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机构地区:[1]新疆维吾尔自治区维吾尔医药研究所新疆维吾尔医方剂学实验室,乌鲁木齐830049 [2]新疆银朵兰维药股份有限公司,乌鲁木齐830013
出 处:《西北药学杂志》2017年第3期322-326,共5页Northwest Pharmaceutical Journal
基 金:新疆维吾尔自治区专利实施计划项目(编号:2009002);乌鲁木齐市科学技术计划项目(编号:C111110002)
摘 要:目的研究尿通卡克乃其的躯体依赖性作用,评价其安全性。方法采用大鼠自然戒断和催促戒断实验进行躯体依赖性实验。大鼠自然戒断实验,恒量给药30d,观察给药期间和停药后大鼠的一般状况和体质量变化;大鼠催促戒断实验,递增给药14d,给药第13天采用自主活动实验,测定大鼠的活动性,末次给药后2h,腹腔注射盐酸纳洛酮,评价躯体戒断症状。结果在大鼠自然戒断实验中,尿通卡克乃其低、中、高剂量组给药期间以及停药后大鼠未出现明显戒断反应和体质量下降现象;催促戒断实验中尿通卡克乃其低、中、高剂量组给药期间以及停药后大鼠未出现体质量明显下降现象,递增给药13d时,尿通卡克乃其高剂量组明显降低大鼠活动次数、活动总时间、修饰次数以及增加排便粒数,腹腔注射盐酸纳洛酮戒断后,尿通卡克乃其高剂量组的120min总评分明显升高,大鼠出现显著性催促戒断反应症状。结论尿通卡克乃其在正常口服剂量范围内,致依赖性风险低,临床应用较安全。Objective To investigate the potential physical dependence of Kursi Kaknaq and evaluate its drug safety.Methods The nature withdrawal and the precipitation withdrawal experiments were used in the present study.In the nature withdrawal experiments in rats,the drug was given in constant dose for 30 days,and the general conditions and body weight change were observed during the treatment period and the rest period.In the precipitation withdrawal experiments in rats,Kursi Kaknaq was used intragastrically according to a progressively increasing program for 14 days.On the 13 th day,the spontaneous activity experiment was used to study the changes of behavior.Then rats were injected intraperitoneally with naloxone hydrochloride at 2hours after the final administration,and the withdrawal syndromes were evaluated.Results In the nature withdrawal experiments,the withdrawal syndromes were not observed and rats body weight did not significantly change in low dosage group,middle dosage group and high dosage group of Kursi Kaknaq during the treatment period and the rest period.In the precipitation withdrawal experiments,the results showed that rats body weight did not significantly change in low dosage group,middle dosage group and high dosage group of Kursi Kaknaq during the treatment period and the rest period,but high dosage group of Kursi Kaknaq can obviously decrease the rats activity frequency,activity times and modification times and fecal pellet on the 13 th day;Kursi Kaknaq high-dose group showed significantly withdrawal syndromes precipitated by naloxone at 120 min.Conclusion Within the normal oral dose range of Kursi Kaknaq,the potential of physical dependence is quite weak and clinical application is safe.
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