Oral Dispersible System: A New Approach in Drug Delivery System

Dosage form is a mean used for the delivery of drug to a living body. In order to get the desired effect the drug should be delivered to its site of action at such rate and concentration to achieve the maximum therapeutic effect and minimum adverse effect. Since oral route is still widely accepted route but having a common drawback of difficulty in swallowing of tablets and capsules. Therefore a lot of research has been done on novel drug delivery systems. This review is about oral dispersible tablets a novel approach in drug delivery systems that are now a day''s more focused in formulation world, and laid a new path that, helped the patients to build their compliance level with the therapy, also reduced the cost and ease the administration especially in case of pediatrics and geriatrics. Quick absorption, rapid onset of action and reduction in drug loss properties are the basic advantages of this dosage form.     

复方丹参滴丸对老年冠心病患者血流变学、血脂及炎性反应递质的影响

目的：探究复方丹参滴丸对老年冠心病患者血流变学、血脂及炎性反应递质的影响。方法：选取2015年1月至2017年12月海南省人民医院收治的老年冠心病患者154例作为研究对象，按照随机数字表法随机分为对照组和观察组，每组77例。对照组采用常规西药治疗，观察组在此基础上加服复方丹参滴丸。比较治疗前后2组患者的血流变学、血脂、炎性反应递质和疗效。结果：观察组治疗有效率为92.21%，明显高于对照组治疗有效率79.22%，差异有统计学意义（P<0.05）。治疗后，2组总胆固醇（TC）、三酰甘油（TG）和低密度脂蛋白（LDL）水平均升高，差异有统计学意义（P<0.05），且观察组高于对照组，2组差异有统计学意义（P<0.05）。2组血流变学指标、高密度脂蛋白（HDL）、IL-6和TNF-α水平治疗后均降低（P<0.05），且观察组降低更明显，差异有统计学意义（P<0.05）。结论：复方丹参滴丸联合常规西药治疗冠心病患者，能够调节脂代谢，降低炎性反应，改善血流变学。     

石斛合剂对高脂高糖糖尿病大鼠心肌细胞Ca^2+代谢的影响

目的以糖尿病心肌病大鼠为研究对象,探讨石斛合剂对糖尿病心肌病心肌细胞Ca^2+代谢的影响。方法 Wistar大鼠24只,取5只作为正常组,余19只采用高脂高糖饮食联合链脲佐菌素腹腔注射进行糖尿病心肌病造模。成模后,随机分为模型组、二甲双胍组、石斛合剂组。二甲双胍组、石斛合剂组分别予二甲双胍、石斛合剂灌胃,正常组、模型组予生理盐水灌胃。4周后,测空腹血糖,取左心室心肌组织进行组织病理学观察和心肌细胞内游离钙(MyoCa^2+)浓度测定,Western blot法检测肌浆网Ca^2+-ATP酶(SERCA2a)、L型钙通道α1C亚单位蛋白(CACNA1C)蛋白表达,RT-PCR法测定SERCA2a mRNA表达。结果石斛合剂组心肌纤维较模型组、二甲双胍组排列整齐,断裂较少。与正常组比较,模型组血糖、心肌细胞MyoCa^2+含量和CACNA1C蛋白表达明显升高(P<0.01,P<0.05),SERCA2a mRNA和蛋白表达明显降低(P<0.01)。与模型组比较,石斛合剂组血糖、心肌细胞MyoCa^2+含量和CACNA1C蛋白表达明显降低(P<0.01,P<0.05),SERCA2a mRNA和蛋白表达明显升高(P<0.01,P<0.05);二甲双胍组血糖明显降低(P<0.01)。与二甲双胍组比较,石斛合剂组心肌细胞MyoCa^2+含量明显降低(P<0.01,P<0.05),血糖、SERCA2a mRNA和蛋白表达明显升高(P<0.05)。结论石斛合剂通过提高SERCA2a mRNA和蛋白表达,加快摄取Ca^2+的速率,降低细胞质Ca^2+负荷,缓解钙超载,最终达到维持糖尿病心肌病钙稳态的作用,有效维持心肌细胞的正常收缩舒张功能;其降糖作用不是预防糖尿病心肌病的主要机理,而在于抑制CACNA1C蛋白表达,抑制钙诱导钙释放过程。     

Matrine,oxymatrine, and compound Kushen injection from the roots of Sophora flavescens: an overview of their anticancer activities

