影响主动载药法制备硫酸长春新碱脂质体包封率的因素

 目的采用主动载药法制备硫酸长春新碱脂质体,考察包封率的影响因素。方法采用阳离子交换树脂分离脂质体与游离药物,用HPLC测定包封率;考察了温度、pH调节剂、药脂比、包衣辅料及制备工艺对包封率的影响。结果脂质体的包封率随温度的升高而增加、随药脂比增大而降低、Na₂HPO₄最适合作pH调节剂;以pH梯度法和(NH₄)₂SO₄梯度法制备的脂质体包封率分别为86.9%,70.8%;加入聚乙二醇单甲醚2000胆固醇琥珀酸酯(methoxypolyethyeneglycol2000cholesterylsuccinate,CHS-PEG₂₀₀₀),包封率提高到92.8%,97.6%。结论主动载药法适于制备硫酸长春新碱脂质体;温度,pH调节剂和药脂比是影响包封率的重要因素。     

高效液相色谱法测定硫酸吗啡缓释栓含量

摘 要 目的： 制备硫酸吗啡缓释栓剂,采用高效液相色谱法测定硫酸吗啡缓释栓剂的含量。方法: 采用Eclipse XDB C18柱（150 mm×4.6mm,5μm）;以甲醇 庚烷磺酸钠醋酸溶液（取庚烷磺酸钠2.02 g,加水适量溶解,加冰醋酸5 ml,加水稀释至1 000 ml,摇匀）（50∶50）为流动相;流速为1.0 ml·min^-1;检测波长:233 nm;柱温:25℃;进样量:10 μl。结果: 3批样品中硫酸吗啡平均含量为99.9%,在4.18～86.60 μg·ml^-1浓度范围内线性关系良好(r=0.999 3),平均回收率100.6%,RSD=1.58%(n =9)。结论:该检测方法灵敏、快速、结果准确,适用于硫酸吗啡缓释栓剂质量控制。     

两种硫酸长春新碱脂质体包封率测定方法的比较

目的:建立两种测定硫酸长春新碱脂质体包封率的方法,并对测定结果进行比较.方法:分别以葡聚糖凝胶Sephadex G-50柱和阳离子交换树脂柱分离硫酸长春新碱脂质体和游离药物,采用HPLC法测定药物含量,计算包封率,并用SPSS软件进行t检验.结果:两种方法测定不同药脂比的硫酸长春新碱脂质体包封率,测定结果无显著性差异.结论:葡聚糖凝胶柱法的建立需详细考察凝胶的种类对分离度的影响;阳离子交换树脂法分离度良好,分离速度快,为优选的方法.     

Acute irritant contact dermatitis: recovery time in man

Our understanding of the details of the recovery time of acute irritant contact dermatitis (ICD) is limited. We examined skin reactivity to a model surfactant, sodium lauryl sulfate (SLS). on previous acute ICD and normal sites over time with visual grading and noninvasive instruments. Acute ICD was induced on the upper arms of 18 volunteers (aged 30 to 51 years) by occluded application of 1% SLS for 24 h. Previous ICD and normal sites were provoked by occluded application of 2% or 7.5% SLS 30 min daily 4 consecutive days. Skin reactivity was assessed daily by visual erythema scoring (VES), transepidermal water loss (TEWL), skin color reflectance (SCR) and electrical capacitance (EC). Skin function of previous ICD sites assessed, by VES, TEWL. SCR, and EC did not normalize until 2 weeks later: all parameters of previous ICD returned to normal after 3 weeks. While skin reactivity to 2% und 7.5% SLS showed no differences between previous ICD and normal sites at 4 weeks, differences of irritant reactivity especially 7,5% SLS between previous ICD and normal sites were significant at 3 weeks post-provocation. Our results demonstrate that irritation evaluated with irritant provocation was long-lasting, even though skin functional parameters assessed by various bioengineering instruments returned to normal. Complete recovery of skin function including irritability after acute ICD induced by 1% SLS was achieved approximately 4 weeks later. The date were generated with a model surfactant: it remains to be determined whether similar responses will be noted with chemicals of different physicochemical properties.     

围术期输注硫酸镁对全麻术后吗啡用量的影响

目的观察围术期输注硫酸镁对全麻术后吗啡用量的影响。方法选择40例ASAⅠ-Ⅱ级,拟在全麻下行全子宫切除术的患者,随机分为对照组(NS组)和硫酸镁组(MG组)。MG组术前静脉给予25%MgSO4负荷剂量25mg/kg(即0·1ml/kg),继以200mg/h持续输注至术后48h。NS组给予同等容量的生理盐水以同样技术予以输注。术后应用吗啡静脉自控镇痛(PCIA),记录患者首次要求镇痛的时间(患者主观VAS评分>4cm时),术后4、8、18、24、48h疼痛评分(VAS)、镇静评分(OAA/S)、吗啡用量及术后恶心、呕吐情况。结果从手术结束到患者首次要求镇痛的时间,MG组30·2±5·2min比NS组20·0±4·3min显著延长(P<0·01)。MG组术后48h内吗啡的总用量22·8±4·8mg,显著低于NS组27·0±6·8mg(P<0·01)。术后恶心呕吐的发生率MG组与NS组分别为10%和30%(P<0·05)。结论全麻下行子宫切除术的病人,围术期输注硫酸镁可延长患者术后首次要求镇痛的时间,减少术后48h内吗啡的用量及术后恶心呕吐的发生率。     

