Enhanced antitumour activity of doxorubicin and simvastatin combination loaded nanoemulsion treatment against a Swiss albino mouse model of Ehrlich ascites carcinoma

Doxorubicin (DOX) is the most commonly used anticancer drug; however, it has limited use because prolonged administration may result in severe cardiotoxicity. Simvastatin (SIM), generally prescribed for hypercholesterolaemia, has also shown salubrious results in the monotherapy or combinational drug therapy of different cancers in various models. Nanoparticle drug delivery systems are a novel way of improving therapeutics and also improving the absorption and specificity of drugs towards tumour cells. In this study, we exploited this technology to increase drug specificity and minimize imminent adverse effects. In this study, the antitumour activity of the combination formulas of DOX and SIM, either loaded in water (DOX‐SIM‐Solution) or nanoemulsions (NEs) (DOX‐SIM‐NE), was evaluated in a Swiss albino mouse model of Ehrlich ascites carcinoma. The anticancer effect was assessed by quantifying the change in body weight, mean survival time, and percent increase in lifespan (%ILS), determining haematological and serum biochemical parameters (liver function test, kidney function test and lipid profile parameters) as well as studying the histopathological alterations in liver tissues. We observed a clear increase in %ILS of the DOX‐SIM‐Solution group (265.30) that was double the %ILS of the DOX‐SIM‐NE group (134.70). However, DOX‐SIM‐NE had a non‐toxic effect on the haematological parameters, whereas DOX‐SIM‐Solution increased the levels of haemoglobin and lymphocytes. Furthermore, the encapsulation of SIM and DOX into NEs improved the levels of all serum biochemical parameters compared to the DOX‐SIM‐Solution. A reduction in the side effects of DOX‐SIM‐NE on the liver was also established using light microscopy, which revealed that the morphologies of the hepatocytes of the mice were less affected by administration of the DOX‐SIM‐NE treatment than with the DOX‐SIM‐Solution treatment. The study showed that incorporating SIM into the DOX‐loaded‐NE formulation remarkably improved its efficiency and simultaneously reduced its adverse effects.     

愈骨疗伤片的处方筛选及制备工艺研究

  目的：优化愈骨疗伤片的制备工艺,筛选最优制剂处方。  方法：在考察提取物粒径基础上,以片剂中川续断皂苷溶出量作为考察指标,采用正交试验对搅拌速度、制粒速度和聚维酮K30浆液浓度三者关系进一步考察。采用单因素进一步优选润滑剂和包衣工艺条件。  结果：最佳的愈骨疗伤片处方为提取物颗粒中加入10%乳糖、7.5%羧甲基淀粉钠和2.5%聚维酮K30,以及0.5%硬脂酸镁混合后压片；采用低浓度乙醇包衣液进行包衣。  结论：制得的愈骨疗伤片制剂工艺稳定,包衣后改善了片剂的吸潮性,增加了产品的稳定性,更便于保存和运输。     

扶正固本法对青少年哮喘患者基因表达的影响

目的 研究复方中药敏康片治疗青少年哮喘的疗效和作用机理。方法 选择20例青少年哮喘患者进行治疗，另设青少年特应性皮炎患者组（20例）和青少年正常组（19例）为对照。哮喘组和皮炎组口服敏康片，疗程为6个月，观察疗效、血清总IgE及FcεRIβ、IL-4Rα基因表达改变情况。结果 哮喘组显效6例，有效12例，无效2例，总有效率90％；皮炎组显效4例，有效13例，无效3例，总有效率85％；哮喘组IgE治疗前后有显著差异（P〈0．01）。皮炎组IgE治疗前后有差异（P〈0．05）；用Northern blot法检测FctRlt3、IL-4Rα基因，IL-4Rα吸光度值两组治疗前均较正常组高，哮喘组治疗后降低。FcεRIβ吸光度值两组治疗前均较正常组高，治疗后均降低。结论 复方中药可以调整青少年哮喘患者相关基因表达，改善患者过敏状态，缓解临床症状。     

辛伐他汀5mg与普伐他汀10mg治疗高胆固醇血症的比较

目的：探讨低剂量辛伐他汀治疗高胆固醇血症的临床疗效及耐受性。方法：低、中度原发性高胆固醇血症病人６２例，随机分为２组，Ａ组３１例（男性２６例，女性５例；年龄６４±ｓ１４ａ）采用辛伐他汀５ｍｇ，ｐｏ，ｑｄ。Ｂ组３１例（男性２５例，女性６例；年龄６１±１３ａ）采用普伐他汀１０ｍｇ，ｐｏ，ｑｄ。疗程均为４ｗｋ。结果：辛伐他汀组在降低ＴＣ，ＬＤＬ＿ｃｈ及提高ＨＤＬ＿ｃｈ的平均变化率上分别为１７％±９％，２５％±１２％（Ｐ＜０．０１）和１１％±１１％（Ｐ＞０．０５），与普伐他汀组疗效相当，组间比较，Ｐ值＞０．０５。２种药物治疗期间病人均无显著不良反应。结论：小剂量辛伐他汀疗效可与普伐他汀媲美，５ｍｇ／ｄ可作为治疗高胆固醇血症的起始剂量     

