胃灵颗粒质量标准的提高

摘 要 目的： 建立胃灵颗粒的质量标准。方法: 采用TLC法对胃灵颗粒中的主要药味白芍、甘草、延胡索及山楂进行定性鉴别;采用HPLC法测定白芍中芍药苷的含量,色谱柱：Agilent XDB-C₁₈（250 mm×4.6 mm,5 μm）,流动相：乙腈-0.1％磷酸溶液（10∶90）,检测波长：230 nm,流速：1.0 ml·min^-1。结果: 薄层色谱斑点清晰,在与对照药材或对照品相应的位置上显相同颜色的斑点,阴性对照无干扰;白芍中芍药苷的线性范围0.151～1.212 μg,r=0.999 9,平均回收率为99.63%,RSD为2.01%（n=9）。结论:本方法操作简单,结果准确可靠,重复性好,可作为胃灵颗粒的质量控制方法。     

原料药粒径对头孢地尼颗粒体外溶出行为的影响

目的：考察原料药粒径对头孢地尼颗粒体外溶出度的影响。方法参照2010版中国药典第二法,以 pH ＝6．8磷酸盐缓冲液为溶出介质,转速为50 r·min －1,采用紫外分光光度法为分析方法,考察不同粒径的原料制备的头孢地尼颗粒与参比制剂溶出的一致性。结果粒径为 D90：142．90μm、D50：30．25μm、D10：3．47μm（100目筛）和 D90：51．21μm、D50：10．71μm、D10：2．25μm（200目筛）的头孢地尼原料制成的颗粒溶出行为与原研不相似;在不同溶出介质中,D90：35．62μm、D50：6．98μm、D10：1．66μm 的头孢地尼原料制成的颗粒,与参比制剂的溶出行为均相似。结论建立的分析方法简单可靠,原料微粉化能够有效提高难溶性药物的溶出度。     

清热解肌颗粒中挥发油的初步质量研究

目的 建立清热解肌颗粒中挥发油成分的质量标准.方法 采用薄层色谱法(TLC)对清热解肌颗粒中挥发油进行定性鉴别;采用气—质联用色谱仪(GC-MS)对挥发油提取物的成分进行鉴定;采用气相色谱法(GC)测定制剂中挥发油的含量.结果 薄层色谱斑点清晰,重现性好,阴性对照无干扰.GC-MS共检出13个色谱峰并鉴定出12个化合物.α-蒎烯、β-蒎烯、桉油精线性范围分别为1.89～605.00mg·L-1(r=1.000),1.25 ～99.60mg· L-1(r=1.000),2.32 ～185.81 mg·L-1(r=1.000),平均加样回收率分别为92.82％(RSD =4.83％)、94.29％(RSD=3.10％)和104.23％ (RSD =3.14％) (n =9).结论 所建立的方法准确、可靠、专属性强,可用于该制剂的质量控制.     

康复新液保留灌肠治疗放射性肠炎的临床观察

目的：优选枇杷清肺颗粒的最佳醇提工艺。方法醇提工艺以盐酸小檗碱含量和浸膏得率为指标,采用正交试验优选枇杷清肺颗粒最佳醇提工艺。结果醇提最佳工艺条件为加10倍量70％乙醇,回流提取3次,每次2 h。结论优选出的提取工艺稳定,主要有效成分转移率高,为枇杷清肺颗粒的成型工艺研究奠定了基础。     

乙酰半胱氨酸颗粒在健康人体的生物等效性研究

目的：建立人血浆乙酰半胱氨酸浓度测定方法,研究乙酰半胱氨酸颗粒在健康人体内的相对生物利用度与生物等效性。方法采用二制剂三周期自身对照完全三交叉试验设计,其中每位受试者有一周期不服药,健康男性受试者24例分别单剂量口服乙酰半胱氨酸受试制剂或参比制剂0.6 g。高效液相色谱串联质谱法测定血浆乙酰半胱氨酸浓度,应用DAS 3.0版统计软件计算药动学参数并评价两种制剂生物等效性。结果单剂量口服乙酰半胱氨酸颗粒受试制剂和参比制剂0.6 g的主要药动学参数：AUC0→t分别为(8547.64±2860.04)和(8783.07±4042.10)μg·h·L-1;AUC0→∞分别为(9481.64±3444.76)和(9540.51±4239.30)μg·h·L-1;Cmax分别为(1994.39±726.42)和(2090.27±885.46)μg·L-1;tmax分别为(1.18±0.60)和(1.13±0.53) h;t1/2分别为(8.60±3.76)和(7.75±5.01) h;相对生物利用度以AUC0→t和AUC0→∞计算分别为(107.0±43.3)％和(106.5±40.1)％。结论乙酰半胱氨酸颗粒两种制剂具有生物等效性。     

Sorafenib,a multikinase inhibitor,induces formation of stress granules in hepatocarcinoma cells

