Aflatoxin B1 (AFB1) is a potent hepatotoxin that induces oxidative stress, inflammation, and mitochondrial dysfunction. Dipsacoside B (DB), a bioactive triterpenoid saponin from Flos Lonicerae (Shanyinhua), is recognized for its antioxidant, anti-inflammatory, and cytoprotective properties. This study investigates the protective effects of DB against AFB1-induced liver injury and the underlying mechanisms. Male C57BL/6 mice were assigned to control, AFB1, DB, and AFB1 + DB groups, receiving oral treatments for 4 weeks. The results showed that DB significantly alleviated AFB1-induced weight loss and liver damage, as evidenced by histopathological changes and serum biochemical markers. DB reduced hepatic H₂O₂ and MDA levels, enhanced the activities of antioxidant enzymes such as T-SOD, GSH-Px, CAT, and total antioxidant capacity (T-AOC), inhibited the expression of IL-6, IL-1β, and TNF-α genes, and modulated metabolic enzymes by downregulating Phase I genes (CYP1A2, CYP3A11) while upregulating the Phase II gene GSTA3. Notably, DB upregulated AFB1-suppressed Nrf2 and its downstream targets (HO-1, NQO1, SOD1, GCLC, GCLM, GSS). DB also reversed AFB1-induced mitochondrial damage, including swelling and cristae disruption, and inhibited apoptosis by restoring Bcl-2 and reducing p53, Bax, Cyt-c, caspase-9, and caspase-3 expression. These findings suggest that DB protects against AFB1-induced liver injury by regulating oxidative stress, inflammation, apoptosis, and metabolic enzymes, suggesting it has significant potential as a therapeutic strategy for aflatoxin-related hepatic disorders.

IntroductionMacranthoidin B (MB) is a primary active component of Flos Lonicerae. In Chinese veterinary clinics, Flos Lonicerae is frequently used in combination with florfenicol to prevent and treat infections in livestock and poultry. However, potential interactions between Flos Lonicerae and florfenicol remain unclear. To systematically study these interactions, it is crucial to investigate the individual phytochemicals within Flos Lonicerae. Therefore, MB was selected for this study to assess its effect on the pharmacokinetics of florfenicol in vivo and to explore the underlying mechanisms involved.MethodsMale Sprague-Dawley rats were administered MB (60 mg/kg BW) or sterile water orally for 7 consecutive days. On the 8th day, a single oral dose of florfenicol (25 mg/kg BW) was given. Florfenicol pharmacokinetics were analyzed using ultra-high performance liquid chromatography. The hepatic expression levels of cytochrome P450 (CYP1A2, CYP2C11, CYP3A1), UDP-glucuronosyltransferase (UGT1A1), P-glycoprotein (P-gp), and nuclear receptors, including constitutive androstane receptor (CAR), pregnane X receptor (PXR), and retinoid X receptor alpha (RXRα), were quantified via reverse transcription-quantitative polymerase chain reaction and Western blotting (WB). Hepatic CYP1A2 and CYP2C11 activities were measured using a cocktail method. Additionally, the subcellular expression and localization of CAR, PXR, and RXRαin hepatocytes was assessed using WB and immunofluorescence staining.ResultsMB significantly reduces the AUC(0-∞) and MRT(0-∞) of florfenicol. MB also markedly upregulates the mRNA and protein expression of hepatic CYP1A2 and CYP2C11, along with their catalytic activities. Substantial upregulation of CAR and PXR proteins occurs in the hepatocyte nucleus, along with significant nuclear colocalization of the transcriptionally active CAR/RXRα and PXR/RXRαheterodimers, indicating MB-induced nuclear translocation of both CAR and PXR.DiscussionThese findings suggest that MB-induced alterations in florfenicol pharmacokinetics, particularly its accelerated elimination, may be due to increased expression and activities of CYP1A2 and CYP2C11, with CAR and PXR potentially involved in these regulatory effects. Further investigation is yet needed to fully elucidate the clinical implications of these interactions concerning the efficacy of florfenicol in veterinary medicine.

