目的:研究复方甘菊利多卡因(Compound Chamomile and Lidocaine,CCL)对口腔溃疡的促愈合作用及发挥临床治疗作用的可能药理机制.方法:化学灼烧法建立新西兰兔口腔溃疡动物模型,每日各组分别涂抹CCL、成纤维生长因子(basic fibroblast growth factor,bFGF)3次,记录口腔溃疡面积;3、5、7d取溃疡组织固定,HE染色进行组织病理学观察;免疫组化检测各组IL-8、TNF-α和SOD的表达差异.抑菌环实验评价CCL对金黄色葡萄球菌、大肠埃希菌的抑菌能力.结果:CCL对兔口腔溃疡的促愈合作用不明显,7 d CCL组溃疡区虽可见增生的移行上皮层,结缔组织内仍见大量炎症细胞;但免疫组化显示,CCL组中IL-8,SOD表达水平接近bFGF组,均显著低于空白对照组(P<0.05);抑菌环实验显示,CCL对金黄色葡萄球菌和大肠埃希菌的抑菌作用与金霉素相当,与bFGF凝胶相比具有绝对的抑菌优势(P<0.001).结论:除了具有明确的止痛作用外,降低某些炎症因子的表达及加强局部的抗感染能力可能是CCL发挥临床治疗作用的主要机制.

目的 制备羧甲基化白及多糖-壳聚糖载姜黄素聚电解质复合膜,进行处方、制备工艺优化,并进行质量评价.方法 对白及多糖进行羧甲基化修饰,羧甲基化白及多糖与壳聚糖通过静电结合形成水不溶性复合物.以姜黄素为模型药物,采用溶剂挥发法制备载药聚电解质复合膜;通过单因素和正交设计法进行处方优化,用扫描电子显微镜和显微红外光谱对复合膜的形态和结构进行表征.结果 最优处方为羧甲基白及多糖117 mg,壳聚糖233 mg,甘油含量为25％,姜黄素为20 mg.平均厚度为(74.0±2.0)μm,载药量为95.41％,体外累积释放率可达93.78％.结论 优化条件下制备的载药复合膜外观光滑平整,分布均匀,载药量和累积释放度良好.

The original teaching of clinical pharmacy for stomatology course did not let students aware of the importance of drugs in the treatment of oral diseases. The original teaching framework was rearranged:decentralizing knowledge of oral diseased related clinical pharmacy into several mod-ules;setting general knowledge into the oral basic medical module;adding the practice of visiting the pharmacy and manufacturing laboratory. Teaching process was closely combined with clinics and was integrated with disease-centered oral medicine curriculum integration system. Students responded that the teaching effect was better. The rearranged teaching method can enhance students' attention on drug treatment for oral diseases,improve their ability of clinical medication and promote the teaching quality.

To combine the theory teaching and clinical practice medicine knowledge effectively through adding noviciate in Clinical Pharmacy of Stomatology ,enhance the ability of using oral clinical medica-tion ,make up for the inadequacy of domestic existing oral teaching curriculum model .

目的 研究复方碘甘油的质量标准.方法 采用氯化铜法鉴别复方碘甘油中的丙三醇;并采用HPLC-ELSD测定其丙三醇的含量.结果 氯化铜法鉴别丙三醇现象明显,重复性强,阴性无干扰.丙三醇含量在2.0124 ～7.5465 μg范围内呈现良好的线性关系,r=0.9998,平均回收率为96.30％,RSD为1.31％.结论 本方法准确,易行,重复性好,为复方碘甘油的质量标准研究提供依据.

目的建立利用UHPLC-MS/MS法同时测定大鼠血浆中Gomisin D、Gomisin E、五味子醇甲、五味子甲素、Gomisin R和五味子乙素6种木脂素的分析方法,并研究大鼠灌胃给予五味子提取物后的药代动力学特征。方法采用Agilent Poroshell 120 EC-C18色谱柱,流动相为乙腈-0.1%甲酸水溶液梯度洗脱,采用电喷雾电离源（ESI）,扫描方式为多反应离子监测（MRM）。结果大鼠血浆中6种木脂素成分的校正曲线线性关系良好,日内、日间精密度和准确度符合要求,提取回收率75.76%~88.82%。结论该方法简便、快速、灵敏、稳定,适用于五味子提取物的体内分析,为其进一步研究奠定基础。

An HPLC method was established for the determination of chlortetracycline hydrochloride,dyclonine hydrochloride and prednisone acetate in compound chlortetracycline film.A Diamonsil C18 column was used,with the mobile phase of acetonitrile︰0.2% phosphoric acid by gradient elution at the detection wavelength of 254 nm.The calibration curves for chlortetracycline hydrochloride,dyclonine hydrochloride and prednisone acetate were linear in the ranges of 40.0-120.0,15.0-45.0 and 5.0-15.0 ug/ml,respectively.Their average recoveries were 101.0%,100.1% and 100.3%,with RSDs of 0.91%,1.3% and 1.1%,respectively.

