对《中国药典》2000年版二部附录散剂及混悬剂的修改意见

《中国药典》2000年版二部附录18页附录IP散剂中[粒度],仅规定局部用散剂用七号筛检查,而口服散剂没有规定筛号,是否可认为口服散剂不检查粒度? [装量差异]检查法:“取散剂10包(瓶),除去包装,分别精密称定每包(瓶)内容物的重量,每包(瓶)与标示量相比应符合规定,超出装量差异限度的散剂不得多于2包(瓶),并不得有1包(瓶)超出装量     

制剂压片中的常见问题及解决方法探讨

在压片机压片过程中，会遇到一些问题，如重量差异超限、硬度不足、顶裂、崩解时间延长等。上述问题，有的在压片开始时出现；有的在压片的某一时段出现。既有物料方面的原因，又有设备方面的原因。要做到具体问题具体分析，及时发现问题及时解决，确保生产出合格的产品。 1重量差异超限 　　药片重量差异较大，无法保证患者用药剂量。《药典》规定 0． 30克以下药片的重量差异限度为± 7． 5％， 0． 30克或 0． 30克以上的药片重量差异限度为± 5％。引起重量差异的原因有物料和机械两方面的因素。 1． 1压片过程中由于待压混合物流动性较…     

中药制剂的重量(装量)差异与含量限度

重量（装量）差异是药物制剂的重要质量指标,与药物制剂的含量限度密切相关。正确理解重量（装量）差异与含量限度的相互关系对药物制剂的生产与检验有重要意义。国家药品标准（药典及部颁标准）和地方药品标准的部分品种存在着规格（标示量）、重量（装量）差异检查、含量限度不相关的现象,直接影响药品的质量控制。现分述如下,供制定或修订标准时参考。１　重量（装量）差异检查的比较标准１－１　以标示重量（装量）为比较标准。药典规定：丸剂（按丸服用的）、散剂、冲剂（无含量测定项）、糖浆剂、合剂、胶囊剂（无含量测定项）、…     

浅析中国药典溶出度判断标准

《中国药典》1995年版溶出度测定的复试判断标准:如6片(个)中有1片低于Q-10%,应另取6片(个)复试;初、复试的12片(个)中仅有1一2片(个)低于Q-10%,且其平均溶出量不低于规定限度时,亦可判为符合规定。对该复试判断标准拟提出以下问题及建议同药学工作同仁讨论。     

关于《中国药典》2000年版丸剂重量差异检查方法的商榷

《中国药典》 2 0 0 0年版一部附录ＩＡ丸剂的[重量差异 ]检查方法分为两种 :按丸服用的丸剂照第一法检查 ,按重量服用的丸剂照第二法检查。与 1995年版药典相比较 ,第一法未作修订 ,仍要求将测定结果与标示总量或标示重量相比较后 ,按药典附表规定 ,判断是否符合限度要求 ;第二法稍作修改 ,增加了“有标示量的与标示量相比较”的规定 ,扩大了适用范围。但在实际执行过程中 ,仍然存在某些不能按第一法检查的品种。因为若无标示重量或无法确定标示重量 ,则无法按第一法检查。由于药典所具有的法规严肃性 ,既然要求按第一法检查 ,则不允许以第…     

制剂压片中的常见的问题及解决方法探讨

在压片机压片过程中,会遇到一些问题,如重量差异超限、硬度不足、顶裂、崩解时间延长等.上述问题,有的在压片开始时出现;有的在压片的某一时段出现.既有物料方面的原因,又有设备方面的原因.要做到具体问题具体分析,及时发现问题及时解决,确保生产出合格的产品. 1重量差异超限 药片重量差异较大,无法保证患者用药剂量.<药典>规定0.30克以下药片的重量差异限度为±7.5%,0.30克或0.30克以上的药片重量差异限度为±5%.引起重量差异的原因有物料和机械两方面的因素. 1.1压片过程中由于待压混合物流动性较差或待压混合物粒径相差悬殊,会产生较大的重量差异.这是高速压片中存在的问题之一.     

