Benzoyl Peroxide Solubility and Stability in Hydric Solvents

Saturated solubility and reaction rate constants for the decomposition of benzoyl peroxide in solution and suspension were determined for use in formulation development. The solvents studied included ethanol, propylene glycol, and cosolvent mixtures of PEG 400 and water. The solubility of benzoyl peroxide was inversely related to the solvent polarity, with greater solubility occurring with semipolar solvents. The stability of benzoyl peroxide in solution was dependent on the solvent, concentration of benzoyl peroxide, and temperature. The compound was least stable in PEG 400. Stability was improved when water was added to PEG 400. Similar solvent effects were observed in suspension. In benzoyl peroxide suspensions of PEG 400 and PEG 400/water blends, benzoyl peroxide stability was dependent on solubility, with improved stability occurring in blends where the benzoyl peroxide was least soluble. Thus, solution formulations of benzoyl peroxide in pharmaceutically acceptable solvents are unlikely to show good stability; however, suspension formulations should be reasonably stable if the vehicle is selected to provide low benzoyl peroxide solubility.     

A comparative study of the proteolytic enzymes of Trypanosoma brucei, T. equiperdum, T. evansi, T. vivax, Leishmania tarentolae and Crithidia fasciculata

Four types of proteolytic activity were detected in the bloodstream form of each of the four Trypanosoma species: (i) HPAase, active on hide powder azure and detected on polyacrylamide gels containing denatured haemoglobin; (ii) AZCase, active on azocasein; (iii) type 1, active on the chromogenic peptide N-benzoyl-L-prolyl-L-phenylalanyl-L-arginine p-nitroanilide in the presence of dithiothreitol, and (iv) type 2, active against several nitroanilide derivatives in the absence of dithiothreitol. Studies of the pH optimum, dithiothreitol requirement and inhibitor sensitivities of the proteolytic activities suggested that: (a) HPAase and type 1 activities could be due to the same enzymes, probably a family of cysteine proteinases; (b) AZCase had some characteristics of a cysteine proteinase, but was not identical to HPAase, and (c) type 2 activity could be due to a serine proteinase. Procyclic T. brucei contained relatively low cysteine proteinase activities (HPAase, AZCase and type 1) but high type 2 activity. Their proteolytic enzymes thus were apparently more similar to those in Crithidia fasciculata and Leishmania tarentolae promastigotes than those in T. brucei bloodstream forms.     

苦参总碱抗实验性心律失常的作用

目的：研究苦参总碱抗实验性心律失常的作用。方法：本研究采用冠脉结扎，BaCl2肾上腺素，乌头碱，哇巴因诱发的心律失常模型。结果：苦参总碱能明显对抗大鼠冠脉结扎后诱发的早期缺血性心律失常；对BaCl2诱发的大鼠心律失常有预防和治疗作用；缩短静注肾上腺素诱发的家兔心律失常持续时间；增加乌头碱诱发大鼠心律失常的剂量；增加哇巴因诱发豚鼠心律失常的剂量。结论：苦参总碱对多种心律失常模型有预防或治疗作用，其抗心律失常机制是多方面的。     

Study on Metabolites of Aconitum Alkaloids in Human Urine

TheaconitebelongstoplantsofgenusAconituminfamilyofRanunculaceaandhavenotableclinicalfunctionsintreatingrheumaticarthritis ,heartfailure ,etc .However,accidentsofaconitine(fromaconite)poisoningfrequentlyoccurtomanypeopletakingtheseherbs .Theplantsofthisfamilycontainaconitine ,mesaconitine ,hypaconitineandotheraco nitumalkaloids .Theyarehighlytoxic ,andtheirtreatmentdoseapproachestothetoxicdoseorlethaldose .Duringtheperiodfrom 1989- 1995 ,morethan 30casesofpoisoningcausedbyaconitineinsometradit…     

基于AHP-熵权法优选黑顺片炮制工艺及生物碱类成分动态变化研究

目的 采用主观评价层次分析法（analytic hierarchy process，AHP）-熵权法优选黑顺片炮制工艺，探究炮制过程中生物碱类成分动态变化规律。方法 采用外观性状、水溶性浸出物、苯甲酰新乌头原碱含量、苯甲酰乌头原碱含量、苯甲酰次乌头原碱含量、双酯型生物碱总量作为评价指标，基于单因素考察结果，以煮制时间、水漂次数、蒸制时间、干燥温度为主要因素建立正交实验，通过AHP-熵权法优选黑顺片最佳炮制工艺参数。采用HPLC法对各炮制环节的附子进行含量测定，分析比较6种酯型生物碱的含量变化。结果 在质量分数20%以上的胆巴溶液中浸泡能达到防腐的目的，且浸泡20d以上附子的质量相对稳定。黑顺片炮制的最佳工艺条件为煮制时间8min，水漂次数4次，蒸制时间3h，干燥温度60℃；炮制过程中双酯型生物碱总量逐渐降低，泡胆和漂洗过程单酯型生物碱含量降低，煮制和蒸制过程单酯型生物碱含量升高。结论 实验优化所得的黑顺片炮制工艺合理、稳定、可行，炮制过程中各环节对酯型生物碱类成分均有不同程度的影响，可为进一步探讨黑顺片的现代炮制方法提供参考。     

