胆道手术病人中头孢曲松钠的药动学

目的研究头孢曲松钠(CTRX)在6例施各类胆道手术附胆总管引流患者的药动学.方法采用微生物学的方法测定血清及胆汁中头孢曲松钠浓度.结果静滴头孢曲松钠3g或2g即刻血药浓度分别可达到(470.9±23.4)μg·ml-1和(288.1±14.3)μg·ml-1,8h后仍保持(91.7±5.1)μg·ml-1和(54.6±4.2)μg·ml-1;T型管胆汁药物峰浓度可达到(1645.81±201.3)μg·ml-1和(1123.8±140.4)μg·     

硝基咪唑类药物在授乳妇女中的乳药分析

目的:研究甲硝唑、替硝唑在授乳妇女乳汁中的分泌。方法:高效液相色谱法。Ultraspbere-ODS柱,甲硝唑乳药分析用流动相为乙腈-0.1％冰醋酸(50:50),替硝唑乳药分析用流动相为乙腈-水(60:40),流速1.0mL·min~(-1) ,检测波长318nm。结果:甲硝唑乳汁药物浓度在2h时为(10.11±5.390)μg·mL~(-1),8h时尚可测得(4.478±2.669)μg·mL~(-1)。替硝唑乳汁药物浓度在2h时为(14.17±5.746)μg·mL~(-1),8h时尚可测得(9.364±5.123)μg·mL~(-1)。结论:本文建立的高效液相色谱法简单、灵敏,适用于乳药浓度的测定,建议授乳妇女避开给药时间哺乳。     

国产和进口缬沙坦胶囊的人体生物利用度

目的研究国产和进口缬沙坦胶囊的相对生物利用度.方法22名健康受试者随机、自身交叉服用单剂量的缬沙坦160 mg,用HPLC法测定血浆中的药物浓度,梯形法计算药时曲线下面积,并对主要参数进行统计学分析.结果国产制剂与进口制剂的主要药动学参数 Cmax为(2.1±0.6),(2.1±0.8) μg·ml-1;Tmax为(2.3±0.5),(2.4±0.6) h;AUC0～24为(10.5±3.2),(10.8±3.5) μg·ml-1·h-1;AUC0～∞为(11.7±3.4),(12.0±3.5) μg·ml-1·     

盐酸黄连素对肾移植受者环孢素A增效作用的临床药代动力学研究

目的研究盐酸黄连素对肾移植受者使用环孢素A增效作用的体内动力学过程.方法选择肾移植术后1个月以内、连续服用环孢素A 2周、肝肾功能稳定的患者6名,环孢素A剂量6mg.kg-1·d-1,用FPIA方法(单抗)检测合用黄连素前后各时间点环孢素A全血浓度.结果单服环孢素A的主要药代动力学参数分别为tmax(h)1.33±0.52,Cmax(μg·L-1)1224.75±296 20,Cmin(μg·L-1)173.95±78.71,t1/2(h)2.62±1.00,AUC μg·h·L-14681.34±1300.45,CL/F(L·h-1)35±15;与黄连素合用的主要药代动力学参数为tmax(h)3.00±1.26,Cmax(μg·L-1)1050.10±290.86,Cmin(μg·L-1)321.31±161.29,t1/2(h)5.33±2.60,AUCμg·h·L-16265.71±1 871.33,CL/F(L·     

环丙沙星对苯妥英钠药动学的影响

目的研究环丙沙星对苯妥英血药浓度及药动学参数的影响.方法应用紫外分光光度法测定家兔喂服环丙沙星(25 mg·kg-1)前及1周后单剂量静注苯妥英钠(10 mg·kg-1)的经时血药浓度,以"3P87"药动学程序拟合药动学参数.结果合用环丙沙星后,苯妥英血药浓度明显下降(P<0.05), AUC由合并用药前(6639.0±893.9) mg·L-1·min-1降为(4200.7±874.4) mg·L-1·     