口腔临床药物学是现代药学与口腔临床医学相结合的产物,对于口腔专业学生来说是十分必要且重要的一门学科.口腔临床药物学课程的设置就是为了帮助学生在临床上能够做到合理正确地使用药物.这门课程的设计需要理论与实践相互结合,对于教师来说,既要给学生传授基础知识和基本技能,还要培养学生在实践中应用知识的能力.人民出版社出版的《口腔临床药物学》(第4版)教材中,第十七章到第十九章是在前面章节不同类型药物的理论学习基础上,介绍针对口腔不同疾病包括牙体牙髓病、牙周病及口腔黏膜病的临床用药[1].如果说前面章节的学习是让口腔医学专业的学生了解一些常用药物的基本知识,那么后面3章则是教会学生将知识用于临床实践.

目的:建立大鼠血浆中决明子特有蒽醌类成分的超高效液相色谱-串联质谱(UPLC-MS/MS)分析方法,并对其在大鼠体内药动学进行研究.方法:大鼠ig决明子浸膏(5 g/kg)后,分别于0、5、10、20、30、45 min和1、2、3、4、6、8、12、24 h取血样,以UPLC-MS/MS法测定血浆中橙黄决明素、黄决明素、决明素和1-去甲基决明素的质量浓度.色谱柱为Agilent Poroshell 120 EC-C18,流动相为乙腈-30 mmol/L乙酸铵水溶液(梯度洗脱),流速为0.4 ml/min,柱温为30℃;质谱采用多反应监测(MRM),用于定量分析的离子对依次为:m/z 343.0→298.1(橙黄决明素)、m/z 359.0→286.0(黄决明素)、m/z 329.0→271.1(决明素)、m/z 343.0→242.0(1-去甲基决明素)和m/z 239.0→211.0(1,8-二羟基蒽醌).结果:橙黄决明素、黄决明素、决明素、1-去甲基决明素回归方程分别为y=0.034x-0.019(r=0.999 9)、y=0.034x+0.139 (r=0.999 9)、y=0.009x+0.136 (r=0.999 9)、y=0.066x+0.380(r=0.999 9),橙黄决明素质量浓度在3.24～1 296 ng/ml、黄决明素质量浓度在0.77～618 ng/ml、决明素质量浓度在34.55～1 818 ng/ml、1-去甲基决明素质量浓度在1.86～1 485 ng/ml范围内与其峰面积和内标峰面积比值呈良好线性关系.橙黄决明素、黄决明素、决明素、1-去甲基决明素的药动学参数t1/2分别为(9.28±0.12)、(8.69±0.57)、(8.28±0.51)、(7.01±0.62)h,cmax分别为(210.28±4.16)、(46.18±1.91)、(119.30±9.74)、(109.28±3.09) μ.g/L,AUC(0-t)分别为(1668.17±62.18)、(265.30±44.39)、(357.81±15.11)、(540.92±19.57) μg/(L·h).结论:所建立的大鼠体内决明子蒽醌类成分的测定方法灵敏度高、专一性好,可用于决明子蒽醌类成分的体内药动学研究.

A sensitive and reliable ultra-high-performance liquid chromatography-electrospray ionization-tandem mass spectrometry (UHPLC-MS/MS) method was developed and validated for the simultaneous determination of four active components of Semen Cassiae extract (aurantio-obtusin, chrysoobtusin, obtusin and 1-desmethylobtusin) in rat plasma after oral administration. Chromatographic separation was achieved on an Agilent Poroshell 120 C18 column with gradient elution using a mobile phase that consisted of acetonitrile-ammonium acetate in water (30 mm) at a flow rate of 0.4 mL/min. Detection was performed by a triple-quadrupole tandem mass spectrometer in multiple reaction monitoring mode. The calibration curve was linear over a range of 3.24-1296 ng/mL for aurantio-obtusin, 0.77-618 ng/mL for chrysoobtusin, 34.55-1818 ng/mL for obtusin and 1.86-1485 ng/mL for 1-desmethylobtusin. Inter- and intra-day assay variation was <15%. All analytes were shown to be stable during all sample storage and analysis procedures.