医药行业科技成果产业化的风险控制

医药行业科技成果产业化与其他行业科技成果转化相比具有更高的风险，转化能力也是最低的，因此，对其从事前、事中、事后三方面加强风险控制具有重要的观实意义。     

马来酸罗格列酮胃漂浮型缓释片的研究

目的：根据流体动力学平衡控释原理（HBS）研制了马来酸罗列酮胃漂浮型缓释片。方法；以体外释放度和漂浮情况为筛选指标，采用单因素考察和正交试验设计相结合， 对胃漂浮缓释片的处方、制备工艺及体外释放条件进行优化筛选；采用γ闪烁照相技术对优化处方的内漂浮情况进行胃内动态观察。结果：马来酸罗格列酮胃漂浮缓释片在释放介质中迅速起漂，持漂时间超过12h,12h达最大累积释放；初步确定在胃内滞留时间达3h以上。结论：优化处方的释放过程符合Higuchi方程，释放机制为异常扩散；胃漂浮片在胃滞时间明显长于普通片。     

罗红霉素分散片人体相对生物利用度及其药代动力学研究

目的:通过人血清中罗红霉素的微生物测定法,考察丽珠集团丽珠制药厂研制的罗红霉素分散片丽珠星相对于法国罗素-优克福公司的罗红霉素普通片罗力得的生物等效性,并估算其药代动力学参数.方法:以藤黄八叠球菌为检定菌,通过抑菌圈直径测定血药浓度.临床实验方案采用交叉实验设计,10名受试者随机分两组服用罗红霉素分散片和普通片.结果:本方法日内、日间变异系数均小于15%,线性范围为0.25～10.0 μg/ml(r=0.9992),最低检测浓度为0.25 μg/ml.罗红霉素分散片和普通片的主要药动学参数为:AUC0→36分别为61.41±13.53 μg·h/ml和57.63±11.29 μg·h/ml;AUC0→∞分别为66.62±17.89 μg·h/ml和62.93±14.62 μg·h/ml;cmax分别为7.15±0.18 μg/ml和7.37±0.42 μg/ml;tmax分别为1.10±0.44 h和1.20±0.26 h;T1/2分别为8.21±2.92 h和8.28±2.46 h.方差分析表明两种制剂的药代动力学参数间均无显著性差异.双单侧t检验表明两制剂吸收程度相同.结论:本方法简便准确.分散片的相对生物利用度为(105.9±13.8)%,表明分散片与普通片吸收程度生物等效.     

辛伐他汀对人低密度脂蛋白氧化修饰影响的实验研究

目的研究辛伐他汀在体外对低密度脂蛋白氧化修饰的影响.方法以低密度脂蛋白氧化修饰为模型,以硫代巴比妥酸反应物质(TBARS)生成量及相对电泳迁移率(REM)为指标,研究了辛伐他汀对铜离子(Cu2 )诱导低密度脂蛋白氧化修饰的抑制作用.结果随辛伐他汀浓度从1～10μmol/L的增加,TBARS值分别减少67.3%,73.9%,81.9%,REM值减少48.3%,55.2%,58.6%,呈浓度及时间依赖关系.其中10μmol/L辛伐他汀可几乎完全抑制低密度脂蛋白氧化.结论辛伐他汀在体外能明显抑制Cu2 诱导的低密度脂蛋白氧化修饰.     

参七黄稳斑胶囊合用辛伐他汀对家兔动脉粥样硬化斑块的影响

目的探讨参七黄稳斑胶囊单用及合用辛伐他汀对家兔动脉粥样硬化（As）斑块的影响。方法将45只家兔随机分为正常对照组（A组）、不稳定斑块对照组（B组）、参七黄稳斑胶囊治疗组（C组）、辛伐他汀治疗组（D组）、参七黄稳斑胶囊和辛伐他汀合用治疗组（E组）。A组用普通饲料，其他组用高胆固醇饲料喂养；12周末造模成功后，如前喂养，C、D、E组分别给予不同药物干预。24周末在腹主动脉注射药物触发斑块破裂，2周后检测各组血清中血管细胞粘附分子-1（VCAM-1）、细胞间粘附分子-1（ICAM-1）和超敏C反应蛋白（hs-CRP）的水平；测定斑块面积、内膜厚度、中膜厚度、纤维帽厚度。结果与B组相比，C、D、E组血清中VCAM-1、ICAM-1、hs—CRP的水平及斑块面积、内膜厚度明显降低，纤维帽明显增厚（P〈0．01）；其中C组优于D组（P〈0．05），E组优于C组（P〈0．01）。结论参七黄稳斑胶囊有较好的稳定斑块的作用，与辛伐他汀有协同作用。     

Bioavailability and Pharmacokinetics of a New Sustained-Release Potassium Chloride Tablet

The bioavailability of a new sustained-release potassium chloride (KC1) tablet, designed for once-a-day dosing, was compared to a KC1 elixir using urinary excretion data. The study utilized 25 male volunteers dosed in a crossover design in a dietary/activity-controlled environment. The regimens consisted of a total of 80 mEq of potassium in three equally divided doses of elixir every 6 hr and a single 80-mEq dose using four 20-mEq sustained-release (SR) tablets. The mean time to maximum rate of potassium urinary excretion was 2.2 hr for the first elixir dose and 5.5 hr after the SR tablet (P < 0.01), thereby supporting the prolonged-release properties of this formulation. After correction for baseline urinary potassium excretion, the mean total 24-hr urinary potassium excretion was 42.18 mEq for the elixir and 40.41 mEq for the SR tablet. The results indicate that the absorption pattern from the SR tablet is equal to three doses of KC1 elixir dosed 6 hr apart.