便民颗粒分取药管的设计与研究

目的设计一种适用于袋装颗粒制剂细分服用剂量时使用的取药管,对其取药误差进行对比研究。方法根据颗粒具有流动性和质量M=ρ_b*V(ρ_b为堆密度)的性质,将颗粒制剂分取的度量方式转换到本研究设计的取药管的可视高度上来,即M=ρ_b*V=ρ_b*sh;进行实验对照研究,分手工组和取药管组,分别分取8种颗粒剂1/3包和1/2包剂量,分取后通过称重的方式测算分取误差情况。结果手工组和取药管组1/3包的平均取药误差率分别为8.068±4.586、2.925±2.146(P<0.01),1/2包分别为7.896±5.709、3.745±2.627(P<0.01);1/3包误差的平均超限率分别为35.19%、0.96%(P<0.01),1/2包分别为35.19%、0.48%(P<0.01)。结论本研究设计的取药管能显著降低取药误差。     

罗红霉素颗粒剂的药物动力学与相对生物利用度

目的:对罗红霉素颗粒剂的药物动力学与相对生物利用度进行研究.方法:采用微生物法测定8名志愿者单剂量po 300mg罗红霉素颗粒剂与片剂的血药浓度,计算两者的药物动力学参数与相对生物利用度.结果:两者药-时曲线以一级吸收双室模型拟合较好,两者的c—分别为(6.64土0·80)与(6.44土0·89)μg/ml;t_(max)_分别为(1.60土0.45)与(2.00土0.34)h;T_1/2分别为(14. 78士0.99)与(14.00士1.60)h;AUC_o_oo～分别为(100.03士18.40)与(99.01士19.21)μg·h/ml,统计学处理表明两者无显著性差异(P>0.05).结论:罗红霉素颗粒剂与片剂为生物等效制剂,罗红霉素颗粒剂的相对生物利用度为101·56%.     

黄连解毒组方颗粒剂对小鼠肠黏膜的影响

目的 观察不同剂量的黄连解毒组方颗粒剂对小鼠肠道菌群及细菌移位的影响.方法 根据传统黄连解毒汤的配方,用相对应的单味中药颗粒剂组成黄连解毒组方颗粒剂;用不同剂量的黄连解毒组方颗粒剂对小鼠进行灌胃;与正常小鼠比较,观察黄连解毒组方颗粒剂对小鼠肠道组织的影响.结果 低剂量组和正常组均未出现细菌移位现象,回肠黏膜完整,球杆菌比例正常;高、中剂量组细菌移位现象明显,回肠黏膜损伤脱落,盲肠水肿,盲肠内容物涂片镜检可见球杆菌比大于1/3,与正常组相比差异有统计学意义(P＜0.05).结论 使用高中剂量黄连解毒颗组方粒剂一定时间后,小鼠肠道组织黏膜损伤,出现细菌移位及球杆菌比例失调现象,而低剂量对小鼠肠道组织无明显损伤作用.     

布洛芬微囊颗粒剂的药物动力学研究

用交叉双盲单剂量药物动力学研究法对布洛芬(Ibuprofen,Ⅰ)微囊颗粒剂和树脂剂颗粒剂进行比较。8例健康志愿者,男女各4人,平均年龄23岁。SGOT、SGPT、血清肌酐均正常。受试者交替随机服两种颗粒剂、剂量各为600 mg。采用基于形成药物的甲酯,以重氮甲烷作内标的改良GLC 法,测定血浆中Ⅰ的浓度。本方法在建立一改良的血提取相以及内标的选择方面属首创。结果表明,两种颗粒剂处方之间的差异无显著统计意义,与树脂剂颗粒比较,微囊颗粒剂的t1/2、平均t_(max)均     