琥珀酸美托洛尔缓释片在中国人体的药动学特性

目的研究琥珀酸美托洛尔缓释片在中国人体的药动学特性.方法采用HPLC荧光检测法测定血浆中美托洛尔的浓度.结果22名健康受试者口服单剂量50mg琥珀酸美托洛尔缓释片后的AUC0-t为(173.15±99.52)μg·h·L-1,AUC0-∞为(237.44±162.11)μg·h·L-1,cmax为(15.67±7.69)μg·L-1,tmax为(6.14±2.55)h,MRT为(14.17±4.01)h;多剂量口服50mg缓释片后的AUCss0-t为(335.42±235.19)μg·h·L-1,cmax为(23.03±15.16)μg·L-1,tmax为(5.8±2.2)h,cmin(6.73±4.98)μg·L-1,平均稳态血药浓度cav是(13.98±9.80)μg·L-1,血药浓度波动度DF(%)(122.55±53.93)%.结论单剂量给予缓释片的结果与美托洛尔普通片相比,tmax明显延长(5.8vs 1.1 h),cmax明显降低(15.67×2vs 186.2μg·L-1).琥珀酸美托洛片缓释片与普通片相比在中国健康受试者中的缓释特征明显,安全性良好.在整个试验过程中监测血压、心率,无低血压、血晕等不良反应发生.     

格列吡嗪片在健康志愿者体内的生物等效性评价

目的比较两种格列吡嗪片剂在健康志愿者体内的药动学及生物等效性.方法12例男性健康志愿受试者,采用标准两周期交叉设计自身对照试验法,单剂量口服进口和国产格列吡嗪片10mg,以高效液相色谱法测定血浆中格列吡嗪的经时浓度,以双单侧t检验统计法比较两种格列吡嗪片之间的差异.结果两种格列吡嗪片在健康志愿者体内的药-时曲线均符合一级吸收的单室模型,国产格列吡嗪片主要的药动学参数Tmax、Cmax和AUC(0-17)分别为(2.6±0.5)h,(609.7±112.9)ng·ml-1和(4499.8±969.0)ng·h-1·ml-1;进口格列吡嗪片主要的药动学参数Tmax、Cmax和AUC(0-17)分别为(2.6±0.5)h,(568.8±101.9)ng·ml-1和(4108.3±724.9)ng·h·     

环丙沙星缓释微粒溶出度与兔眼内的药动学

目的研究环丙沙星(CPFX)缓释微粒是否具有缓释长效作用.方法应用HPLC法测定CPFX微粒体外溶出度和在兔眼内释放的药物浓度.结果CPFX微粒在体外72h内累积释放率为86%,K=0.0524.在兔眼内药动学参数为T1/2(Ka)为9.115h,T1/2(ke)为10.55h,Tmax为18.08h,Cmax为1.28μg·ml-1,AUC为57.46μg·h·     

缓释醋酸亮丙瑞林微球对大鼠子宫异位内膜的抑制作用

目的观察国内研制的醋酸亮丙瑞林(LE)微球对异位子宫内膜的抑制作用,并与进口醋酸亮丙瑞林微球(enanton)及醋酸亮丙瑞林(LE)注射溶液进行疗效比较.方法以手术方法制备大鼠子宫内膜异位症模型,将动物分为辅料组、原料药组(LE,20μg·kg-1·d-1×28d,sc)、进口微球组(enanton20μg·kg-1·d-1,sc)、国产微球组(国产LE微球2、20、200μg·kg-1·d-1,sc).结果辅料组异位内膜体积呈增长趋势,阳性对照药LE20μg·kg-1(sc×28d)、enanton20μg·kg-1·d-1,及国产LE微球2、20、200μg·kg-1·d-1对异位内膜均有明显抑制作用,且后者具有一定的剂量相关性.结论国产醋酸亮丙瑞林微球20μg·kg-1·     