In the present review, we updated current information on the chemistry, contents, and anticancer properties of matrine (MT), oxymatrine (OMT), and compound Kushen injection (CKI). The anticancer properties were focused on lung, breast, and liver cancer cells because they are most susceptible. Sources of information were from Google, Google Scholar, PubMed, PubMed Central, Science Direct, PubChem, J-Stage, Directory of Open Access Journals (DOAJ), and China National Knowledge Infrastructure (CNKI). Reference was also made on botanical websites, such as Flora of China and World Flora Online. MT and OMT are dominant quinolizidine alkaloids from the roots of Sophora flavescens (Kushen) of the family Fabaceae. Against lung, breast, and liver cancer cells, MT and OMT inhibit cell proliferation; induce cell cycle arrest, apoptosis, and autophagy; restrict angiogenesis; and inhibit cell metastasis, invasion, and migration. The processes involve various molecular targets and signaling pathways. CKI is a traditional Chinese medicine (TCM) composed of root extracts of S. flavescens and Smilax glabra (Baituling) of the family Smilacaceae. With MT and OMT as major components, CKI has been approved for the treatment of cancer in China more than 20 years ago. In recent years, systematic reviews and meta-analysis have been undertaken to evaluate the anticancer effects of CKI. When CKI is used alone and in combination with chemotherapy of western medicine, there is much to be learned concerning their interactions besides their individual and integrated efficacy. Some perspectives of MT, OMT, and CKI are discussed, and their suggestions for future research are provided.     

美托洛尔用于老年COPD合并冠心病史治疗的临床疗效观察

目的:探讨美托洛尔(β1受体阻滞剂)用于老年COPD合并冠心病史治疗的临床疗效。方法:选取2018年6月—2019年6月在我院接受治疗的60岁以上(包括60岁)COPD合并冠心病史老年患者,分为对照组与观察组。对照组给予接受布地奈德福莫特罗粉吸入剂治疗,观察组在使用布地奈德福莫特罗粉吸入剂治疗的基础上口服琥珀酸美托洛尔缓释片治疗,观察对比两组治疗效果。结果:观察组临床治疗效果优于对照组,观察组住院时长以及并发症的发生率低于对照组(P<0.05),差异具有统计学意义。结论:老年COPD合并冠心病史接受美托洛尔治疗,可有效缩短住院时长、用药效果明显、有效提升用药安全性,值得临床推广。     

基于化学模式识别技术提升参威骨痹片的质量标准并监测其生产中质控指标的转移率变化

目的:提升参威骨痹片的质量标准,初步探索其质量控制指标成分在批间含量差异较大的原因。方法:采用HPLC建立参威骨痹片的指纹图谱,以Diamonsil C18(4. 6 mm×250 mm,5μm)为色谱柱,流动相乙腈(A)-0. 1%磷酸水溶液(B)梯度洗脱(0～5 min,10%A;5～15 min,10%～12%A;15～30 min,12%～26%A;30～43 min,26%～31%A,43～50 min,31%～40%A,50～70 min,40%～55%A;70～84 min,55%～72. 5%A),检测波长230 nm。以共有峰为自变量绘制正交偏最小二乘法-判别分析-变量重要性投影(OPLS-DA-VIP)图,将共有峰对该制剂各批次间指纹图谱差异的贡献度量化,寻找差异较大的色谱峰,结合相关文献,筛选出与参威骨痹片临床适应症相关的成分并进行其含量测定的专属性试验,最终选定质控指标。通过HPLC-二极管阵列检测器(DAD)同时对本品及其生产过程中间体中质控指标进行测定,检测波长236,276,230,322 nm,其他条件同HPLC指纹图谱检测方法。结果:HPLC指纹图谱共标定了26个共有峰,各批次样品指纹图谱与对照指纹图谱的相似度均≥0. 950。优选出马钱苷酸、龙胆苦苷、芍药苷、蛇床子素为参威骨痹片的质控指标,四者的平均质量分数分别为161. 02,401. 80,255. 54,80. 68μg·g-1。结论:所建立的指纹图谱及多指标定量分析方法稳定、可靠,可用于参威骨痹片的质量控制。原料药批间质控指标成分含量差异和生产过程中间体的质控方法不够完善是引起该制剂批间质控指标成分含量差异较大的主要原因。     