病区药房6种掰分药品微生物污染状况及重量差异的考察

目的:考察掰分药品微生物污染状况及重量差异。方法:对6种掰分药品的微生物限度及重量差异按《中国药典》(2005年版)要求考察。结果:6种掰分药品的重量差异均不符合《中国药典》(2005年版)规定,并有不同程度的微生物污染。结论:随手掰药存在剂量和质量隐患,不利于病人安全、有效使用药品。需加强规范使用管理。     

中药制剂的重量(装量)差异检查的质控探讨

重量(装量)差异是药物制剂的重要质量指标,与药物制剂的含量限度密切相关。正确理解重量(装量)差异与含量限度的相互关系对药物制剂的生产与检验有重要意义。 国家药品标准(药典及部颁标准)和地方药品标准的部分品种存在着规格(标示量)、重量(装量)差异检查、含量限度不相关的现象,直接影响药品的质量控制。现分述如下,供制定或修订标准时参考。     

对掰分药片重量差异及微生物污染的考察

目的:提高用药安全性和有效性。方法:对5种掰分药片的重量差异及微生物限度按《中国药典》要求进行考察。结果:5种掰分药片的重量差异不符合《中国药典》规定,并有不同程度的微生物污染。结论:建议制药企业增加适合小儿、妇女、老人及特殊病人使用的剂量规格药品。如必须掰分药品,药剂人员应采用无菌法在超净化工作台上将药品掰开分装在环氧乙烷灭菌塑料小袋中,并于当天用于病人。     

中成药制剂重（装）量差异计算方法

目前,在制剂重（装）量差异检查计算中,检验人员经常忽视或者不清楚怎样按照药典凡例规定把限度值的最后一位数字看成有效位去运算,从而造成人为计算误差,缩小了制剂重（装）量差异允许范围,怎样把限度值作为有效限度值运用到重（装）量差异计算中去？为了工作上的方便,能不能把直接同标示总量或标示重（装）量相比较的九散颗粒剂的重（装）量差异允许范围预先计算出来？我们依照国家标准数值修约规则和检查中所要求的“精密称定”及“称定”出来的重（装）量数值的有效位数,通过计算分析、验证归纳出一种制剂重（装）量差异计算方法…     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg.kg) or i.p. (50 mg.kg) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) l.h. kg in the male rat and 10.6 (95% CI: 7.5, 15.0) l.h. kg in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p 0.001) in plasma obtained from the male (8.8 2.0%) compared with the female rat (11.7 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

Quantitative in vivo and in vitro sex differences in artemisinin metabolism in rat

1. The pharmacokinetics of the antimalarial compound artemisinin were compared in the male and female Sprague-Dawley rat after single dose i.v. (20 mg x kg(-1)) or i.p. (50 mg x kg(-1)) administration of an emulsion formulation. 2. Plasma clearance of artemisinin was 12.0 (95% confidence interval: 10.4, 13.0) 1 x h(-1) x kg(-1) in the male rat and 10.6 (95% CI: 7.5, 15.0) 1 x h(-1) x kg(-1) in the female rat suggesting high hepatic extraction in combination with erythrocyte uptake or clearance. Artemisinin half-life was approximately 0.5 h after both routes of administration in both sexes. Values for plasma clearance and half-lives did not statistically differ between the sexes. 3. After i.p. administration artemisinin AUCs were 2-fold higher in the female compared with male rat (p < 0.001). Artemisinin disappearance was 3.9-fold greater in microsomes from male compared with female livers and it was inhibited in male microsomes by goat or rabbit serum containing antibodies against CYP2C11 and CYP3A2 but not CYP2B1 or CYP2E1. 4. The unbound fraction of artemisinin in plasma was lower (p < 0.001) in plasma obtained from the male (8.8 +/- 2.0%) compared with the female rat (11.7 +/- 2.2%). 5. The possibility of a marked sex difference, dependent on the route of administration, has to be taken into account in the design and interpretation of toxicological studies of artemisinin in this species.     

Interindividual variability in metabolic activation in humans in vivo

In assessing interindividual variability in metabolic activation, the toxic metabolite is often too unstable for conventional analysis. Possible alternatives include a stable product of the reactive metabolite e.g. cysteinyl derivatives of N-acetyl-4-benzoquinoneimine, the toxic metabolite of paracetamol, adducts with DNA or protein, and indirect measurement of the activity of the enzyme(s) producing the active metabolite. An example of the last approach is the use of furafylline, a highly specific inhibitor of human CYP1A2, to determine the extent of the metabolic activation of the cooked food mutagens PhIP and MeIQx. The extent of inhibition, determined from levels of unchanged amine in urine, is an indirect measure of the activity of the activation pathway. Further refinement of this approach, allied to improved measures of the biological process of interest should prove of value in evaluating interindividual variability and its role in the risk assessment process.     