治疗窗窄药片5种分剂量准确性研究

目的了解5种治疗窗窄药片分剂量的准确性,为临床合理用药提供参考。方法应用药片切割器、剪刀、刀片对5种药片分剂量成2等份及4等份。结果 5种治疗窗窄药片中,硬度最大和最小的药片分别为氨茶碱、地高辛;直径最大和最小的药片分别为卡马西平、地高辛;厚度最大和最小的药片分别为卡马西平、地高辛。地高辛（切）、苯妥英钠（切）FW1/2和FW1/4与TW1/2和TW1/4比较差异有统计学意义（P〈0.05）;地高辛（剪）、氨茶碱（剪）、华法林钠（剪）、苯妥英钠（剪）FW1/4与TW1/4比较差异有统计学意义（P〈0.05和P〈0.01）;华法林钠（刀）FW1/2和FW1/4与TW1/2和TW1/4比较差异有统计学意义（P〈0.01）。5种药片用3种工具分剂量至少有5片超出质量差异15%,均不符合欧洲药典标准。分剂量成2等份时,应用剪刀超出平均质量15%的药片数均较其他2种方法多;分剂量成4等份时,3种方法超出平均质量15%的药片数均较分剂量成2等份时多。结论 5种治疗窗窄药片应用3种工具分剂量准确性较差,临床用药应引起足够的注意。需要调整给药剂量时,可考虑用液体制剂分剂量。     

治疗窗窄药片5种分剂量准确性研究

目的 了解5种治疗窗窄药片分剂量的准确性,为临床合理用药提供参考.方法 应用药片切割器、剪刀、刀片对5种药片分剂量成2等份及4等份.结果 5种治疗窗窄药片中,硬度最大和最小的药片分别为氨茶碱、地高辛;直径最大和最小的药片分别为卡马西平、地高辛;厚度最大和最小的药片分别为卡马西平、地高辛.地高辛(切)、苯妥英钠(切)FW(1/2)和FW(1/4)与TW(1/2)和TW(1/4)比较差异有统计学意义(P<0.05);地高辛(剪)、氨茶碱(剪)、华法林钠(剪)、苯妥英钠(剪)FW(1/4)与TW(1/4)比较差异有统计学意义(P<0.05和P<0.01);华法林钠(刀)FW(1/2)和FW(1/4)与TW(1/2)和TW(1/4)比较差异有统计学意义(P<0.01).5种药片用3种工具分剂量至少有5片超出质量差异15%,均不符合欧洲药典标准.分剂量成2等份时,应用剪刀超出平均质量15%的药片数均较其他2种方法多;分剂量成4等份时,3种方法超出平均质量15%的药片数均较分剂量成2等份时多.结论 5种治疗窗窄药片应用3种工具分剂量准确性较差,临床用药应引起足够的注意.需要调整给药剂量时,可考虑用液体制剂分剂量.     

美沙拉嗪肠溶缓释颗粒剂的药代动力学研究

目的评价美沙拉嗪肠溶缓释颗粒剂体内药物代谢动力学,通过与市售制剂的药动学特征比较,阐述美沙拉嗪肠溶缓释颗粒剂的临床前药代动力学特征,为新药评价提供可靠依据。方法以单剂量和多剂量2种方式口服给药,选取比格犬为受试对象,采用LC-MS/MS法测定血浆样品药物浓度。通过药动学参数估算和统计分析,评价美沙拉嗪肠溶缓释颗粒剂的体内吸收和消除过程、相对生物利用度、体内蓄积效应以及与市售制剂的药动学特征进行比较。结果美沙拉嗪肠溶缓释颗粒剂在比格犬体内单剂量口服(灌胃)给药后,美沙拉嗪缓释颗粒剂和美沙拉嗪肠溶片以美沙拉嗪表征的相对生物利用度分别为101.30%±20.20%、109.20%±30.80%。多剂量口服(灌胃)给药后,体内无蓄积效应。通过相对生物利用度和药代动力学参数的统计分析比较研究,提示美沙拉嗪肠溶缓释颗粒剂与市售的2种制剂无显著性差异。结论美沙拉嗪肠溶缓释颗粒剂吸收和消除过程基本呈线性动力学特征,多剂量给药后5 d左右达稳态、体内无蓄积,药动学参数与市售制剂无显著性差异。     

