丁姜和胃贴膏组方药物超临界CO_2提取工艺研究

目的:研究丁姜和胃贴膏组方药物挥发性成分超临界CO_2提取最佳工艺。方法:以萃取率和丁香酚含量为指标,采用L9(34)正交设计试验方案,考察萃取温度、萃取压力及萃取时间对组方药物丁香、砂仁、生姜的影响。结果:超临界CO_2提取最佳条件为:萃取温度46℃,萃取压力35 MPa,萃取时间2.5 h。此时萃取物萃取率为3.916%,丁香酚含量为28.688%(m L/g)。结论:该工艺简便、高效,可为优化丁姜和胃贴膏的制备工艺提供参数。     

Retention strengths of five luting cements on prefabricated dowels after root canal obturation with a zinc oxide/eugenol sealer: 1. Dowel space preparation/cementation at one week after obturation

PURPOSE: This investigation examined the effect of 5 different cements on the retention strength of prefabricated endodontic dowels placed into root canals previously obturated with gutta percha and a zinc oxide/eugenol (ZOE) sealer. MATERIALS AND METHODS: Ninety-six single-rooted teeth were decoronated, filed, cleaned, sequentially shaped, and divided into 6 groups of 16 specimens each. Five of the groups were then obturated with gutta percha and a ZOE sealer. One group was not obturated and served as the control group. Dowel space preparation and dowel cementation for all groups were completed 1 week later. Ten-mm deep dowel spaces were prepared using size 6 Gates Glidden drills. Size 5 Paraposts were then cemented with 5 different cements: Panavia 21 for group 1 (unobturated controls) and group 2; Ketac-Cem glass ionomer for group 3; Fleck's zinc phosphate for group 4; Parapost (composite) Cement for group 5; and C&B Metabond 4-META for group 6. After 48 hours, the dowels were removed using a universal testing machine in tensile mode at 1 mm min(-1). RESULTS: The following results were found (all values in kg): group 1 (controls; Panavia 21) mean = 61.81, 95% CI = +/-8.65; group 2 (Panavia 21), mean=43.15, 95% CI = +/-7.81; group 3 (Ketac-Cem), mean =34.45, 95% CI = +/-4.93; group 4 (zinc phosphate), mean = 25.07, 95% CI = +/-5.03; group 5 (Parapost Cement), mean = 24.99, 95% CI = +/-5.35. None of the group 6 (C&B Metabond) specimens developed measurable bond strengths, so this group was excluded from parametric statistical analyses. An analysis of variance (ANOVA) showed a significant effect of group; pairwise multiple comparison procedures (Tukey test) showed that group 1 (controls) had significantly greater retention than all other groups (p <0.001); group 2 (Panavia 21) had significantly greater retention than groups 4 (zinc phosphate) and 5 (Parapost cement) (p <0.001). None of the other pairwise comparisons were statistically different. CONCLUSION: Paraposts cemented with Panavia 21 in unobturated root canals exhibited significantly higher retention than Paraposts luted with Panavia 21 and 4 different cements into dowel spaces prepared 1 week after obturation with gutta percha/ZOE sealer (p <0.001). Among the obturated groups, Panavia 21 cement (group 2) demonstrated significantly greater retention of Paraposts than zinc phosphate (group 4) and Parapost composite (group 5) cements (p <0.001). Ketac-Cem glass ionomer cement (group 3) had intermediate retention values that were not statistically different than those of groups 2, 4, and 5 (p >0.05). The 4-META cement, C&B Metabond, failed to polymerize.     

Eugenol delays the onset of ouabain-induced ventricular cardiac arrhythmias in guinea pigs

Eugenol is an aromatic compound used in the manufacture of medicines, perfumes, cosmetics and as an anaesthetic due to the ability of the drug to block the neuronal isoform of voltage-gated Na⁺ channels (Na_V). Some arrhythmias are associated with gain of function in the sodium current (I_Na) found in cardiomyocytes, and antiarrhythmic sodium channel blockers are commonly used in the clinical practice. This study sought to elucidate the potential mechanisms of eugenol's protection in the arrhythmic model of ouabain-induced arrhythmias in guinea pig heart. Ex vivo arrhythmias were induced using 50 μM of ouabain. The antiarrhythmic properties of eugenol were evaluated in the ex vivo heart preparation and isolated ventricular cardiomyocytes. The compound's effects on cardiac sodium current and action potential using the patch-clamp technique were evaluated. In all, eugenol decreased the ex vivo cardiac arrhythmias induced by ouabain. Furthermore, eugenol showed concentration dependent effect upon peak I_Na, left-shifted the stationary inactivation curve and delayed the recovery from inactivation of the I_Na. All these aspects are considered to be antiarrhythmic. Our findings demonstrate that eugenol has antiarrhythmic activity, which may be partially explained by the ability of eugenol to change de biophysical properties of I_Na of cardiomyocytes.     

