吉非罗齐胶囊剂的相对生物利用度

8名健康受试者口服两种吉非罗齐胶囊剂后,血清样品经提取、甲酯化,以气相色谱法测定吉非罗齐的含量。其血药浓度-时间过程符合一房室模型。国产制剂的药代动力学参数分别为:k_a=2.97±2.84h^(-1),k=0.761±0.215h^(-1),t_(max)=1.42±0.83h,C_(max)=21.68±6.50mg/l,t_0=0.65±0.52h,V/F=0.122±0.040l,AUC=61.4±14.0mg·h/l。国外制剂的药代动力学参数分别为:k_a=3.26±2.94h^(-1),k=0.712±0.266h^(-1),t_(max)=1.26±0.54h,C_(max)=18.56±7.46mg/l,t_0=0.33±0.43h,V/F=0.153±0.045l,AUC=53.74±10.57mg·h/l。两者相对生物利用度F=1.14。4名受试者3次服药的峰浓度与谷浓度同单剂量给药的药代动力学参数结果的拟合值较为一致。

吉非罗齐胶囊的药动学及相对生物利用度

目的 :研究吉非罗齐胶囊在人体内的药代动力学及相对生物利用度。方法 :采用反相高效液相色谱法测定 1 0名受试者单剂量口服 60 0mg吉非罗齐供试胶囊与参比胶囊后的血药浓度变化情况。结果 :药时曲线下面积分别为 (95 .71± 1 0 .0 4 ) μg·h·ml- 1 与 (96 .55± 1 0 .78) μg·h·ml- 1 ,达峰时间分别为 (2 .0 5± 0 .44)h与 (2 1 0±0 39)h ,峰浓度分别为 (2 9.80± 2 .60 ) μg·ml- 1 与 (2 9.35± 4 .47) μg·ml- 1 ,均无显著性差异 (P >0 .0 5) ,供试胶囊的相对生物利用度为 99.72 %± 1 0 .76 %。结论

吉非罗齐片和胶囊在健康人体内药物动力学和相对生物利用度比较

目的:测定吉非罗齐的体内过程,作出相对生物利用度评价,为临床合理用药提供依据.方法:8名健康受试者交叉口服单剂量古非罗齐片和胶囊后,用HPLC法测定不同时间的血药浓度,经MCPKP软件拟合处理,并计算药物动力学参数.结果:吉非罗齐片和胶囊均符合开放一室模型,T_(max),C_(max),AUC_(0～∞)分别为(1.61±0.49)和(1.66±0.47)h,(37.28±9.71)和(29.97±5.58)μg/ml;(128.48±24.36)和(119.55±19.48)μg/(h·ml).结论:吉非罗齐片剂对胶囊剂的相对生物利用度为107.26%.

吉非罗齐合成工艺的研究

本文通过实验改进吉非罗齐的合成工艺,该工艺的特点是改变 C-C 键的切割位置,达到以格氏试剂代替锂试剂,从而降低成本,提高收率。

小剂量吉非罗齐治疗高脂血症的疗效观察

近年来,我院对以甘油三脂(TG)增高为主的高脂血症患者采用小剂量吉非罗齐治疗,取得满意疗效,总结分析如下。

血脂康和吉非罗齐对2型糖尿病合并高脂血症调脂作用的比较

单一对糖尿病患者进行降糖治疗,对糖尿病患者并发症的控制极其不利。我们采取综合治疗,在降糖的同时,对并发有高脂血症的患者给予调脂药,观察比较了血脂康。

益气活血法治疗高脂血症临床观察

观察益气活血法治疗高脂血症的疗效 ,随机分设益气活血治疗组 (黄芪、苍术、白术、红花、桃仁、川芎、丹参 ) 60例 ,与吉非罗齐对照组 3 0例进行疗效比较 ,疗程均为 8周。结果 :在降血脂方面 ,治疗组与对照组的总有效率分别为5 1 66%和 5 0 0 0 % (P >0 .0 5 ) ;在改善症状方面分别为 71 66%和 5 3 3 4 % ,治疗组疗效优于对照组 (P <0 .0 5 )。

RAPD-SCAR Markers for Genetically Improved NEW GIFT Nile Tilapia (Oreochromis niloticus niloticus L.) and Their Application in Strain Identification

The NEW GIFT Nile tilapia （Oreochromis niloticus niloticus L.） is a nationally certificated new strain selected over 14 years and 9 generations from the base strain of GIFT Nile tilapia, introduced in 1994. This new variety has been extended in most of areas of China. The management of genetically improved strains, including the genetic markers for identification is needed urgently. RAPD analysis was conducted and their conversion to SCAR markers was developed. From NEW GIFT Nile tilapia, two strain-specific RAPD bands, S304624 bp and S36568 bp were identified. The strain-specific RAPD bands were gel-purified, cloned, and sequenced. Locus-specific primers were then designed to amplify the strain-specific bands. PCR amplification was conducted to test the variations in allele frequencies of two converted SCAR markers among the NEW GIFT Nile tilapia and its base strains, as well as 7 additional farmed strains worldwide. The frequency of SCAR marker Ⅰ （553 bp） was 85.7% in NEW GIFT Nile tilapia, but 16.7% in the base strain. The frequency of SCAR marker Ⅱ （558 bp） was 91.4% in NEW GIFT Nile tilapia, but 0% 70% in the 7 other strains. In order to confirm the utility of these two markers, an examination was conducted for a wild population from Egypt, resulted the frequency of SCAR Ⅰ and Ⅱ was 10% and 70%, respectively, much lower than that of New GIFT strain. The increase in allele frequency of these two SCAR markers suggests that these markers might be genetically linked to the quantitative trait loci （QTL） underlining the performance traits by long term selection, and indicate the bright potential of SCAR marker technology for tracking generations during selection progress and for distinguishing among genetically improved strain and other strains.

Effects of Copper and Manganese on Hemocyte Apoptosis and Antagonism of Iron and Zinc in Oreochromis niloticus

This study aimed to investigate the effects of copper and manganese on hemocyte apoptosis and the antagonism of iron and zinc in Oreochromis niloticus The heavy metal contents in fish blood and feed were determined by atomic absorption spectrophotometry, and the hemocyte apoptosis was determined by flow cytometry. A total of 360 tilapias were selected, and they were divided randomly and evenly into 12 groups. In the challenge groups, the tilapias were fed with con stant-level copper sulfate（0, 200 mg/kg） and manganese sulfate（0, 120 mg/kg）; in the antagonism groups, the tilapias were fed with constant-level zinc sulfate（20320 mg/kg） and iron sulfate（150, 350 mg/kg）. After 20-week aquaculture, the hemocyte apoptosis rates in the copper and manganese groups were significantly increased; with the increased addition levels of iron and zinc, the hemocyte apopto sis rates in the iron and zinc groups were significantly reduced, but they were stil higher than that in the control group. In conclusion, excessive copper and manganese can cause apoptosis in hemocytes of O. niloticus. However, the toxic effects of copper and manganese can be antagonized by iron and zinc.