蓝萼香茶菜增加小鼠心肌血流灌注量的药效动力学

目的探讨蓝萼香茶菜药效动力学。方法以小鼠心肌血流灌注量为指标进行测定。结果蓝萼香茶菜在小鼠体内并非呈简单的房室模型,其最低起效剂量为生药0.7899 g.kg-1,效应达峰时间约为1 h,效应作用期长达6 h以上。结论蓝萼香茶菜体内具有吸收快,消除慢和作用维持时间长等特点。     

14C-尿素在小鼠中的药代动力学研究

目的　研究1 4C 尿素在小鼠体内的药代动力学变化。方法　用液体闪烁计数法测定小鼠口服1 4C 尿素后的1 4C血药浓度、各种组织和代谢物中1 4C的放射性。结果　小鼠按体重口服 2 96MBq kg1 4C 尿素后 ,血药浓度 时间曲线符合二房室开放模型 ,吸收相半衰期为 0 72h ,消除相半衰期为 5 15h ,峰值时间为 0 11h ,峰浓度为 1 5 7kBq ml,清除率为 0 6 17L·kg- 1 ·h- 1 。小鼠口服1 4C 尿素后在 0 2 5h肾、肝、肺、脾等组织放射性最高 ,心、胃、肠、肌肉次之 ,脑、脂肪最少 ,2h肺中最高。 2 4h组织中放射性随时间减少而肝中相对较高。 2 4h粪尿排出量占口服量的 6 4 75 % ,其中由尿排出4 5 4 5 % ,由粪排出 19 30 %。结论　小鼠口服1 4C 尿素吸收迅速 ,清除较快 ,排泄以尿为主 ,组织中未见特异性浓聚。     

盐酸川芎嗪透皮贴剂药代动力学研究

目的建立SD大鼠盐酸川芎嗪（TMPH）贴剂和灌胃给药后体内血药浓度的测定方法,计算贴剂组和灌胃组的药代动力学参数并进行比较。方法贴剂组：自制贴剂,SD大鼠背部给药（1.04 g/kg）,分别于给药后0.5、1.5、3、4、5、6、7、8、9、12、17、24 h从尾部静脉取血;灌胃组：SD大鼠灌胃给药（1.6 mg/kg）,分别在给药后5、8、10、13、15、21、34、45、61 min从尾部静脉取血;用HPLC测定两组大鼠体内TMPH的血药浓度,用DAS软件计算。结果灌胃组药代动力学参数：Tmax=0.167 h,Cmax=1.97 mg/L,T1/2=0.076 h,Auc0-t=0.597[（μg·h）/ml],Auc0-∞=0.650[（μg·h）/ml];贴剂组药代动力学参数：Tmax=5.917 h,Cmax=253 mg/L,T1/2=5.95 h,Auc0-t=3547.56[（μg.h）/ml],Auc0-∞=4132.47[（μg.h）/ml]。结论 TMPH灌胃给药时,达峰时间和半衰期都很短,说明TMPH普通制剂在体内吸收代谢非常迅速,难以长时间维持有效血药浓度;TMPH贴剂给药的达峰时间和半衰期大大延长,能够在较长时间内维持较高的血药浓度。     

麝香保心分散片的制备和人参总皂苷的体外溶出度研究

目的　制备麝香保心分散片 ,考察人参总皂苷的体外溶出度。方法　以PVPP为崩解剂、MCC为填充剂、CMC Ca为溶胀性辅料、1%HPMC水溶液为粘合剂 ,制备麝香保心分散片 ;采用比色法以人参总皂苷为测定指标 ,考察其体外溶出度。结果与结论　按最佳工艺制备的麝香保心分散片在 (2 0± 1)℃水中于 15s内可完全崩解且分散均匀 ,其指标性成分人参总皂苷的溶出速率明显高于麝香保心丸     

龙血素B在模拟失重大鼠体内的血浆药物动力学研究

目的研究模拟失重大鼠灌胃龙血竭后有效成分龙血素B的血浆药物动力学。方法采用3周尾吊大鼠模型模拟失重状态,单次灌胃给予10.6 g/kg龙血竭后,收集各个时间点血浆样本,HPLC-MS/MS法测定尾吊大鼠血浆中龙血素B的含量,并求算药物动力学参数。结果龙血素B在模拟失重大鼠体内血药浓度-时间曲线下面积(AUC0-T)为(23.4±12.4)μg/L·h,达峰时间(Tmax)为(0.33±0.11)h,达峰浓度Cmax(2.77±0.71)μg/L,表观分布容积(Vc)为(677.6±111.6)L/kg。生物半衰期(T0.5)为(8.47±1.7)h。结论本文首次报道了龙血素B在模拟失重大鼠体内的药物动力学参数,为龙血竭对抗空间疾病的相关研究提供了药动学数据。     