Objective:To observe the effect of Shegan Mahuang drug-pair on airway inflammation and peripheral blood Thl/Th2 balance in OVA-induced asthmatic Balb/c mice.Method:80 female Balb/c mice were divided into 8 groups randomly,namely the normal control group,the asthmatic model group,the dexamethasone group,the Shegan group,the Mahuang group,and the drug-pair groups with different proportions of Shegan and Mahuang(n = 10 in each group).Asthmatic mouse model was established by intraperitoneal injection of ovalbumin.After the treatment,the number of eosinophil and leucoyte in bronchoalveolar lavage fluid(BALF) were counted.The ELISA was employed to detect the contents of IL-4,IL-5,IL-13 and IFN-γin peripheral blood,and the inflammatory state in lung tissue was evaluated with hematoxylin-eosin(HE) staining.Result:The levels of eosinophils and leucoyte in BALF were declined in drug-pair groups.The levels of IL-4,IL-5 and IL-13 in peripheral blood were reduced while IFN-γwas increased in drugpair groups,which showed significant differences when compared with the Shegan group and Mahuang group.Conclusion:Shegan Mahuang drug-pair could be applied to treat asthma by relieving the asthmatic symptoms,decreasing airway inflammation and modulating the Thl/Th2 imbalance.

在高等教育改革大背景下,全面提升我国高等医学教育教学质量势在必行。本文提出了在《口腔临床药物学》教学工作中引入"以口腔疾病为中心"的课程讲授及"以问题为中心"的教学方法等,期望有助于学生的系统学习,提高口腔医学教育的质量,适应教育改革的总体形势。

AIM To study the hot melt extrusion to improve the baicalin dissolution in Angong Niuhuang Dispersion.METHODS Poloxamer-188 and polyethylene glycol 6000 were adopted as hydrophilic carrier.Ethanolic extract,from Gardeniae Fructus,Scutellariae Radix,Coptidis Rhizoma and Curcumae Radix,and carriers mingled with each other in the proportion of 1∶ 4 to prepare the physical mixture as compared with the mixture made in hot melt extrusion,and made the comparison between them in the differential scanning calorimetry spectrum and the cumulative dissolution curves.RESULTS The dissolution results showed that the 20 min cumulative dissolution of baicalin in both the two solid dispersion reached 90%,but hot melt extrusion was significantly better than the physical mixture.CONCLUSION Hot melt extrusion can improve the dissolution of insoluble components like baicalin in Angong Niuhuang Dispersion.

A sensitive and reliable ultra-high performance liquid chromatography-electrospray ionization-tandem mass spectrometry has been developed and partially validated to evaluate the quality of Semen Cassiae (Cassia obtusifolia L.) through simultaneous determination of 11 anthraquinones and two naphtha-γ-pyrone compounds. The analysis was achieved on a Poroshell 120 EC-C(18) column (100 mm × 2.1 mm, 2.7 μm; Agilent, Palo Alto, CA, USA) with gradient elution using a mobile phase that consisted of acetonitrile-water (30 mM ammonium acetate) at a flow rate of 0.4 mL/min. For quantitative analysis, all calibration curves showed perfect linear regression (r(2) > 0.99) within the testing range. This method was also validated with respect to precision and accuracy, and was successfully applied to quantify the 13 components in nine batches of Semen Cassiae samples from different areas. The performance of developed method was compared with that of conventional high-performance liquid chromatography method. The significant advantages of the former include high-speed chromatographic separation, four times faster than high-performance liquid chromatography with conventional columns, and great enhancement in sensitivity. This developed method provided a new basis for overall assessment on quality of Semen Cassiae.