丹皮酚、丁香酚、胡椒碱经皮微透析体内外回收率的研究

建立活血止痛膏中有效成分丹皮酚、丁香酚、胡椒碱微透析体内外回收率校正方法,为其经皮药动学研究提供依据。利用高效液相色谱法测定透析液中丹皮酚、丁香酚、胡椒碱的浓度,并计算微透析探针回收率;研究浓度、校正方法对3种成分微透析探针回收率的影响,并考察探针吸附性、体内外回收率的稳定性和重复性。结果表明,以30%乙醇生理盐水作为灌流液时,探针对3种成分均无明显的吸附,短时间内即可从探针上被完全洗脱下来;在8 h内,3种成分体内外回收率均能保持稳定;交替用含药溶液和空白灌流液灌流探针3次,3种成分体内外回收率基本不变。不同质量浓度丹皮酚(2.46~53.64 mg·L~(-1))、丁香酚(4.26~32.15 mg·L~(-1))和胡椒碱(5.75~45.87 mg·L~(-1))体外回收率分别为(45.7±4.66)%,(41.3±3.96)%,(27.82±2.95)%,即3种成分的探针回收率对浓度没有依赖性;在相同条件下,零净通量法、透析法和反透析法所测得的探针体外回收率几乎相等。因此,采集部位药物的浓度可用体外测得的回收率或在体回收率进行校正。同时也证明了该研究建立的微透析方法可用于活血止痛膏的经皮药动学研究。     

活血止痛微乳凝胶剂的体外释放和透皮吸收评价

目的:研究活血止痛微乳凝胶的体外释放和透皮吸收特性,为该制剂的研发提供参考。方法:采用改良Franz扩散池装置,分别以半透膜和离体小鼠皮肤为体外模型,采用UPLC同时测定接收液和皮肤中丹皮酚、丁香酚和水杨酸甲酯的含量,流动相乙腈(A)-0.1%甲酸水溶液(B)梯度洗脱(0~4 min,10%~90%A),检测波长280 nm,流速0.6 m L·min~(-1),进样量1μL。结果:活血止痛微乳凝胶中丹皮酚、丁香酚和水杨酸甲酯在6 h内的累积释放率分别为70.35%,59.40%,54.64%,释放速率分别为1.138,11.57,73.54μg·cm-2·h~(-1);体外透皮试验6 h累积透过率分别为40.34%,36.34%,41.44%,透过速率分别为0.657,7.127,56.04μg·cm-2·h~(-1)。结论:活血止痛微乳凝胶具有较好的体外释放和透皮性能,体外释放符合Higuchi方程,经皮渗透行为符合零级动力学方程。     

GC校正因子在黄樟醚、甲基丁香酚定量分析中的应用

目的:将GC校正因子应用于细辛中黄樟醚、甲基丁香酚定量分析。方法:首先采用Agilent 6890N气相色谱仪,FID检测器,DB-WAX毛细管柱(250μm×30 m,0.25μm),检测器温度250℃,进样口温度230℃,载气氮气,恒压模式,进样量1μL,流速1.0 m L·min~(-1),氢气流速45 m L·min~(-1),空气流速450 m L·min~(-1),尾吹氮气流速35 m L·min~(-1),温度条件(起始温度135℃保持2 min,以5℃·min~(-1)升至160℃保持7 min,再以20℃·min~(-1)升至220℃保持3 min);再通过不同测定及计算方法得多个GC校正因子值;最后经稳定性、重复性、加样回收率试验验证可行性,筛选校正因子值应用于黄樟醚、甲基丁香酚的定量分析。结果:各校正因子值计算稳定性、重复性试验结果 RSD均3%;黄樟醚平均加样回收率范围为92.96%~121.35%,RSD 3.4%~4.8%,甲基丁香酚为88.80%~112.54%,RSD 2.0%~3.4%;最终获得应用于10批细辛中黄樟醚、甲基丁香酚定量分析。结论:2个GC校正因子值定量分析10批细辛中黄樟醚、甲基丁香酚结果相差不大,多个GC校正因子值的筛选应用有利于提高实验检测结果的准确性。     

Surface antibacterial properties of glass ionomer cements used in atraumatic restorative treatment

BACKGROUND: Atraumatic restorative treatment (ART) is recommended for use worldwide, not only in developing countries where resources are not readily available, but also in more industrialized countries. The antibacterial properties of restorative dental materials may improve the restorative treatment outcome. Glass ionomer cement (GIC) has been advocated as the preferred restoration material for ART. The authors evaluated the antibacterial properties of restorative materials-three GICs and a zinc oxide eugenol (ZOE)-in vitro. METHODS: Streptococcus mutans, Actinomyces viscosus and Enterococcus faecalis were the test microorganisms. The authors used a quantitative microtiter spectrophotometric assay to evaluate the antibacterial effect of the restorative materials using the direct contact test (DCT) of freshly prepared and one-week-aged materials. RESULTS: The freshly prepared GICs and ZOE showed no bacterial growth in all tested bacteria compared with a control. This effect lasted for at least one week for S. mutans and A. viscosus but not for E. faecalis. CONCLUSIONS: Conventional GICs used in ART showed antibacterial surface properties against cariogenic bacteria for at least one week. Further study on the long-term antimicrobial effects of GICs is needed. CLINICAL IMPLICATIONS: The antimicrobial properties of freshly prepared restorative materials and aged restorative materials used in ART have a potent effect against cariogenic bacteria. These properties have crucial importance in preventing secondary caries.     

3种中草药单体治疗豚鼠皮肤马拉色菌感染的实验研究

目的:筛选出有效的抗马拉色菌的中草药单体.方法:采用连续7 d涂菌法诱导豚鼠皮肤感染马拉色菌,并将苦参碱、柠檬醛、丁香酚3种中草药单体参考品及酮康唑粉制成2%凡士林霜剂,采用自身对照法观察治疗后培养皿中的真菌菌落数、真菌转阴率.结果:连续用药4 d后,柠檬醛、丁香酚组菌落数明显少于阴性及空白对照组,并且柠檬醛组真菌转阴率与酮康唑组差异无统计学意义;连续用药7d后,3种实验药物组的菌落数及真菌转阴率均明显低于阴性对照组及空白对照组,而与酮康唑组差异无统计学意义.结论:苦参碱、柠檬醛、丁香酚在体内具有较强的抗马拉色菌作用.皮肤菌落计数是定量指标,更能反应药物的短期疗效.