为了探究川射干提取物对急性肺损伤的防治效果及其对TLR4/NF-κB信号通路相关蛋白表达的影响,试验将 24 只雌性 Balb/c 小鼠随机分为空白对照(CTR)组、模型(LPS)组、地塞米松(DEX)组及川射干提取物(ITR)组,每组 6 只.ITR 组每只每天灌胃 12.5 mg/mL 川射干提取物0.2 mL,其他组灌胃等体积生理盐水,连续7 d.末次给药 1 h后,LPS组、DEX组和ITR组每只小鼠腹腔注射1 mg/mL脂多糖0.2 mL造模,CTR组腹腔注射等体积生理盐水.DEX组于造模前 1 小时每只小鼠腹腔注射0.5 mg/mL地塞米松0.2 mL.造模6 h后采集血液,制备血清;处死各组小鼠,分别采集肺泡灌洗液(BALF)和肺脏,通过ELISA法检测血清和肺泡灌洗液中趋化因子 1(CXCL1)、肿瘤坏死因子-α(TNF-α)、白细胞介素(IL)-1β、IL-6、IL-8 和IL-10 的含量;对肺脏组织进行H.E.染色,观察肺脏病理变化;通过Western-blot检测Toll样受体4(TLR4)、核因子κB(NF-κB)信号通路相关蛋白的表达情况.结果表明:与LPS组相比,ITR组血清和肺泡灌洗液中CXCL1、TNF-α、IL-1β、IL-6、IL-8 含量均显著或极显著下降(P<0.05 或P<0.01),IL-10 含量显著或极显著升高(P<0.05 或P<0.01);与LPS组比较,ITR组肺泡内炎症细胞浸润程度明显减轻,仅局部肺泡腔内出现少量巨噬细胞或淋巴细胞浸润.与LPS组比较,ITR组肺脏TLR4、MyD88、TRIF和NF-κB p-p65 蛋白表达量显著或极显著降低(P<0.05 或P<0.01).说明川射干提取物可通过调节TLR4/NF-κB信号通路缓解脂多糖诱导的小鼠急性肺损伤.

Abstract Coptisine (COP) is the main active ingredient of Coptis chinensis. In Chinese veterinary clinics, Coptis chinensis is commonly used alongside florfenicol to treat intestinal infections. The goal of this study was to investigate the impact of COP co-administration on the pharmacokinetics of florfenicol in rats. Male Sprague-Dawley rats were orally administered COP (50 mg/kg BW) or sterile water for 7 consecutive days, followed by a single oral dose of florfenicol (25 mg/kg BW) on the 8th day. Pharmacokinetics of florfenicol were analysed using non-compartmental methods, while expression levels of cytochrome P450 (CYP) isoforms in the liver and P-glycoprotein (P-gp) in the jejunum were measured using real-time RT-PCR, Western blot and immunohistochemical analyses. Co-administration of COP and florfenicol significantly increased AUC(0-∞), MRT(0-∞), and Cmax of florfenicol, while CLz/F was significantly decreased. COP down-regulated the expression of CYP1A2, CYP2C11, and CYP3A1 in the liver, as well as P-gp in the jejunum. These findings suggest that co-administration of COP with florfenicol alters the pharmacokinetics of florfenicol in rats. The down-regulation of CYP and P-gp expression may contribute to this effect. Therefore, the co-administration of COP with florfenicol may enhance the prophylactic or therapeutic efficacy of florfenicol in veterinary practice.

川续断属于川产道地药材,主产于四川攀西等盆周山地,用于防治跌打损伤、崩漏安胎,是临床常用中药材.文章在充分查阅川续断相关文献的基础上对川续断资源分布、化学成分、药理药效、种植现状进行全面的综述,同时对其壮阳、补肝肾、壮筋骨、安胎等药理活性在畜牧业生产中用于种畜保健、母畜保胎及蛋鸡产蛋性能等良好的应用前景进行了阐述,为扩大川续断药材资源在畜禽健康养殖中合理利用以及动保行业开发利用川续断资源提供参考.