Objective To establish a method for determining twelve anthraquinones in cassia semen.Methods Diamonsil C18(150 mm×4.6 mm,5 μm)was used with the mobile phase consisting of acetonitrile-0.1% formic acid solution gradient at a flow rate of 1.0 ml · min-1.The detection wavelength was set at 280 nm and the column temperature was 25 ℃.Results Complete separation was obtained within 80 min for twelve compounds(casside,2-gluco-aurantioobtusin,2-gluco-obtusin,2-gluco-chrysoobtusin,auranto-obtusin,rhein,chrysoobtusin,obtusin,aloe-emodin,1-desmethylobtusin,chrysophanol,physcion).A linear relationship between the peak area and concentration of each compound was obtained.The average recovery(n=6) of the above compounds was 98.1%(RSD1.2%),98.9%(RSD2.1%),96.87%(RSD2.87%),97.12%(RSD2.1%),102.8%(RSD1.3%),98.92%(RSD2.0%),96.15%(RSD1.7%),98.5%(RSD1.9%),103.2%(RSD1.9%),102.3%(RSD2.6%),98.9%(RSD1.6%),97.67%(RSD1.4%).Conclusion The method established,sensitive,accurate and well repeatable,can be used for determination of anthraquinones in cassia semen.

Objective To establish the quality standards of Yuanren Capsules.Methods The TLC was used for qualitative discrimination of jujuboside A in capsules.HPLC was used for determination of tetrahydropalmatine in capsules.Results Based on the experimental results,three batches of the prepared products was consistent with the standards of capsules in Chinese Pharmacopeia(2010 edition).Jujuboside A could be identified by TCL.Tetrahydropalmatine could be identified by HPLC.A linear range of 0.2-2.0 μg(r = 0.999 9),all average recovery of 99.3% with RSD of 1.31%(n = 9) were obtained for determination of tetrahydropalmatine by HPLC.Conclusion The rapid and specific method is established for the quality control of Yuanren Capsules.

目的筛选决明子中蒽醌类化学成分的最佳提取方法。方法采用HPLC/UV法,以游离蒽醌、蒽醌苷类及12种蒽醌总质量分数为评判指标,通过L9(34)正交试验设计,考察乙醇质量分数、提取时间、固液比和提取次数等因素对决明子蒽醌类化学成分提取效果的影响。结果最佳提取方法为50倍70%乙醇回流提取1次,提取时间2 h。结论综合比较后,该提取方法对决明子药材中蒽醌类成分提取效率最高,操作经济省时,合理可靠,为决明子的进一步分析研究提供科学依据。

Lignans in the drug Fructus Schisandrae chinensis (FSC) exhibit potent biological activities such as antihepatotoxic, antiasthmatic, and antigastric ulcer. An ultrahigh-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry method has been developed to evaluate the quality of FSC through simultaneous qualitative and quantitative analysis of 15 lignans, including schizandrin A, B, and C; schizandrol A and B; gomisin B, C, D, E, G, H, J, and N; tigloylgomisin H; and angeloylgomisin H. The compounds were separated on a Zorbax Eclipse Plus C(18) (2.1 × 100 mm, 1.8 μm) column with a gradient elution of acetonitrile and 0.1% formic acid. Lignans were identified through their retention times, accurate mass data, and characteristic ions by comparison with a reference substance. All calibration curves showed perfect linear regression (r(2) > 0.99) within the test range. The limits of detection and quantitation fell in the ranges of 0.1-4 ng/mL for all the analytes with an injection of 10 μL. Good results were obtained with respect to repeatability (relative standard deviation <4.6%) and recovery (85.58-105.82%). Meanwhile, the entire sample analysis time was less than 10 min. This developed method provided a new basis for the overall assessment of the quality of FSC.

Ardipusilloside I, extracted from ARDISIA PUSILLA A.DC, effectively inhibits the progression of several cancers in animal models and is a potential anti-cancer drug candidate. However, the metabolism and pharmacokinetic characteristics of ardipusilloside I remain unknown. In this study, we developed a highly sensitive liquid chromatography-tandem MS method to determine the ardipusilloside I concentration in rat plasma using ginsenoside Re (whose structure is similar to ardipusilloside I) as the internal standard. After oral administration of ardipusilloside I, its four possible metabolites (M1, M2, M3, and M4, whose structures were determined by MS) were detected in the content from rat small intestine. In rat plasma, however, only M3 and M4 were detected after oral administration of ardipusilloside I. None of the metabolites were detected in plasma samples after intravenous administration of ardipusilloside I to rats. These results indicated that the metabolites, but not the drug itself, were absorbed into plasma after oral administration of ardipusilloside I to rats and that M3 and M4 may be responsible for the antitumor activity of orally administered ardipusilloside I in rat models of cancer.