偏二甲基肼在小鼠体内的毒物动力学及分布特征

目的研究小鼠静脉注射（iv）和灌胃（ig）偏二甲基肼（UDMH）的毒物动力学，及iv UDMH的组织分布。方法iv组，剂量39．0mg／kg；ig组，剂量39．0mg／kg和78．0mg／kg；iv组织分布组，剂量78．0mg／kg。染毒后不同时间断头取血及剖取相关脏器组织，并测定样品中UDMH浓度。结果小鼠iv UDMH呈二室开放模型，分布相半衰期（t1／2α）仅为2．98min，清除相半衰期（t1／2β）为30．0～39．6min。小鼠ig UDMH为一级吸收一室模型，吸收相半衰期（t1／2ka）仅3．6～4．5min，吸收达峰时间（tp）不足15min，吸收分数（F）为100％。小鼠iv UDMH，脏器中UDMH浓度，除脑外均呈单项指数函数下降，在脑中还有一个上升相。各脏器组织的靶向系数（te）均大于1，消化道的重量加权靶向系数（te^＊）高达7．1。结论UDMH经小鼠消化道吸收快且完全，分布很快且广泛；血脑屏障对UDMH进入脑有一定的阻碍作用；消除快，物质蓄积性弱。     

胰岛素经眼给药的药物代谢动力学

用国产胰岛素在54只新西兰大耳白家兔体内观察其经眼给药后药物代谢动力学特征。结果表明：分子量约为6000的胰岛素滴眼后能有效地进入血液循环，体内药物动力学为开放性一级动力学一房室模型。消除半衰期为40-60min，与静脉注射相比，消除半衰期明显延长，达峰时间为20-50min。金属络合剂EDTA对胰岛素的经眼吸收有促进作用，经眼给药后体内药物的浓度呈现出剂量依赖性。     

麝香保心片对心肌缺血缺氧的保护作用

目的：观察麝香保心片对实验性心肌缺血的药理效应。方法：用垂体后叶素造成大鼠急性心肌缺血模型，观察麝香保心片对心电图T波的影响；用腹腔注射异丙肾上腺素造成小鼠急性心肌缺血模型，观察麝香保心片对小鼠心肌组织丙二醛含量及心肌酶谱的影响。结果：麝香保心片组与模型组相比，可以显改善心电图缺血性改变（P＜0．05）；减少心肌组织丙二醛的生成（P＜0．01），抑制心肌AST、LDH、CPK、CK－MB的升高。结论：麝香保心片可以有效改善冠脉循环，保护缺血心肌。     

厚朴酚与和厚朴酚在大鼠体内的药代动力学

目的　观察厚朴酚与和厚朴酚在Wistar大鼠体内的动力学过程。方法　用实验建立的RP -HPLC法测定大鼠灌胃给予上述两种成分后不同时间各组织和体液中药物的含量及其蛋白结合率 ,并计算其在血中的药代动力学。结果　建立的方法能够良好分离两种成分 ,浓度 -色谱响应间线性相关系数均 >0 .999,平均加样回收率 >90 % ;两种成分在大鼠体内代谢符合一级消除动力学二室开放模型 ,Cmax　分别为 0 .974和 0 .5 2 2mg·L-1,T1/ 2 β　为 3.136和 3.2 84h ,T1/ 2ka　　为 0 .16 0和 0 .2 6 1h ;进入体内后 ,主要滞留于胃肠内 ,其他主要分布于肝、肺、肾组织中 ;血浆蛋白结合率分别为 6 8.5 4 %和 5 3.81% ;以粪排出为主 ,尿和胆汁排出量只有约 5 %。结论　厚朴酚与和厚朴酚吸收较差 ,进入循环后以肝代谢和肾排泄为主。     