大剂量氯吡格雷对选择性经皮冠状动脉介入术的影响

目的 研究大剂量氯吡格雷用于选择性经皮冠脉介入治疗（PCI）患者的疗效及安全性.方法 确诊冠心病并接受择期PCI的患者173例,分成氯吡格雷强化组（波立维600 mg,87例）和氯吡格雷标准组 （波立维300 mg,86例）.PCI治疗前两组患者分别给予波立维600 mg和波立维300 mg治疗;PCI术后每日分别给予150 mg和75 mg,共 7 d;以后均服用波立维75 mg至1年以上.观察两组患者的疗效及不良反应的发生情况.结果 氯吡格雷强化组和氯吡咯雷标准组达到的完全血运重建率分别为93.8% 和 87.2%（P＜0.05）;两组主要不良心脑血管事件（MACCE）发生率分别为2.0%和6.8%,差异均有统计学意义（P＜0.01）;而出血和血管并发症的发生率差异无统计学意义（1.6%比1.7%,P＞0.05）.结论 氯吡格雷强化组PCI的疗效和安全性均优于氯吡格雷标准组.     

Simplified determination of serum cholesterol sulfate by gas-liquid chromatography combined with cyclohexylsilane-bonded phase column purification

Summary A new gas-liquid chromatographic (GLC) determination of cholesterol sulfate (CS) and dehydroepiandrosterone sulfate (DHEAS) for a biochemical diagnosis of recessive X-linked ichthyosis (RXLI) is described. Although the GLC method for determination of CS is known to be more sensitive than the thin layer chromatographic (TLC) method, the former method has not been widely employed because of its complicated pre-purification steps. The present method allows us to measure the serum levels of CS and DHEAS without tedious purification steps such as multiple conventional column chromatography and preparative thin layer chromatography. Sulfated steroids are rapidly purified with a commercially available mini disposable cyclohexylsilane-bonded phase (CH) column, CH BOND ELUT, and the purified steroids after desulfation are converted to water-resistant tert-butyldimethylsilyl ether derivatives for the GLC analysis on dual 2 m glass columns packed with 2% XE-60 on Chromosorb W.By the present method, serum CS concentrations in RXLI patients were shown to be about 10 times higher than those in patients with ichthyosis vulgaris, carriers of RXLI, and healthy subjects. This method is more suitable not only for a biochemical diagnosis of RXLI but also for studies on the metabolism of sulfated steroids than the previous time-consuming GLC methods.     

HPLC法测定硫酸头孢匹罗的含量及有关物质

目的:建立硫酸头孢匹罗含量及其有关物质的HPLC检测方法.方法:采用Lichrospher-C18色谱柱(250 mm×4.6 mm,5 μm);流动相为 0.03 mol·L-1磷酸二氢铵缓冲液(pH3.3)-乙腈(9:1),流量 1.0 mL·min-1,检测波长 270 nm.结果:硫酸头孢匹罗在149.1～347. 9 μg·mL-1浓度范围内线性关系良好(r=0.9999),与中间体1、中间体2及副产物完全分离,中间体1和中间体2的最低检测浓度分别为 27.2 ng·mL-1、25.8 ng·mL-1.结论:本测定法简便快速,灵敏度高,准确可靠,可同时测定硫酸头孢匹罗的含量及有关物质.     

Capacitively coupled electrical stimulation of bovine growth plate chondrocytes grown in pellet form

Pellets formed from isolated bovine growth plate chondrocytes were grown in various capacitively coupled electrical fields. The signals chosen were 0, 10, 100, 250, 500, 750, 1,000, and 1,500 V peak-to-peak, 60 kHz. The effect on cell proliferation and matrix production of these different voltages was determined by [3H]thymidine and [35S]sulfate uptake, respectively, Cyclic AMP assays were done to determine if increases in either thymidine or sulfate uptake were associated with changes in cAMP levels. Significantly increased cell proliferation occurred at 500, 750, and 1,000 V peak to peak. The calculated electric fields were 1.5 to 3.0 x 10(-2) V/cm. Proliferation was significantly inhibited at 1,500 V peak-to-peak with a calculated field of 4.5 x 10(-2) V/cm. Little if any change was seen in cAMP levels at 30 or 60 min following application of the appropriate electric signals.     

Human cutaneous irritation: induced hyporeactivity

The variation in human skin response to sodium lauryl sulfate (SLS) was determined with patch and open applications. Reactions in different subjects and in multiple simultaneous patch tests were compared. Skin responses were assessed with visual scoring (VS), laser Doppler velocimetry (LDV) and transepidermal water loss (TEWL). Previous open, unpatched SLS exposure decreased patch test reactivity to 1% SLS assessed with VS (p less than 0.05) or LDV (p less than 0.05). Corresponding TEWL alteration was inconstant. Variation in reactivity at different test sites in multiple simultaneous tests was considerable, though less than the variation at different test times (p less than 0.05). Inter-subject variation in test reactivity was greater than the variation between different test times or adjacent test sites. Repeated open applications and the subclinical dermatitis appear to have produced a hyporeactive state. The results suggest that non-specific skin inflammation is elicited by multiple factors, e.g., stratum corneum integrity and vascular reactivity. Their balance determines the ensuing reactions. The induced hyporeactivity may be one of many causes of false negative diagnostic patch tests.