Pharmacokinetics and Pharmacodynamics of a Depolymerized Glycosaminoglycan from Holothuria fuscopunctata,a Novel Anticoagulant Candidate,in Rats by Bioanalytical Methods

dHG-5 (Mw 5.3 kD) is a depolymerized glycosaminoglycan from sea cucumber Holothuria fuscopunctata. As a selective inhibitor of intrinsic Xase (iXase), preclinical study showed it was a promising anticoagulant candidate without obvious bleeding risk. In this work, two bioanalytical methods based on the anti-iXase and activated partial thromboplastin time (APTT) prolongation activities were established and validated to determine dHG-5 concentrations in plasma and urine samples. After single subcutaneous administration of dHG-5 at 5, 9, and 16.2 mg/kg to rats, the time to peak concentration (T_max) was at about 1 h, and the peak concentration (C_max) was 2.70, 6.50, and 10.11 μg/mL, respectively. The plasma elimination half-life(T_1/2β) was also about 1 h and dHG-5 could be almost completely absorbed after s.c. administration. Additionally, the pharmacodynamics of dHG-5 was positively correlated with its pharmacokinetics, as determined by rat plasma APTT and anti-iXase method, respectively. dHG-5 was mainly excreted by urine as the unchanged parent drug and about 60% was excreted within 48 h. The results suggested that dHG-5 could be almost completely absorbed after subcutaneous injection and the pharmacokinetics of dHG-5 are predictable. Studying pharmacokinetics of dHG-5 could provide valuable information for future clinical studies.     

金莲花植物成分及其药剂的研究进展

综述了金莲花的植物学及植物化学、成分分析、药理作用、临床应用及制剂等方面的研究状况，并对目前研究存在的问题及以后的发展前景进行了讨论。     

氨基糖苷类药物抗生素后效应的研究进展

对氨基糖苷类药物抗生素后效应的产生机制、体内外的研究方法、影响因素及常用氨基糖苷类药物抗生素后效应的研究现状进行概述,为评价氨基糖苷类药物的药效学指标和在兽医临床的合理应用提供理论基础。     

治疗多重耐药革兰氏阴性菌感染的有效抗菌药——多黏菌素

综述了多黏菌素的理化性质、抗菌活性、药动学、药效学、临床应用、残留等方面的特点和研究概况,以期为该药在兽医临床上的应用提供依据。     

新型莫西菌素浇泼剂对羊蜱蝇和消化道线虫驱虫药效评价

试验旨在通过新型莫西菌素（moxidectin,MOX）浇泼剂对羊的驱虫试验,评价MOX浇泼剂对羊蜱蝇和消化道线虫的临床药效。将150只阿勒泰羊经产母羊随机分为6组,每组25只,分别为不用药对照组、螨净药浴组、MOX注射组和MOX低（0.05 mL/（kg·BW））、中（0.1 mL/（kg·BW））和高（0.2 mL/（kg·BW））剂量浇泼组,试验期为1周。试验第1天按前述分组中方法和剂量驱虫1次。观察受试动物临床表现,测定给药前1天和给药后第7天体温、脉搏和呼吸（TPR）,血液生理、生化和尿常规指标;测定羊蜱蝇减虫率、治愈率。采取粪样测定消化道线虫每克粪中虫卵个数（EPG）减少率及转阴率。结果显示,与不用药对照组相比,给药后第7天各驱虫组TPR、血液生理、生化及尿常规指标均无显著差异（P>0.05）。螨净药浴组羊蜱蝇减虫率为43.7%,而MOX注射组及MOX低、中、高剂量浇泼组均为100%。螨净药浴组治愈率为13.0%,而MOX注射组及MOX低、中、高剂量浇泼组均为100%;与不用药对照组相比,螨净药浴组消化道线虫卵减少率为0,而MOX注射组及MOX低、中、高剂量浇泼组分别为91.6%、93.1%、94.9%和97.8%。螨净药浴组虫卵转阴率为0,而MOX注射组及MOX低、中、高剂量浇泼组分别为77.0%、69.2%、69.2%和84.6%。本试验结果表明,新型MOX浇泼剂对体外寄生虫和消化道线虫均有显著疗效,且优于螨净药浴,与MOX注射剂等效。实践应用中最适MOX浇泼剂量推荐为0.05 mL/（kg·BW）（即0.25 mg/（kg·BW））。     