激光联合复方血栓通胶囊治疗糖尿病视网膜病变合并黄斑水肿的疗效观察

目的:分析糖尿病视网膜病变合并黄斑水肿联合采用激光与复方血栓通胶囊治疗的临床疗效。方法:选取我院2017年1月—2019年1月收治的200例糖尿病视网膜病变合并黄斑水肿患者为研究对象,随机分为两组。对照组单独行激光治疗,观察组于对照组基础上联合复方血栓通胶囊治疗,对比两组临床疗效、治疗前后IL-6(白介素-6)、VEGF(血管内皮生长因子)、NOS(血清一氧化氮合成酶)水平变化情况。结果:对照组总有效率(68.00%,68/100)较观察组总有效率(98.00%,98/100)更高(P<0.05);与对照组对比,观察组治疗后NOS水平更高,IL-6、VEGF水平更低(P<0.05)。结论:糖尿病视网膜病变合并黄斑水肿联合采用激光与复方血栓通胶囊治疗的临床疗效显著,值得推广。     

复方番石榴制剂治疗超重肥胖2型糖尿病的疗效分析

【目的】评价复方番石榴制剂治疗超重肥胖2型糖尿病的临床疗效。【方法】将120例超重肥胖2型糖尿病患者随机分为治疗组和对照组各60例,治疗组给予口服二甲双胍肠溶片及复方番石榴制剂治疗,对照组给予口服二甲双胍肠溶片治疗,疗程均为12周。观察2组治疗前后腰围(WC)、体质量指数(BMI)、空腹血糖(FBG)、餐后2h血糖(P2hBG)、糖化血红蛋白(HbA1c)、胆固醇(TC)、甘油三酯(TG)、游离脂肪酸(FFA)等的变化情况,评估复方番石榴制剂的临床疗效。【结果】(1)中医证候总疗效:治疗后,治疗组的总有效率为95.00%,优于对照组的70.00%,差异有统计学意义(P0.01)。(2)治疗后,治疗组的WC和BMI均较治疗前显著下降(P0.01),而对照组均无明显下降(P0.05),治疗组对WC和BMI的下降作用均优于对照组(P0.05)。(3)治疗后,2组FBG、P2hBG、HbA1c、TC、TG、FFA水平均较治疗前显著改善(P0.05),且治疗组对上述各项指标的改善作用均优于对照组(P0.05)。(4)安全性评价:除治疗组有3例患者出现轻度的胃部不适感,未予特殊处理后自行缓解外,其余患者均未发现不良反应。【结论】复方番石榴制剂联合二甲双胍治疗超重肥胖2型糖尿病,疗效确切,可有效降糖、降脂、减肥及改善中医证候。     

Pharmacological evaluation and mechanistic study of compound Xishu Granule in hepatocellular carcinoma

ObjectiveIn this study, we used HepG2 human hepatocellular carcinoma cells to study the effects of Compound Xishu Granule (CXG) on cell proliferation, apoptosis, and the cell cycle in vitro. We also used a xenograft tumor model to study the anti-tumor effects of CXG and related mechanisms in vivo.MethodsThe effect of CXG on cell viability was measured using Cell Counting Kit-8 and a colony formation assay. The effect of CXG on apoptosis and the cell cycle was analyzed using flow cytometry. The in vivo anti-tumor effect of CXG was assessed by measuring the volume change in xenograft tumors after drug administration. The CXG anti-tumor mechanism was studied using western blotting assay to detect cell cycle and apoptotic associated proteins.ResultsCXG suppressed HepG2 cell proliferation in a time- and dose-dependent manner in vitro. Colony formation experiments showed that CXG administration for 24 h significantly reduced HepG2 cell formations (P < .01). Flow cytometric analysis showed that CXG treatment for 48 h promoted apoptosis and blocked HepG2 cells in the G2/M phase. Western blotting results showed that Bax was significantly up-regulated and Bcl-2 was down-regulated in graft tumor tissues and HepG2 cells after CXG administration, which increased the Bax/Bcl-2 ratio. PLK1, CDC25C, CDK1, and Cyclin B1 expression were up-regulated. CXG had a good inhibitory effect on graft tumor growth in vivo.ConclusionCXG has good anti-tumor effects in vitro and in vivo. In vitro, CXG promoted HepG2 cell apoptosis and induced G2/M phase arrest. In vivo, CXG significantly inhibited graft tumor growth. The CXG mechanism in treating hepatocellular carcinoma may be that CXG can induce abnormal apoptotic and cell cycle associated protein expression, leading to mitotic catastrophe and apoptosis.