目的:研究注射用益气复脉(冻干)Yi Qi Fu Mai Injection(YQFM)(Lyophilized)对大鼠肝微粒体CYP1A2、CYP3A的诱导作用。方法:将wistar大鼠分为生理盐水对照组,苯巴比妥钠诱导组,YQFM组,连续给药7天后处死,制备肝微粒体。采用Cocktail法,...目的:研究注射用益气复脉(冻干)Yi Qi Fu Mai Injection(YQFM)(Lyophilized)对大鼠肝微粒体CYP1A2、CYP3A的诱导作用。方法:将wistar大鼠分为生理盐水对照组,苯巴比妥钠诱导组,YQFM组,连续给药7天后处死,制备肝微粒体。采用Cocktail法,将特异性探针底物非那西丁(CYP1A2)、睾酮(CYP3A)与肝微粒体共孵育,采用高效液相色谱测定孵育所得代谢产物对乙酰氨基酚和6β-羟基睾酮的生成速率,来评价YQFM对CYP1A2、CYP3A的诱导作用。结果:空白对照组、诱导组和YQFM组的对乙酰氨基酚的生成速率分别为(18.04±1.00)、(43.07±2.90)、(27.6±4.5)ng.(mg pro-tein)-1.min-1,6β-羟基睾酮的生成速率分别为(15.79±1.43)、(40.86±3.32)、(32.8±3.67)ng.(mg protein)-1.min-1。结论:YQFM对大鼠肝微粒体CYP1A2、CYP3A有诱导作用。展开更多
Background Multimodal cocktail periarticular injection (MCPI) with a large volume of low concentration local anesthetics, adrenaline, and anti-inflammatory agents such as non-steroidal anti-inflammatory drug or ster...Background Multimodal cocktail periarticular injection (MCPI) with a large volume of low concentration local anesthetics, adrenaline, and anti-inflammatory agents such as non-steroidal anti-inflammatory drug or steroids have shown good pain control and improvement in range of motion after surgery. This study compares the efficacy of pain control after total knee arthroplasty, using multimodal cocktail periarticular injection with steroid or without steroid.展开更多
Objective Re Du Ning Injection (RDN), a Chinese materia medica injection, is made from the extracts of LoniceraeJaponicae Flos, Gardeniae Fructus, and Artemisiae Annuae Herba. Since last decade, RDN has been widely ...Objective Re Du Ning Injection (RDN), a Chinese materia medica injection, is made from the extracts of LoniceraeJaponicae Flos, Gardeniae Fructus, and Artemisiae Annuae Herba. Since last decade, RDN has been widely used in China for the treatment of viral infection, fever, and inflammation. To assess the potential interacting of RDN with co-administered drugs, the inhibitory effects of RDN on the enzyme activities (CYP1A1, CYP1A2, CYP2C11, CYP2D1, and CYP3A1/2) of rat liver microsomes were investigated by a cocktail method. Methods A sensitive and specific LC-MS method capable of simultaneous quantification of five metabolites in rat liver microsomes was developed and validated. Then RDN (0.625%-1.0%) was incubated with rat liver microsomes and specific substrates. The enzyme activities were expressed as the formation rate of the specific metabolites of the substrates (pmol- mg. protein-1 . min-1). Results RDN competitively inhibited the activities of CYP1A2 and CYP2C11, with inhibition constant (/~) values determined to be 0.18% and 0.63%, respectively. RDN exhibited the mixed inhibition on the activity of CYP2D1, with a K1 value of 0.15%. The activities of CYP1A1 and CYP3A1/2 were not markedly inhibited even by 1.0% RDN. Conclusion RDN could inhibit the rat enzyme activities of CYP1A2, 2Cll, and 2D1 in vitro with different inhibition modes, which is worthy of promoting safety and efficacy of RDN.展开更多
目的评价腘动脉-膝关节后囊间隙(infiltration between the popliteal artery and the capsule of the posterior knee,iPACK)阻滞对比关节周围注射(periarticular injection,PAI)在全膝关节置换(total knee arthroplasty,TKA)术后镇痛...目的评价腘动脉-膝关节后囊间隙(infiltration between the popliteal artery and the capsule of the posterior knee,iPACK)阻滞对比关节周围注射(periarticular injection,PAI)在全膝关节置换(total knee arthroplasty,TKA)术后镇痛中的作用。方法检索PubMed、EMBASE、Web of Science、中国生物医学文献数据库(CBM)、中文科技期刊全文数据库(VIP)、中国期刊全文数据库(CNKI)及万方数据库中iPACK对比PAI对TKA术后镇痛的随机对照试验(RCT),时间均从建库至2021年12月。2位研究者按照纳入标准筛选文献、提取资料,2位评价员独立对纳入文献的质量进行评价,采用RevMan5.3进行meta分析。结果纳入6个RCT共440例患者。与PAI相比,iPACK组术后24 h吗啡累积使用量较少(MD=-4.21,95%CI:-7.18~-1.24,P=0.005),术后12 h运动状态和24、48 h静息状态、运动状态下疼痛视觉模拟评分(Visual Analogue Scale,VAS)降低,差异有统计学意义(P<0.05),术后12 h静息状态VAS差异无统计学意义(P>0.05);2组术后第1天、第2天行走距离相当,差异无统计学意义(P>0.05)。结论与PAI相比,iPACK阻滞能更有效地减轻TKA术后疼痛,减少阿片类药物用量,不影响术后活动,用于TKA术后镇痛安全有效。展开更多