盐酸吡利霉素治疗奶牛乳房炎临床药效学及对乳品质影响的研究

本研究依据对黑龙江省部分牧场奶牛乳房炎致病菌分离鉴定以及药敏试验结果,选取盐酸吡利霉素、头孢噻呋钠和复方阿莫西林为试验药物,对患有隐性乳房炎的奶牛进行治疗并对乳品质进行跟踪监测。结果表明盐酸吡利霉素对隐性乳房炎的治愈率最高,对临床型乳房炎的治疗效果略差于复方阿莫西林,盐酸吡利雷素与复方阿莫西林对两种类型乳房炎治疗的总有效率相当,但盐酸吡利霉素对乳品质（尤其是降低体细胞数方面）的改善作用显著好于复方阿莫西林治疗组。     

几种杀菌剂对南方红豆杉炭疽病的田间药效测定

在田间药效测定中,喷雾和注干两种施药方法相比,喷雾防治的效果明显好于注干的防治效果。喷雾试验中,防治效果最好的是甲基托布津,平均防治效果达到78.79%,最差的是退菌特,平均防治效果为57.20%;在注干防治试验中,防治效果最好的依然为甲基托布津,为62.50%,其次为炭克、多菌灵,最差的为退菌特,为46.57%。     

黄葵素对结核分枝杆菌的抑杀作用研究

Objective To evaluate the antituberculous activities of Huangkuisu (HISS). Meth-ods lOStandard human strains of mycobacterium tuberculosis (H37RV) and multi-drug resistant TBstrainswere inoculated in different concentrations of HISS, blank control and positive TB drug culture medium[()observe the growth of mycobacterium tuberculosis and evaluate the antibacterial activity in vitro.②Certain number of standard strains of Mycobacterium tuberculosis H37Rv and drug-resistant strains were injected into the tail vein[()establish a mouse model of mycobacterium tuberculosis infection. The mice were randomly divided into treatment group, rifampicin, HISS treatment group treated lasting for 6 weeks; the control group was given normal saline. The antibacterial activity in vivo were evaluated[()compare the treatment results according[()the pathological changes in lung and spleen tissues (HE staining and acid-fast staining) and charging amount of bacteria. Results lOthe bactreial colonies were grew normally in model group, but were not grew in     

兽用抗寄生虫药莫奈太尔的研究进展

概述了一种新型氨基乙腈衍生物类驱虫药莫奈太尔的理化性质、作用机制、药代动力学、药效学等特点,以期为该药在兽医临床应用提供参考。     

Pharmacokinetics,tissue residues,and ex vivo pharmacodynamics of tylosin against Mycoplasma anatis in ducks

The pharmacokinetics of tylosin were investigated in 3 groups of ducks (n = 6). They received a single dose of tylosin (50 mg/kg) by intravenous (IV), intramuscular (IM), and oral administrations, respectively. Plasma samples were collected at various time points to 24 hr post-administration to evaluate tylosin concentration over time. Additionally, tylosin residues in tissues and its withdrawal time were assessed using 30 ducks which received tylosin orally (50 mg/kg) once daily for 5 consecutive days. After IV administration, the volume of distribution, elimination half-life, area under the plasma concentration–time curve, and the total body clearance were 7.07 ± 1.98 L/kg, 2.04 hr, 19.47 µg hr/ml, and 2.82 L hr⁻¹ kg⁻¹, respectively. After IM and oral administrations, the maximum plasma concentrations were 3.70 and 2.75 µg/ml achieved at 1 and 2 hr, and the bioavailability was 93.95% and 75.77%, respectively. The calculated withdrawal periods of tylosin were 13, 8, and 5 days for kidney, liver, and muscle, respectively. For the pharmacodynamic profile, the minimum inhibitory concentration for tylosin against M. anatis strain 1,340 was 1 µg/ml. The calculated optimal oral dose of tylosin against M. anatis in ducks based on the ex vivo pharmacokinetic/pharmacodynamic modeling was 61 mg kg⁻¹ day⁻¹.