克拉霉素颗粒剂和片剂的正常人体药物动力学和生物等效性

8名健康男性志愿者自身交叉单剂量口服 5 0 0mg克拉霉素颗粒剂和片剂 ,采用微生物法测定经时过程血药浓度 .用 3P87程序拟和 ,两制剂的血药浓度 时间曲线均符合单室模型 .求得克拉霉素颗粒剂和片剂药物动力学参数 .Ka分别为 (3.5 5± 0 .92 )和 (1.6 2± 0 .16 )h-1;t1/2 分别为(4.90± 0 .19)和 (5 .0 6± 0 .2 5 )h ;Cmax分别为 (2 .6 3± 0 .2 7)和 (2 .2 9± 0 .2 6 ) μg/mL ;Tmax分别为(1.12± 0 .10 )和 (1.6 8± 0 .0 6 )h ;AUC分别为 (2 1.6 7± 2 .5 4)和 (2 1.13± 3.19) μg·h/mL .经统计学处理 :两制剂的药动学参数Ka、Cmax、Tmax均有显著性差异 (P <0 0 5 ) ,t1/2 无显著性差异 (P >0 0 5 ) ,克拉霉素颗粒剂相对于片剂的生物利用度F为 (10 3.36± 11.15 ) % .经方差分析、单双侧检验法分析 ,证明两制剂具有生物等效性 .     

番泻叶颗粒剂治疗癌痛病人阿片类药物相关性便秘的临床疗效观察

目的 观察番泻叶颗粒剂治疗癌痛病人阿片类药物相关性便秘(OIC)的疗效.方法 选取患有OIC的癌痛病人120例,采用随机数字表法分为治疗组(番泻叶颗粒剂组)和对照组(乳果糖口服溶液组),分别采用番泻叶颗粒剂和乳果糖口服溶液治疗.根据肠功能指数(BFI)量表对病人便秘进行评分,比较两组病人治疗前、后的便秘评分和治疗疗效,并比较两组病人毒副反应的发生.结果 治疗组60例病人治疗便秘的总有效率为98.3%,对照组60例病人治疗便秘的总有效率为76.67%.秩和检验比较两组病人的治疗疗效,Z值为-3.82,P<0.05,差异有统计学意义.可认为番泻叶颗粒剂治疗癌痛病人OIC疗效高于乳果糖口服溶液.对两组病人治疗前、后便秘评分进行比较,治疗组治疗前、后的便秘评分分别为(68.78±13.18)分和(14.50±10.52)分,对结果进行t检验,差异有统计学意义(t=31.2,P<0.05).对照组治疗前、后的便秘评分分别为(69.89±12.07)分和(26.62±20.23)分.两组治疗前便秘评分差异无统计学意义(t=0.482,P=0.63),两组治疗后便秘评分差异有统计学意义(t=-4.12,P<0.05),治疗组在降低便秘评分上优于对照组.两组病人腹痛(Z=-1.96,P>0.05)、腹泻(Z=-1.97,P>0.05)以及呕吐(Z=-0.58,P>0.05)的发生比较,差异无统计学意义.结论 番泻叶颗粒剂能有效治疗阿片类药物相关性便秘,且毒副反应轻微.     