普卢利沙星片的健康人体药动学

目的健康志愿受试者口服普卢利沙星片后,测定血浆中其活性代谢物(UFX)并作药动学研究。方法10名受试者分别单剂量和多剂量稳态时服用普卢利沙星片(相当于200 mg UFX),采集血浆和尿液样品,液相色谱分离荧光检测UFX浓度,3P97软件计算药动学参数。结果单剂量时测得UFX的主要药动学参数分别为cmax(1.64±0.29)μg.ml-1,tmax(0.7±0.2)h,AUC0-36(6.87±1.78)h.μg.ml-1,AUC0-∞(7.14±1.79)h.μg.ml-1,t1/2(7.54±0.59)h,MRT(8.76±0.65)h;0~36 h尿液累积排泄量为(56.85±9.12)%。稳态时测得UFX的主要药动学参数分别为cmax(1.26±0.41)μg.ml-1,tmax(0.8±0.3)h,AUC0-36(7.77±2.73)h.μg.ml-1,AUC0-∞(8.10±2.70)h.μg.ml-1,t1/2(7.71±1.13)h,MRT(9.85±1.40)h。结论健康志愿受试者口服普卢利沙星片后,在体内转化为活性代谢物(UFX)发挥作用,主要经尿液排泄。每日2次,每次2片(相当于200 mg UFX),在体内无积蓄。男女健康受试者的主要药动学参数无显著性差异。     

Degraded and undegraded carrageenans and experimental gastric and duodenal ulceration

The prevention of histamine-induced gastric and duodenal ulceration in the guinea-pig has been examined using a series of undegraded and degraded carrageenans. Undegraded carrageenans were active at lower doses than degraded carrageenans. The high viscosity of the undegraded carrageenans in solution prevented their use in larger doses. Degradation of carrageenan without serious loss of sulphate, gives a product which allows the dose to be increased to an extent that its effect more than offsets the slight loss in activity caused by the degradation. No single feature of carrageenan structure can be related to anti-ulcer activity although degradation, and hence reduction of molecular size, generally reduces activity. Sulphate contents over 30% have little apparent effect on activity; κ-carrageenans were not consistently different in anti-ulcer activity from Λ-carrageenans. This contrasts with the antipeptic activity of carrageenans where κ-carrageenans are less active than their Λ-counter-parts. As with antipeptic activity, the degree of anti-ulcer activity is probably determined by a combination of structural features which includes molecular size and polyanionic properties.     

Affective and Anxiety Disorders and Alcohol and Drug Dependence:

Depression and anxiety frequently coexist in patients with substance use disorders. This clinically-oriented article examiens the relationship between these conditions and emphasizes data showing that substances of abuse can cause signs and symptoms of both depression and anxiety. These substance-related syndromes appear to have a different course and prognosis than uncomplicated, independent anxiety and major depressive disorders, and clinicians should consider the role of alcohol and other drugs in all patients presenting with these complaints. The authors will also outline an approach for diagnosing and managing patients with the combination of a substance use and depressive or anxiety disorder.     

Alcohol and Substance Use and Abuse in Women and Children

No abstract available for this article.     

Glucosidase and fucosidase inhibitors and Advances in nucleosides and nucleotides.

The American Chemical Society Symposium "Glucosidase and fucosidase inhibitors" took place on 1 April 1998 and was organized by Professors Zbigniew J Witczak (UConn, School of Pharmacy, CT, USA), Kuniaki Tatsuta (Waseda University, Tokyo, Japan) and Waldemar Priebe, MD (Anderson Cancer Center, University of Texas, USA). Professor Witczak provided introductory remarks including the status of existing glucosidase inhibitors, and chaired the morning session, which consisted of six lectures. The symposium was well received, and was particularly attractive for those interested in networking, as attendance was about sixty. In addition, some participants and attendees presented posters on the subject during the regular poster session organized by the Division of Carbohydrate Chemistry.