Stress granules (SGs) are cytoplasmic RNA multimeric bodies that form under stress conditions known to inhibit translation initiation. In most reported stress cases, the formation of SGs was associated with the cell recovery from stress and survival. In cells derived from cancer, SGs formation was shown to promote resistance to either proteasome inhibitors or 5-Fluorouracil used as chemotherapeutic agents. Despite these studies, the induction of SGs by chemotherapeutic drugs contributing to cancer cells resistance is still understudied. Here we identified sorafenib, a tyrosine kinase inhibitor used to treat hepatocarcinoma, as a potent chemotherapeutic inducer of SGs. The formation of SGs in sorafenib-treated hepatocarcionoma cells correlates with inhibition of translation initiation; both events requiring the phosphorylation of the translation initiation factor eIF2α. Further characterisation of the mechanism of sorafenib-induced SGs revealed PERK as the main eIF2α kinase responsible for SGs formation. Depletion experiments support the implication of PERK-eIF2α-SGs pathway in hepatocarcinoma cells resistance to sorafenib. This study also suggests the existence of an unexpected complex regulatory balance between SGs and phospho-eIF2α where SGs dampen the activation of the phospho-eIF2α-downstream ATF4 cell death pathway.     

连黄降浊颗粒治疗高血压性肾损害的临床研究

目的：观察连黄降浊颗粒治疗高血压性肾损害肾功能衰竭期的疗效，并探讨其作用机制。方法：将96例中医辨证符合湿浊内蕴证的高血压性肾损害肾功能衰竭期患者随机分为试验组和对照组，各48例。试验组给予连黄降浊颗粒，对照组给予尿毒清颗粒，均每次1袋，每日3次，治疗2个月。观察治疗前后两组血压、24h尿蛋白定量、血红蛋白（Hb）、肾功能、一氧化氮（NO）、血浆内皮素（ET）、甲状旁腺激素（PTH）、N-乙酰-β-氨基葡萄糖苷酶（NAG）、湿浊内蕴证的症状积分及疗效变化。结果：治疗后试验组患者的血压、24h尿蛋白定量、ET、PTH、NAG、血肌酐（SCr）、尿素氮（BUN）、尿酸（UA）及中医症状积分均较治疗前显著下降（P〈0．05或P〈0．01），而Hb、肌酐清除率（CCr）、NO均显著上升（P〈0．05或P〈0．01），且连黄降浊颗粒作用较尿毒清颗粒更显著。试验组临床总有效率（91．7％）优于对照组（75．0％，x^2=4．8，P〈0．05）。结论：连黄降浊颗粒是治疗高血压性肾损害肾功能衰竭期的有效药物，具有降压、改善肾功能、调节内源性血管活性物质代谢、纠正甲状旁腺功能亢进、改善临床症状等作用。     

祛毒冲剂治疗肠源性内毒素血症的临床研究

目的:观察祛毒冲剂对危重病肠源性内毒素血症的治疗价值.方法:61例肠源性内毒素血症患者随机分为祛毒冲剂组(30例)和思密达组(31例),在治疗前,治疗后1、3和7 d分别观测、记录患者一般体征变化,清晨空腹采外周静脉血测定白细胞计数、血浆内毒素及血清肿瘤坏死因子(TNF)水平.结果:祛毒冲剂组外周血白细胞计数下降速度明显快于思密达组,3 d后差异有显著性(P<0.01),排便次数多于思密达组(P=0.000),并可较快地降低血浆内毒素及血清TNF水平(P均<0.01).结论:祛毒冲剂可以有效地降低血浆内毒素及血清TNF水平,并改善患者的临床症状,促进患者康复.     

益智膏治疗小儿智力低下34例临床观察

[目的]观察应用益智膏配合针刺改善肾精不足型智力低下患儿智能水平的临床疗效。[方法]将68例入组患儿按照随机数字表法分成治疗组和对照组,治疗组34例给予服用益智膏、针刺、康复训练,对照组34例给予针刺、康复训练;采用中国韦氏幼儿、儿童智力量表进行评分,应用尼莫地平法计算智商(IQ)分值提高率。[结果]益智膏配合针刺治疗肾精不足型智力低下有效,临床总体疗效优于对照组,两组比较具有统计学意义(P0.05)。[结论]益智膏配合针刺治疗肾精不足型智力低下临床疗效确切。     

Development of a predictive in vitro dissolution for clarithromycin granular suspension based on in vitro-in vivo correlations

The objective of this study was to evaluate the in vitro behavior of different clarithromycin granular suspensions based on a developed in vitro-in vivo correlation model, using one reference and two test formulations. In vitro release rate data were obtained for each product using the USP apparatus II, operated at 50?rpm under different pH conditions. The dissolution efficiency was used to analyze the dissolution data. In vivo study was performed on six healthy male volunteers under fasting condition. Correlation was made between in vitro release and in vivo absorption. A linear model was developed using percent absorbed data versus percent dissolved data from the three products. Dissolution condition of 0.1N HCl for 1?h and then phosphate buffer at pH 6.8 was found to be the most discriminating dissolution method. Rate of absorption for the reference as estimated by Wagner-Nelson deconvolution was correlated with in vitro release with a correlation coefficient of 0.99. The in vivo results for the two test products were compared to the predicted values using the reference model with a correlation coefficient of 0.94. Furthermore, multiple level C correlations were obtained for some pharmacokinetic parameters with the corresponding in vitro kinetic parameters with correlation coefficients exceeding 0.90. Moreover, the interpretation of the in vitro and in vivo data with reference to formulations was discussed.