阿尼西坦颗粒剂在正常人体内的药动学及相对生物利用度

目的 :研究阿尼西坦颗粒剂在正常人体内的药代动力学及相对于胶囊剂的生物利用度。方法 :采用反相高效液相色谱法 ,测定 8名健康男性志愿者自身交叉单剂量口服阿尼西坦颗粒剂和胶囊剂 (60 0mg)经时血药浓度。结果 :用 3p87程序拟和 ,符合一级吸收、单室模型。阿尼西坦胶囊剂和颗粒剂的药代动动力学参数 :Ka分别为(0 0 76± 0 1 9)min 1 、(0 348± 0 0 54)min 1 ;t1 / 2 分别为 (2 2 .69± 2 .45)min、(2 7.78± 1 .50 )min ;Cmax分别为 (61 .2 4±4 .1 5)ng·ml 1 、(76 .2 4± 3 .60 )ng·ml- 1 ;Tmax分别为 (2 2 .94± 1 .66)min、(1 1 .94± 0 .58)min ;AUC分别为 (3735 .78±1 92 .3)ng·min·ml- 1 、(3754 .98± 1 63 .58)ng·min·ml- 1 。经统计学处理 ,两制剂药代动力学参数t1 / 2 无显著性差异(P >0 .0 5) ,Ka、Cmax、Tmax有显著性差异 (P <0 .0 5) ;阿尼西坦颗粒剂相当于胶囊剂的生物利用度为 1 0 0 50 %±2 59%。结论 :经方差分析、配对双单侧t检验 ,两制剂具有生物等效性     

Readmissions for treatment for alcoholism

First admissions and readmissions for alcoholism have risen steeply in recent decades. This study looked at readmission histories for four cohorts of alcoholics first admitted to inpatient psychiatric treatment in 1967-68, 1973, 1977 or 1979. Over the twelve years the first cohort was observed, alcoholics on average spent 254 days in treatment and had 2.14 alcohol-related readmissions. However the distributions were very skewed: 50% stayed less than 92 days and 45.6% had no readmissions at all. All four cohorts yielded similar results over comparable time periods and all showed markedly skewed distributions reflecting the diversity of readmission histories among alcoholics. Policy decisions about alcoholism inpatient treatment must take account of this diversity.     

Projections for insulin treatment for diabetics

The evolution of insulin treatment of diabetes has dramatically changed the natural course of this disease. Modern recombinant DNA technology has brought about many new insulin analogues with improved pharmacokinetics, resulting in better glycemic control. In addition, improved insulin delivery systems, such as insulin pumps and pens, have been introduced to provide convenience and to enhance patient compliance. Efforts are currently being devoted to developing noninvasive insulin formulations, such as oral and pulmonary insulin. A number of products are at different stages of clinical trials. Meanwhile, the quest for a permanent cure for diabetes continues. The frontier of diabetes research has gone through a period of substantial expansion, with the emergence of new areas that include gene therapy, islet cell transplantation and diabetic vaccine. Technological breakthroughs, such as recombinant DNA, nanotechnology, microarray-aided genomics and proteomics, will provide more profound insights into the pathogenesis, and the immunological and biological basis of diabetes. Our growing knowledge in these areas will ultimately contribute to the discovery of preventive methods against or a cure for this disease.     

Control of craving for methamphetamine: development of scales for dependence and search for medicines for treatment]

Methamphetamine dependence presents a serious problem not only for patients but also for society. Medical treatment has mainly targeted psychotic symptoms such as hallucination and delusion, and ignored the symptoms of craving, which are the major cause of dependence. Therefore, the risk of lapse into methamphetamine reuse remains very high. Although development of both medicines and programs for treatment of craving is needed, progress has been hampered by the lack of appropriate scales for assessing the severity of dependence and craving. On the other hand, recent breakthroughs in genomic sciences and molecular medicine have made it possible to investigate the molecular mechanisms underlying craving in animals. This paper reviews studies on the development of scales for assessing the severity of methamphetamine dependence and craving, together with recent data on candidate medicines for craving treatment in animals. The reliability and validity of the revised Addiction Severity Index -Japanese version (ASI-J) was confirmed after its administration to 100 drug abuse patients. The Craving Index was also newly developed, and its validity for prediction of relapse was confirmed. In animal experiments, fluoxetine, a selective serotonin reuptake inhibitor, was recognized as a candidate medicine for treatment of methamphetamine dependence.     

注射用硫普罗宁细菌内毒素检查法的建立

目的:建立注射用硫普罗宁细菌内毒素检查方法.方法:参照<中国药典>2010年版二部细菌内毒素检查法进行试验.结果:将硫普罗宁稀释至1 mg·mL-1时对细菌内毒素和鲎试剂的反应无干扰作用.结论:该品种可采用细菌内毒素检查法控制药品质量.