Belamcanda chinensis (L.) DC, commonly used with florfenicol in Chinese veterinary clinics for respiratory tract infections, contains the major effective isoflavone, tectoridin (TEC). This study aimed to investigate the impact of TEC co-administration on the pharmacokinetics of florfenicol in vivo. Male rats received oral TEC (50 mg/kg BW) or sterile water for seven days, followed by a single oral dose of florfenicol (25 mg/kg BW) on the 8th day. Non-compartmental methods analysed the pharmacokinetics of florfenicol, while real-time reverse transcription polymerase chain reaction (RT-PCR), Western blot, and immunohistochemical analyses measured expression levels of cytochrome P450 (CYP) isoforms in the liver and P-glycoprotein (P-gp) in the jejunum. TEC significantly decreased florfenicol's AUC(0-infinity), MRT(0-infinity), t 1/2z, Vz/F, and C max by 24.75%, 18.43%, 55.47%, 43.05%, and 19.48%, while increasing CLz/F by 33.33%. TEC also up-regulated hepatic CYP1A2 and CYP3A1 mRNA expression, as well as intestinal MDR1, by 1.39-fold, 1.85-fold, and 1.65-fold. This coincided with a respective increase in protein expression by 1.37-fold, 1.39-fold, and 1.43-fold. These findings suggest that TEC-induced alterations in the pharmacokinetics of florfenicol may be attributed to increased CYP and P-gp expression. Further investigations are warranted to understand the implications of these findings on the clinical effectiveness of florfenicol in veterinary practice.

【Objective】 The aim of this study was to understand the effect of Xiaochengqi powder on the intestinal microbiota of sows with constipation and investigate the mechanism of Xiaochengqi powder to alleviate constipation.【Method】 A total of 27 bi-crossbreeding sows（Yorkshire×Landrace, 3-5 fetal periods） were selected and divided into healthy control group, constipation group and experimental group according to fecal conditions, each group had 3 replicates and each replicate had 3 pigs.The pigs in healthy control group and pigs in constipation group were given normal diets, and experimental group were added Xiaochengqi powder to the diet（60 g/（head·d）） once daily for three consecutive days.The fresh fecal samples of each group were collected on the fourth day, and the total DNA of the microbial genome was extracted.The microbial community diversity of the samples was detected using Illumina MiSeq sequencing technology.【Result】 The microbial flora in the feces of constipation group was significantly changed, and the Simpson index was significantly different from healthy control group and experimental group（P＜0.05）.At the phylum level, there was a significant decrease in Firmicutes and Bacteroidetes（P＜0.05） and extremely significant increase in Proteobacteria（P＜0.01） in the gut microbiome of the sows in constipation group compared to healthy control group.Compared with constipation group, Bacteroidetes were significantly increased（P＜0.05）,and Firmicutes had on increating tendency（P＞0.05）, and Proteobacteria were extremely significantly reduced（P＜0.01） in experimental group.At the genus level, Lactobacillus and Prevotella were extremely significantly decreased（P＜0.01）,Clostridium＿ⅪVa, Ruminococcaceae and Lachnospiraceae were significantly decreased（P＜0.05）,while Acinetobacter and Escherichia＿Shigella were extremely significantly increased（P＜0.01）,Clostridium＿sensu＿stricto and Romboutsia were both significantly increased（P＜0.05） in the intestinal microbiome of sows in constipation group compared to healthy control group.In experimental group, there was an extremely significant increase in Prevotella（P＜0.01）,a significant increase in Lachnospiraceae（P＜0.05）,and an extremely significant decrease in Acinetobacter compared to constipation group（P＜0.01）.Acetic acid, butyric acid, and propionic acid concentrations in the stools of sows in experimental group were all be considerably increased compared to constipation group（P＜0.05）.【Conclusion】 Xiaochengqi powder might enhance the intestinal microbiome structure of sows with constipation, increase the amount of short-chain fatty acids（SCFAs） in the intestine, and accomplish a new balance of intestinal microorganisms.

母猪便秘是养殖场普遍存在的现象,可由神经-内分泌失调、缺乏运动、霉菌毒素蓄积、病原菌感染、高能量低纤维饲料、长期使用吸附性脱霉剂等引起,严重损害母猪健康.通过查阅文献并结合临床实践,整理提出综合防治措施.