415 nm蓝光联合5%过氧苯甲酰凝胶治疗轻中度寻常性痤疮的疗效

 目的 观察415 nm蓝光联合5%过氧苯甲酰凝胶治疗轻中度寻常性痤疮的临床疗效与安全性。方法 选取武警湖北总队医院2019-03至2020-09轻中度寻常性痤疮90例,随机分为3组,每组30例。联合组同时予415 nm蓝光照射联合5%过氧苯甲酰凝胶外用;蓝光组和药物组分别予415 nm蓝光照射和5%过氧苯甲酰凝胶外用。3组均在治疗8周后判定疗效。结果 治疗8周后联合组有效率为83.3％。蓝光组和药物组有效率分别为30％和56.7％,与联合组有效率比较,差异均有统计学意义。治疗过程中不良反应少见且患者均可耐受。结论 415 nm蓝光联合5%过氧苯甲酰凝胶治疗轻中度寻常性痤疮疗效显著,不良反应少。     

采用傅里叶变换红外光谱和HPLC法分析附子炮制品黑顺片和白附片差异

目的 基于成分分析探讨黑顺片和白附片的差异。方法 基于傅里叶红外光谱（fourier transforms infrared,FTIR）和HPLC,结合化学计量学方法,对黑顺片和白附片的整体化学成分进行研究,并通过独立样本t检验对其有效和毒性成分含量进行比较分析。结果 FTIR结合正交偏最小二乘法判别分析（orthogonalpartialleastsquares-discriminationanalysis,OPLS-DA）结果显示,白附片和黑顺片整体化学成分差异明显,饮片类型的差异高于产地差异;HPLC的聚类分析（hierarchical clustering analysis,HCA）、主成分分析（principal component analysis,PCA）、OPLS-DA和相似度分析（similarity analysis,SA）均能将黑顺片、白附片区分为2类,表明2种饮片的成分差异较大;含量测定结果显示,黑顺片的单酯型生物碱量显著高于白附片,具有统计学意义（P<0.01）,而双酯型生物碱含量差异不显著,无统计学意义。结论 白附片和黑顺片化学成分差异较大,临床上应区...     

槲寄生总黄酮苷对缺氧、心肌缺血及心律失常的预防作用的研究

目的研究槲寄生总黄酮苷对缺氧、急性心肌缺血和心律失常的预防作用.方法采用乙醇和有机溶剂萃取方法从槲寄生中提取总黄酮有效成分;用磨口瓶法观察完全密闭小鼠的存活时间;垂体后叶素(1U/kg)致心肌缺血模型,用分光光度法测LDH、MDA、SOD值;用乌头碱(40μg/kg)建立心律失常模型,观测对室颤发生率等的影响.结果耐缺氧实验中给药组小鼠的平均存活时间显著长于对照组(P＜0.05);在心肌缺血实验中,给药组血清中LDH、MDA、SOD的含量与模型组有显著差异(P＜0.05);在心律失常实验中室性心动过速(VT)、室颤(VF)的发生率有降低趋势,室性早搏出现时间有延长趋势,对窦性节律恢复率没有影响.结论槲寄生总黄酮苷可显著增强小鼠耐缺氧能力;槲寄生总黄酮苷对垂体后叶素引起的大鼠急性心肌缺血损伤具有显著的保护作用;槲寄生总黄酮苷对大鼠心律失常有一定拮抗作用.     

附子甘草配伍对乌头碱、甘草酸、甘草苷的动态影响

 目的建立水煎液中甘草苷、甘草酸、乌头碱的HPLC定量测定方法。研究附子与甘草配伍前后产生的化学成分的动态变化现象,探讨附子甘草配伍增效减毒的物质基础。方法用高效液相色谱法测定附子、甘草单煎及附子与甘草配伍合煎液中甘草苷、甘草酸、乌头碱的含量,分别观察在煎煮的0,5,10,20,30,45,60,75,90 min化学成分的动态变化情况。结果附子甘草配伍后乌头碱、甘草苷、甘草酸含量均比单煎时低。结论甘草苷、甘草酸、乌头碱等化学成分的变化是附子甘草配伍能增效减毒的重要物质基础。本实验从组分合和的角度,肯定了附子甘草组分配伍的合理性与科学性。