxymethylcellulose and aluminium sulfate. 3³ factorial design was performed for three independent variables, namely, the particle size of the drug, the size of the microcapsules and the pH of the dissolution medium. The dissolution tests with the formulated microcapsules were carried out according to the United States Pharmacopeia XXII rotating basket method at pH 1.2, 5 and 7.5, which represent the pH of gastrointestinal fluids. Release data were examined kinetically and the ideal kinetic models were estimated and t _63.2 values obtained from RRSBW distribution were used in the factorial design experiment. The influence of the independent variables on the dissolution of nitrofurantoin microcapsules could be expressed as the pH of the dissolution medium > particle size of the microcapsule > particle size of nitrofurantoin. The other aim of this study was to evaluate microcapsule formulation in terms of the United States Pharmacopeia criteria with a minimum of experiments. Our findings suggest that dosage forms which comply with the pharmacopoeia criteria for dissolution can be prepared and selected by factorial design.