AbstractBackgroundBerberine (BBR) is always used in combination with florfenicol for treating avian in China.ObjectiveThis study aims to investigate the effects of BBR on the pharmacokinetics of florfenicol in broilers.MethodsMale broilers were randomly divided into the control group and the BBR group (BG). Note that 50 mg/kg BBR or sterile water was orally administrated to broilers. On the 8th day, florfenicol [30 mg/kg body weight (BW)] was orally administered to broilers in both groups. The plasma concentrations of florfenicol were determined by ultra‐high‐performance liquid chromatography (UHPLC). The levels of cytochrome P450 (CYP) 3A37, multidrug resistance 1 (MDR1), and chicken xenobiotic‐sensing orphan nuclear receptor (CXR) mRNA expression in the liver and jejunum were determined by the real‐time PCR.ResultsThe results showed that the Cmax, t1/2z, MRT(0‐∞), and AUC(0‐∞) of florfenicol in BG were significantly increased (by 55.71%, 28.32%, 35.19%, and 55.62%, respectively), while the Tmax and CLz/F of florfenicol were significantly decreased (by 52.13% and 35.82%, respectively). In BG, the levels of CYP3A37, MDR1, and CXR mRNA expression in the liver were significantly decreased to 0.72‐fold, 0.67‐fold, and 0.59‐fold, respectively, and the corresponding mRNA expression in the jejunum were significantly decreased to 0.66‐fold, 0.55‐fold, and 0.64‐fold levels, respectively, relative to their levels in the control group.ConclusionsBBR altered the pharmacokinetics of florfenicol, probably related to its inhibition of CYP3A37, MDR1, and CXR mRNA expression in the jejunum and liver.

为研究川续断提取物对氟苯尼考在鸡体内药物动力学影响,将30只肉鸡(2.0 kg±0.1 kg)随机分成2组,每组15只.试验组连续7 d分别灌服川续断提取物(0.3 g/kg,1次/d),对照组给予相同体积的生理盐水,第8天2个组各10只鸡灌服氟苯尼考(30 mg/kg)后按时间点连续采血,采用高效液相色谱法检测氟苯尼考血药浓度,数据采用DAS2.0进行分析.各组剩下的5只鸡,处死鸡剖检取肝脏和空肠,荧光定量PCR检测组织中CYP3A37、MDR1和CXRmRNA表达.试验组和对照组的氟苯尼考主要药物动力学参数为:Cmax分别为20.829 mg/L±5.267 mg/L、18.429 mg/L±8.365 mg/L,Tmax分别为0.688 h±0.139h、1.250 h±0.141 h,AUC0-∞分别为57.907 mg/L·h±8.12 mg/L·h、47.729 mg/L·h±11.601 mg/L·h,T1/2分别为3.649 h±0.193 h、2.520 h±0.255 h,MRT 分别为3.885 h±0.487 h、3.151 h±1.604 h,Vd 分别为1.338 L/kg±0.492 L/kg、2.139 L/kg±1.182 L/kg,CL 分别为0.426 L/h·kg±0.071 L/h·kg、0.657L/h·kg±0.148 L/h·kg.川续断提取物的连续使用,引起了氟苯尼考药物动力学特征明显改变,AUC0-∞和T1/2增加(P＜0.05),Tmax和CL降低(P＜0.05).荧光定量PCR检测结果显示,川续断提取物给药组抑制了 CXR和CYP3A37在肉鸡肝脏和空肠中mRNA的表达量(P＜0.05).结果表明,川续断提取物连续给药7 d后,增加了氟苯尼考在鸡体内的吸收速度,延缓了代谢,提示两者在临床上合用有潜在的增效作用.