Theophylline kinetics in peripheral tissues in vivo in humans

Several biochemical and cellular effects have been described for methylxanthines under in vitro conditions. However, it is unknown, whether threshold concentrations required to exert these effects are attained in target tissues in vivo. We therefore employed the microdialysis technique for measuring theophylline concentrations in peripheral tissues under in vivo conditions.Following in vitro and in vivo calibration, microdialysis probes were inserted into the medial vastus muscle and into the periumbilical subcutaneous adipose layer of healthy volunteers. Following single oral dose administration of 300 mg or i.v. infusion of 240 mg theophylline, in vivo time courses of theophylline concentrations were monitored in tissues and plasma. Major pharmacokinetic parameters (c_max, t_max, AUC) were calculated for plasma and tissue time courses. The mean AUC_tissue /AUC_plasma-ratio was 0.56 (p.o.) and 0.55 (i.v.) for muscle and 0.55 (p.o.) and 0.72 (i.v.) for subcutaneous adipose tissue.We conclude that microdialysis provides important information on the distribution and the tissue pharmacokinetics of theophylline.Abbreviations FPIA Fluorescence polarisation immuno assay - AUC Area under the curve - t_max Time to peak concentration - c_max Peak concentration     

休克时血中氧自由基的变化

本实验测定10名休克患者血浆和红细胞的丙二醛(MDA)、血浆总抗的氧化活性(AOA)的含量。结果表明:休克病人红细胞膜和血浆 MDA 含量(4.298±0.722;5.348±0.834)与对照组(3.235±0.682;4.356±1.081)比较明显增高(P<0.05);血浆 AOA(39.65±7.858)与对照组(48.21±10.81)比较明显降低(P<0.01)。提示:休克时,患者机体内自由基反应增强是引起组织细胞损伤的原因之一。     

Changes in angiopoietin expression in glomeruli involved in glomerulosclerosis in rats with daunorubicin-induced nephrosis

AIM: To study the potential pathological role of endogenous angiopoietins in daunorubicin-induced progressive glomerulosclerosis in rats. METHODS: Seventy male Wistar rats were allocated randomly into a daunorubicin group (DRB; n=40) or a control group (n=30). The rats in the DRB group were injected with DRB (15 mg/kg), in their tails. Subsequently, at intervals of 1, 2, 4, 6, 8, and 12 weeks, 5 male Wistar rats in each group were chosen randomly for 24 h urinary protein quantitative measurements (24 h UPQM), and determination of plasma tumor necrosis factor alpha (TNF-alpha), angiopoietin-1 (Ang1), and angiopoietin-2 (Ang2) levels. Kidney sections were examined by electron microscopy, Periodic Acid Schiff (PAS) staining, immunohistochemical staining and in situ hybridization histochemistry. RESULTS: As glomerulosclerosis progressed in the DRB group, expression of Ang1 mRNA and protein in glomeruli decreased and expression of TNF-alpha protein, Ang2 mRNA and protein in glomeruli increased. Expression of Ang1 mRNA and protein in glomeruli were negatively correlated with 24 h UPQM, Fn protein expression, and mean area of extracellular matrix (MAECM). In comparison, expression of Ang2 mRNA and protein in glomeruli were positively correlated with 24 h UPQM, Fn protein expression and MAECM; furthermore, there was a positive correlation between plasma Ang2 and 24 h UPQM. Plasma TNF-alpha and expression of TNF-alpha in glomeruli were positively correlated with expression of Ang2 mRNA and protein in glomeruli. There was a negative correlation between Ang1 protein expression and Ang2 protein expression in glomeruli. CONCLUSION: During DRB-induced glomerulosclerosis, podocyte injury led to a shift in the balance of Ang1 and Ang2 in glomeruli. Increased TNF-alpha in plasma and glomeruli may upregulate Ang2 expression in glomeruli. Elevated Ang2 in both plasma and glomeruli may mediate protein permeability through the glomerular filtration barrier. Moreover, local expression of Ang2 may facilitate the progress of glomerulosclerosis by upregulating a component expression of extracellular matrix.     

Trichinellosis in immigrants in Switzerland

We describe a case of trichinellosis diagnosed at the Division of Infectious Diseases, Hospital of Lugano, in January 2009. This case was associated with a cluster of cases and was traced to the consumption of contaminated meat after a wild boar hunt in Bosnia.