文摘目的:研究注射用益气复脉(冻干)Yi Qi Fu Mai Injection(YQFM)(Lyophilized)对大鼠肝微粒体CYP1A2、CYP3A的诱导作用。方法:将wistar大鼠分为生理盐水对照组,苯巴比妥钠诱导组,YQFM组,连续给药7天后处死,制备肝微粒体。采用Cocktail法,将特异性探针底物非那西丁(CYP1A2)、睾酮(CYP3A)与肝微粒体共孵育,采用高效液相色谱测定孵育所得代谢产物对乙酰氨基酚和6β-羟基睾酮的生成速率,来评价YQFM对CYP1A2、CYP3A的诱导作用。结果:空白对照组、诱导组和YQFM组的对乙酰氨基酚的生成速率分别为(18.04±1.00)、(43.07±2.90)、(27.6±4.5)ng.(mg pro-tein)-1.min-1,6β-羟基睾酮的生成速率分别为(15.79±1.43)、(40.86±3.32)、(32.8±3.67)ng.(mg protein)-1.min-1。结论:YQFM对大鼠肝微粒体CYP1A2、CYP3A有诱导作用。
文摘Background Multimodal cocktail periarticular injection (MCPI) with a large volume of low concentration local anesthetics, adrenaline, and anti-inflammatory agents such as non-steroidal anti-inflammatory drug or steroids have shown good pain control and improvement in range of motion after surgery. This study compares the efficacy of pain control after total knee arthroplasty, using multimodal cocktail periarticular injection with steroid or without steroid.
基金National Science and Technology Major Project“Creation of Major New Drugs”from China(No.2013ZX09402203)Natural Science Foundation of Jiangsu Province(No.BK2013403)
文摘Objective Re Du Ning Injection (RDN), a Chinese materia medica injection, is made from the extracts of LoniceraeJaponicae Flos, Gardeniae Fructus, and Artemisiae Annuae Herba. Since last decade, RDN has been widely used in China for the treatment of viral infection, fever, and inflammation. To assess the potential interacting of RDN with co-administered drugs, the inhibitory effects of RDN on the enzyme activities (CYP1A1, CYP1A2, CYP2C11, CYP2D1, and CYP3A1/2) of rat liver microsomes were investigated by a cocktail method. Methods A sensitive and specific LC-MS method capable of simultaneous quantification of five metabolites in rat liver microsomes was developed and validated. Then RDN (0.625%-1.0%) was incubated with rat liver microsomes and specific substrates. The enzyme activities were expressed as the formation rate of the specific metabolites of the substrates (pmol- mg. protein-1 . min-1). Results RDN competitively inhibited the activities of CYP1A2 and CYP2C11, with inhibition constant (/~) values determined to be 0.18% and 0.63%, respectively. RDN exhibited the mixed inhibition on the activity of CYP2D1, with a K1 value of 0.15%. The activities of CYP1A1 and CYP3A1/2 were not markedly inhibited even by 1.0% RDN. Conclusion RDN could inhibit the rat enzyme activities of CYP1A2, 2Cll, and 2D1 in vitro with different inhibition modes, which is worthy of promoting safety and efficacy of RDN.
文摘目的评价腘动脉-膝关节后囊间隙(infiltration between the popliteal artery and the capsule of the posterior knee,iPACK)阻滞对比关节周围注射(periarticular injection,PAI)在全膝关节置换(total knee arthroplasty,TKA)术后镇痛中的作用。方法检索PubMed、EMBASE、Web of Science、中国生物医学文献数据库(CBM)、中文科技期刊全文数据库(VIP)、中国期刊全文数据库(CNKI)及万方数据库中iPACK对比PAI对TKA术后镇痛的随机对照试验(RCT),时间均从建库至2021年12月。2位研究者按照纳入标准筛选文献、提取资料,2位评价员独立对纳入文献的质量进行评价,采用RevMan5.3进行meta分析。结果纳入6个RCT共440例患者。与PAI相比,iPACK组术后24 h吗啡累积使用量较少(MD=-4.21,95%CI:-7.18~-1.24,P=0.005),术后12 h运动状态和24、48 h静息状态、运动状态下疼痛视觉模拟评分(Visual Analogue Scale,VAS)降低,差异有统计学意义(P<0.05),术后12 h静息状态VAS差异无统计学意义(P>0.05);2组术后第1天、第2天行走距离相当,差异无统计学意义(P>0.05)。结论与PAI相比,iPACK阻滞能更有效地减轻TKA术后疼痛,减少阿片类药物用量,不影响术后活动,用于TKA术后镇痛安全有效。