放射性核素示踪技术用于地尔硫(卓)缓释粘附材料的研究

目的　筛选口服缓释地尔硫的生物粘附材料。方法　通过测定可用于制药的粘附聚合物羟丙基甲基纤维素 (HPMC)类、卡波姆 (Cb)类、聚维酮 (PVP)K30和羧甲基纤维素钠 (CMCNa)与大鼠胃和肠黏膜的最大粘附力及其在大鼠胃和肠道的排空速度 ,筛选出最佳粘附材料 ,再用放射性核素体内示踪技术验证其在犬胃、肠的粘附能力。结果　Cb与大鼠肠黏膜的粘附力为 19.6～ 31.0g,显著大于其他材料 (4.0～ 2 4 .3g)。Cb934在大鼠胃内的排空半衰期为 7.4h,大于其他材料。含5 0 %Cb934的粘附颗粒能将其在犬胃内的排空半衰期延长 1倍 ;8h时犬小肠含Cb9345 0 %和 10 0 %的粘附颗粒滞留量分别为 2 9.6 %和 5 5 .1% ,而不含Cb934的粘附颗粒 6h时即为 0。结论　Cb934可作为口服缓释剂生物粘附材料。     

Knee injury and Osteoarthritis Outcome Score (KOOS) - validation of a Swedish version

The Knee injury and Osteoarthritis Outcome Score (KOOS) is a self-administered instrument measuring outcome after knee injury at impairment, disability, and handicap level in five subscales. Reliability, validity, and responsiveness of a Swedish version was assessed in 142 patients who underwent arthroscopy because of injury to the menisci, anterior cruciate ligament, or cartilage of the knee. The clinimetric properties were found to be good and comparable to the American version of the KOOS. Comparison to the Short Form-36 and the Lysholm knee scoring scale revealed expected correlations and construct validity. Item by item, symptoms and functional limitations were compared between diagnostic groups. High responsiveness was found three months after arthroscopic partial meniscectomy for all subscales but Activities of Daily Living.     

The acutely limping child

Acute limping may be the result of multiple pathologies in children. The differential diagnosis varies based on the age of the child. Irrespective of age, the initial imaging work-up includes AP and frog leg radiographs of the pelvis and ultrasound; MRI may sometimes be helpful. In children less than 3 years, infections and trauma are most frequent. MRI is the imaging modality of choice when osteomyelitis is clinically suspected. Between the ages of 3 and 10 years, transient synovitis of the hip and Legg-Calvé-Perthes disease are main considerations but infection, inflammation and focal bony lesions are also considered. In children over 10 years, slipped capital femoral epiphysis also is considered.     

Do Balance Board Training Programs Reduce the Risk of Ankle Sprains in Athletes?

Introduction Ankle sprains are the most common musculo-skeletal injury that occurs in athletes,particularly in sports that require jumping and landing on one foot such as soccer,and basketball(1-4).These injuries often result in significant time loss from participation,long-term disability,and have a major impact on health care costs and resources(5-8).     

High Intensity Interval Training:New Insights

KEY POINTS ·High-intensity interval training(HIT)is characterized by repeated sessions of relatively brief，intermittent exercise.often performed with an“a11 out”effort or at an intensity close to that which elicits peak oxygen uptake(i.e.，≥90%of VO2 peak).     

Endovascular management of carotid-cavernous fistulas

Objective To investigate endovascular treatment of traumatic direct carotid-cavernous fistulas （CCF） and their complications such as pseudoaneurysms. Methods： Over a five-year period, 22 patients with traumatic direct CCFs were treated endovascularly in our institution. Thirteen patients were treated once with the result of CCF occluded, 8 twice and 1 three times. Treatment modalities included balloon occlusion of the CCF, sacrifice of the ipsilateral internal carotid artery with detachable balloon, coll embolization of the cavernous sinus and secondary pseudoaneurysms, and covered-stem management of the pseudoaneurysms. Results All the direct CCFs were successfully managed endovascularly. Four patients developed a pseudoaneurysm after the occlusion of the CCF with an incidence of pseudoaneurysm formation of 18.2% （4/22）. A total number of 8 patients experienced permanent occlusion of the ICA with a rate of ICA occlusion reaching 36.4% （8/22）. Followed up through telephone consultation from 6 months to 5 years, all did well with no recurrence of CCF symptoms and signs. Conclusion Traumatic direct CCFs can be successfully managed with endovascular means. The pseudoaneurysms secondary to the occlusion of the CCFs can be occluded with stent-assisted coiling and implantation of covered stents.     