研究川续断皂苷乙对氟苯尼考在大鼠体内药动学影响.将24只大鼠(200±10)g随机分成两组,每组12只.试验组连续7 d灌胃川续断皂苷乙(60 mg/kg,1次/d),对照组给予相同体积的生理盐水,第8天两组各6只大鼠灌服氟苯尼考(30 mg/kg)后按时间点连续采血,采用高效液相色谱法检测氟苯尼考血药浓度,数据采用DAS2.0进行分析.处死各组剩下的6只,解剖取肝脏和空肠,荧光定量PCR法和免疫印迹法分别检测组织中CYP1 A2、CYP2 C11、CYP3 A1、MDR1的mRNA表达水平和蛋白表达水平.结果表明,试验组AUC0-∞、MRT0-∞、T1/2和Cmax与对照组相比显著增加(P<0.05),CL与对照组相比显著降低(P<0.05);试验组CYP1 A2、CYP2 C11在肝脏的mRNA表达水平和MDR1在空肠的mRNA表达水平与对照组相比显著降低(P<0.05);试验组大鼠肝脏中CYP1 A2和CYP2 C11酶表达量以及空肠中P-糖蛋白表达量与对照组相比显著降低(P<0.05).川续断皂苷乙连续给药7 d,增加了氟苯尼考在大鼠体内的吸收程度,同时延缓了代谢,可能与川续断皂苷抑制了CYP1 A2酶和CYP2 C11酶在肝脏的表达和P-糖蛋白在空肠的表达有关.

为研究山银花提取物对鸡口服氟苯尼考药代动力学的影响及其作用机制,将30只健康肉公鸡随机平均分成对照组与山银花组,其中山银花组连续7d灌服山银花提取物(0.20 g/kg,1次/d),对照组则给予相同体积的生理盐水,第8天时选取各组10只鸡按30 mg/kg灌服氟苯尼考,给药后按时间点连续采样,高效液相色谱法(HPLC)检测氟苯尼考血药浓度;2组另5只则按荧光定量RT-PCR方法检测肝脏和空肠中细胞色素P4503A37 (CYP3A37)、葡萄糖醛酸转移酶1E (UGT1E)、多药耐药基因1(MDR1)和鸡外源性核受体(CXR) mRNA表达.结果 显示:山银花组药-时曲线下面积(AUC0～24 h)和平均滞留时间(MRT0-24 h)显著增加(P＜0.05),表观清除率(CLz)显著降低(P＜0.05);与对照组相比,山银花组肝脏和空肠中CYP3A37、UGT1E、CXR mRNA表达显著降低(P＜0.05),肝脏、空肠MDR1 mRNA表达无显著差异(P＞0.05).结果 表明:联用山银花后,氟苯尼考在鸡体内药代动力学参数(AUC、MRT和CLz)发生显著变化,可能与山银花抑制CYP3A37、UGT1E、CXR mRNA在肝脏和空肠的表达有关.

The traditional Chinese medicine Platycodon grandiflorum (PG) is often used for the treatment of a number of chronic inflammatory diseases. In Chinese veterinary clinic, PG is always extracted by decoction and taken orally, however, the molecular mechanism of PG extract (PE) to reduce LPS-induced inflammation, especially acute lung injury (ALI) in vivo, are not known. Thus, we have studied the anti-inflammatory effects of PE on lipopolysaccharide (LPS)-induced acute lung injury via TLR4/NF-κBp65 pathway in rat. Sprague-Dawley rats were randomly divided into 4 groups: control group, LPS group, LPS±PE low dose group and LPS±PE high dose group. All rats were given corresponding PE solution or the same amount of normal saline by intragastric administration for 7 days. On the 7th day, 1 h after the last administration, 500 μg of LPS were introduced intratracheally to establish ALI rat model, and the same volume of normal saline was given to control group. The results showed that PE reduced the levels of LPS-induced pro-inflammatory mediators including IL-6, PGE2, and TNF-α, alleviated the lung injury histologically, and down-regulated LPS-induced mRNA and protein levels of TLR4/NF-κBp65 in lung tissue. This study demonstrated that PE has the anti-inflammatory effects on LPS-induced ALI in rats through TLR4/NF-κBp65 signaling pathway, indicating that PE is an effective suppressor for anti-inflammatory activities.