Developmental validation of the PowerPlex(®) ESI 16 and PowerPlex(®) ESI 17 Systems: STR multiplexes for the new European standard

In response to the ENFSI and EDNAP groups’ call for new STR multiplexes for Europe, Promega^® developed a suite of four new DNA profiling kits. This paper describes the developmental validation study performed on the PowerPlex^® ESI 16 (European Standard Investigator 16) and the PowerPlex^® ESI 17 Systems. The PowerPlex^® ESI 16 System combines the 11 loci compatible with the UK National DNA Database^®, contained within the AmpFlSTR^® SGM Plus^® PCR Amplification Kit, with five additional loci: D2S441, D10S1248, D22S1045, D1S1656 and D12S391. The multiplex was designed to reduce the amplicon size of the loci found in the AmpFlSTR^® SGM Plus^® kit. This design facilitates increased robustness and amplification success for the loci used in the national DNA databases created in many countries, when analyzing degraded DNA samples. The PowerPlex^® ESI 17 System amplifies the same loci as the PowerPlex^® ESI 16 System, but with the addition of a primer pair for the SE33 locus. Tests were designed to address the developmental validation guidelines issued by the Scientific Working Group on DNA Analysis Methods (SWGDAM), and those of the DNA Advisory Board (DAB). Samples processed include DNA mixtures, PCR reactions spiked with inhibitors, a sensitivity series, and 306 United Kingdom donor samples to determine concordance with data generated with the AmpFlSTR^® SGM Plus^® kit. Allele frequencies from 242 white Caucasian samples collected in the United Kingdom are also presented. The PowerPlex^® ESI 16 and ESI 17 Systems are robust and sensitive tools, suitable for the analysis of forensic DNA samples. Full profiles were routinely observed with 62.5 pg of a fully heterozygous single source DNA template. This high level of sensitivity was found to impact on mixture analyses, where 54–86% of unique minor contributor alleles were routinely observed in a 1:19 mixture ratio. Improved sensitivity combined with the robustness afforded by smaller amplicons has substantially improved the quantity of data obtained from degraded samples, and the improved chemistry confers exceptional tolerance to high levels of laboratory prepared inhibitors.     

Bronchial stump fistula :treatment with covered retrievable hinged metallic stents-preliminary clinical experience

Objective To evaluate the preliminaily clinical efficacy and retrievability of a retrievable hinged covered metallic stent in the treatment of the bronchial stump fistula （BSF）. Methods Between April 2003 and March 2005, 8 patients with bronchial stump fistula after pneumonectomy or lobectomy were treated with two types （A and B） of retrievable hinged covered metallic stents. Type A stent was placed in 6 patients and type B in 2 under fluoroscopic guidance. The stent was removed with a retrieval set when BSF was healed or complications occurred. Results Stent placement in the bronchial tree was technically successful in all patients, without procedure-related complications. Immediate closure of the BSF was achieved in all patients after the procedure. Stents were removed from all patients but one. Removal of the stents was difficult in two patients due to tissue hyperplasia. Patients were followed up for 6 - 21 months. Placement of the stents remained stable in all patients except one due to severe cough. Permanent closure of BSF was achieved in 7 （87.5%） of 8 patients. Conclusion Use of a retrievable hinged covered expandable metallic stent is a simple, safe, and effective procedure for closure of the BSF. Retrieval of the stent seems to be feasible. （J Intervent Radiol, 2007, 16： 253-257）     

Prevalence and severity of hip and groin pain in sub‐elite male football: a cross‐sectional cohort study of 695 players

The purpose of this study was twofold: (a) to investigate the prevalence of hip and groin pain in sub‐elite male adult football in Denmark and (b) to explore the association between prevalence and duration of hip and groin pain in the previous season with the Copenhagen Hip and Groin Outcome Score (HAGOS) in the beginning of the new season. In total 695 respondents from 40 teams (Division 1–4) were included. Players completed in the beginning of the new season (July–Sept 2011) a self‐reported paper questionnaire on hip and/or groin pain during the previous season and HAGOS. In total 49% (95% CI: 45–52%) reported hip and/or groin pain during the previous season. Of these, 31% (95% CI: 26–36%) reported pain for >6 weeks. Players with the longest duration of pain during the previous season had the lowest HAGOS scores, when assessed at the beginning of the new season, P < 0.001. This study documents that half of sub‐elite male adult football players report pain in the hip and/or groin during a football season. The football players with the longest duration of pain in previous season displayed the lowest HAGOS scores in the beginning of the new season.