研究参金止痢口服液对腹泻哺乳仔猪肠道微生物菌群的影响.选取同等饲养条件下7～15日龄体重相近的"杜×长×大"三元杂交仔猪共计9头,其中有腹泻症状的6头将其随机平均分为腹泻空白组(FXK)和腹泻中药组(FZ),正常的3头为健康空白组(JK),中药组灌服参金止痢口服液,空白组灌服同等体积生理盐水,连续灌胃5 d,在给药后的第8天对仔猪采血进行抗体及细胞因子水平测定,并采集结肠内容物提取样本中菌群总DNA进行16S rRNA高通量测序.结果显示:与FXK组相比,FZ组血清中IgG含量显著升高(P<0.05),IgM含量显著降低(P<0.05),炎性因子IL-1β、IL-6、TNF-α含量显著下调(P<0.01).α、β多样性分析结果表明,三个组结肠肠道菌群结构差异显著.在门分类水平上,FZ组仔猪肠道拟杆菌门相对丰度显著高于FXK组(P<0.05),变形菌门相对丰度显著低于FXK组(P<0.05),而FZ与JK组之间两个菌门差异不显著.属水平上,FZ组韦荣球菌属和乳杆菌属相对丰度显著低于FXK组(P<0.05),普雷沃氏菌属相对丰度显著高于FXK组(P<0.05),FZ组与JK组之间这三个菌属差异不显著.综上结果表明,参金止痢口服液可能通过调节免疫及炎性相关因子水平和肠道菌群结构从而发挥治疗哺乳仔猪腹泻的作用.

Borneol is a traditional Chinese medicine. In Chinese veterinary clinics, borneol and its related compounds are often used in combination with florfenicol to treat respiratory infections. This study investigated whether the pharmacokinetics of florfenicol in rats was affected by its concomitant use with borneol. Sprague-Dawley rats were intragastrically administered borneol (50 mg/kg body weight (BW)) or 0.5% carboxymethyl-cellulose sodium for 7 consecutive days, and then intragastrically administered florfenicol (25 mg/kg BW) on the eighth day. Pharmacokinetic studies showed that borneol significantly decreased the area under the concentration-time curve from zero to infinity (AUC(0-t)), time to reach peak concentration (Tmax), and the peak concentration (Cmax) values of florfenicol, whereas the values of mean residence time from zero to infinity (MRT(0-t)), elimination half-life (t1/2z), apparent volume of distribution fraction of the dose absorbed (Vz), and plasma clearance fraction of the dose absorbed (CLz) were increased significantly. Furthermore, the mRNA expression levels of multidrug resistance 1 (MDR1) and cytochrome P450 3A1 (CYP3A1) in the jejunum and of CYP1A2 and CYP2C11 in the liver were significantly upregulated by borneol. In conclusion, borneol decreased absorption, increased clearance, improved distribution, and increased the mean residence time of florfenicol in rats, possibly through regulating the mRNA expression levels of drug-metabolizing enzymes and efflux transporters.

Background: The traditional Chinese medicine Scutellariae radix is often used in combination with antibiotics, such as florfenicol, in Chinese veterinary medicine. Baicalin (5, 6, 7-trihydroxyflavone-7-β-D-glucuronide) is the main active constituent of S. radix. The effects of baicalin on the pharmacokinetics of florfenicol are not known. Thus, we have studied the effects of baicalin on florfenicol pharmacokinetics and the mRNA expression of drug-metabolizing enzymes/efflux transporters in rats. Materials and Methods: Sprague-Dawley rats were given baicalin (50 mg/kg BW or 100 mg/kg BW) or 0.9% sodium chloride solution by intragastric administration for 7 days. They were then fed florfenicol by intragastric administration (25 mg/kg BW) on the 8th day. Blood samples were collected at various times, and the plasma concentrations of florfenicol were estimated with ultra-high performance liquid chromatography. The mRNA expression levels of cytochrome P450 (CYP) CYP1A2, CYP2C11, CYP3A1, UDP-glucuronosyltransferase 1A (UGT1A), multidrug resistance 1, and ATP-binding cassette C2 (ABCC2) in the liver and jejunum were analyzed with a real-time polymerase chain reaction. Results: The area under the concentration-time curve from zero to infinity, mean residence time from zero to infinity, elimination half-life, and peak concentration of florfenicol were significantly increased and the apparent volume of distribution fraction of the dose absorbed and plasma clearance fraction of the dose absorbed were significantly decreased by baicalin; the mRNA expression levels of CYP1A2, CYP2C11, CYP3A1, UGT1A1, and ABCC2 were down-regulated by baicalin. Conclusion: Baicalin affected the pharmacokinetics of florfenicol in rats, increased the plasma concentration and residence time of florfenicol, probably by decreasing the mRNA expression levels of CYP1A2, CYP2C11, CYP3A1, UGT1A1, and ABCC2 in the liver and jejunum.

为研究双黄连口服液对鸡口服氟苯尼考药代动力学的影响.将20只鸡随机分成对照组与双黄连口服液联用组,各10只.联用组连续7 d灌服双黄连口服液(2 mL/kg,1次/d),对照组则给予相同体积的生理盐水,第8天两组各10只鸡按30 mg/kg灌服氟苯尼考,给药后按时间点连续采样,高效液相色谱法(HPLC)检测氟苯尼考血药浓度,DAS2.0分析药代学参数.结果显示:联用双黄连口服液后,氟苯尼考药时曲线下面积(AUC0-24h)和平均滞留时间(MRT0-24h)显著增加(P<0.01),清除速率(CLz)极显著降低(P<0.01).双黄连口服液与氟苯尼考联用可降低氟苯尼考在鸡体内消除速度,提高口服生物利用度,对氟苯尼考有增效作用.

甘草是传统常用中药,药理作用多样,临床用途广泛,对细胞色素P450酶和P-糖蛋白活性具有双重调节作用,合用时可对一些化学药物如咪达唑仑、环孢素、安替比林、氯沙坦、洛伐他汀、格列美脲、阿米替林、左氧氧氟沙星、氟苯尼考等的体内代谢产生影响,发生药物代谢动力学特征的改变,引起疗效改变和不良反应.了解甘草在体内外作用机制以及可能引起的潜在中西药药动学相互作用,对于保障临床用药安全具有重要意义.论文总结近年来甘草与其他化学药物药动学相互作用研究,促进对甘草的全面认识,推动中西药结合理论的发展.

Pulsatillae radix, a traditional Chinese medicine (TCM), is often used in combination with florfenicol for treatment of intestinal infection in Chinese veterinary clinics. Anemoside B4 (AB4) is the major effective saponin in Pulsatillae radix. This study aimed to investigate whether the pharmacokinetics of florfenicol in broilers was affected by the combination of AB4. In this study, broilers were given AB4 (50 mg/kg BW), or 0.9% sodium chloride solution by oral administration for 7 days. They were then fed florfenicol orally (30 mg/kg BW) on the eighth day. The results showed that the AUC(0-∞), MRT(0-∞), t1/2z and Cmax of florfenicol were significantly decreased, and the Vz/F and CLz/F were significantly increased by AB4; the mRNA expression levels of CXR, CYP3A37 and MDR1 (except CXR and CYP3A37 in the liver) were up-regulated by AB4. In conclusion, AB4 altered the pharmacokinetics of florfenicol, resulting in lower plasma concentrations of florfenicol, this was probably related to the mRNA expression of CXR, CYP3A37 and MDR1 in the jejunum and liver (except CXR and CYP3A37) increased by AB4. The implications of these findings on the effect of traditional Chinese medicine containing AB4 on the effectiveness of florfenicol in veterinary practice deserve study.

为研究黄芩素对氟苯尼考在大鼠体内药动学的影响,将12只大鼠随机分成单用组、合用组,合用组连续7d灌服黄芩素(50 mg/kg,1次/d),单用组则给予相同体积的生理盐水,第8d两组大鼠均按25 mg/kg剂量灌服氟苯尼考,给药后按时间点连续采样,数据采用DAS2.0分析.试验结果表明,黄芩素连续给药7d,可以增加氟苯尼考在大鼠体内的吸收,减缓代谢消除,提高口服生物利用度,提示这两种药物在临床上合用具有潜在的药动学相互作用.