医药行业科技成果产业化的风险控制

医药行业科技成果产业化与其他行业科技成果转化相比具有更高的风险，转化能力也是最低的，因此，对其从事前、事中、事后三方面加强风险控制具有重要的观实意义。     

Bioavailability and Pharmacokinetics of a New Sustained-Release Potassium Chloride Tablet

The bioavailability of a new sustained-release potassium chloride (KC1) tablet, designed for once-a-day dosing, was compared to a KC1 elixir using urinary excretion data. The study utilized 25 male volunteers dosed in a crossover design in a dietary/activity-controlled environment. The regimens consisted of a total of 80 mEq of potassium in three equally divided doses of elixir every 6 hr and a single 80-mEq dose using four 20-mEq sustained-release (SR) tablets. The mean time to maximum rate of potassium urinary excretion was 2.2 hr for the first elixir dose and 5.5 hr after the SR tablet (P < 0.01), thereby supporting the prolonged-release properties of this formulation. After correction for baseline urinary potassium excretion, the mean total 24-hr urinary potassium excretion was 42.18 mEq for the elixir and 40.41 mEq for the SR tablet. The results indicate that the absorption pattern from the SR tablet is equal to three doses of KC1 elixir dosed 6 hr apart.     

左旋氨氯地平治疗轻中度高血压疗效及不良反应的临床研究

目的:为评价左旋氨氯地平降压疗效及不良反应,并与氨氯地平相比较。方法:采用随机分组平行对照方法,将120例轻、中度高血压患者分成左旋氨氯地平组(60例),口服2.5～5mg·d~(-1)和氨氯地平组(60例),口服5～10mg·d~(-1)。观察5周。每周一次上午延迟1～4小时用药并测诊室谷值坐位血压、心率、观察不良反应。结果:5周未左旋氨氯地平与氨氯地平组治疗有效反应率分别为86.7％和83.3％,每组治疗前后比较差异非常显著(P<0.01)。组间比无显著性差异(P>0.05)。左旋氨氯地平组不良反应发生率6.7％,氨氯地平组为16.7％(P>0.05),但试验组不良反应程度更轻微。结论:左旋氨氯地平与氨氯地平治疗高血压同样有效,不良反应可能更小。     

泰勒宁片和科洛曲片用于隆乳术后镇痛的比较

目的:评价泰勒宁片和科洛曲片对隆乳手术后疼痛的疗效和不良反应。方法:采用随机开放平行对照试验。共完成60例,其中A组30例予泰勒宁片,单次1片;B组30例予科洛曲片,单次1片。结果:泰勒宁片对隆乳手术后引起的中度或重度疼痛总有效率可达96.7%,科洛曲片的总有效率可达83.3%。服药后泰勒宁片组的疼痛强度差均高于科洛曲组,经统计学处理,有显著性差异(P<0.05)。不良反应发生率较科洛曲片组高。结论:泰勒宁片为中强度镇痛药,对于隆乳手术后引起的中重度疼痛有良好的镇痛效果。     

紫外分光光度法测定对乙酰氨基酚泡腾片含量

本文用紫外分光光度法在２５７±１ｎｍ波长处测定对乙酰氨基酚泡腾片的含量，其浓度与吸收度的线性关系良好，相关系数ｒ＝０．９９９９８。平均回收率为９９．９４％，变异系数为０．２０％。本法简便、快速、结果准确。     

尼莫地平片溶出度的研究

采用转篮法对尼莫地平国产市售片，进口片和自制片在不同介质、不同转速和ＰＨ条件下的溶出度进行测试。结果表明，介质对尼莫地平溶出具有很大的影响，而最佳测定方法是以０．１％的十二烷基硫酸钠水溶液为介质，转速１５０ｒ／ｍｉｎ。     

头孢氨苄缓释片在健康人体内的生物利用度和药物动力学

目的:比较头孢氨苄缓释片和普通胶囊的生物利用度和药物动力学。方法：10例健康志愿者分别单剂量口服500mg头孢氨苄缓释片和普通胶囊，血药浓度测定方法为HPLC法。结果：两种剂型体内过程均符合一室开放模型，缓释片的达峰时间（Tmax）为（2．58±0．59）h，峰浓度（Cmax）为（10．08±1．68）μg／ml．吸收速率常数（Ka）为（0．90±0．53）／h，消除速率常数（Ke）为（0.26±0.02）／g，半衰期（T1／2）为（2.67±0.23）h，清除率（Cl）为（6.93±1.71）L／h，分布容积（Vd）为（26.66±6.72）L，药一时曲线下面积（AUC）为（48.31±9.32）μg·h／ml。两种剂型T一C一Ka、Ke、T1／2和Cl均存在显著性差异（P＜0．01），Vd、AUC无显著性差异（P＞0．05）；缓释片的相对生物利用度为（104．90±8．35）％。结论：缓释片的吸收减慢，Tmax推迟，T1／2延长，可减少服药次数，提高药物治疗的顺应性。     

吡哌酸片的电荷转移反应分光光度测定

研究了吡哌酸与四氯苯醌间的荷移反应．两者在硼砂缓冲溶液中形成１∶１的络合物，其λ_（ｍａｘ）为３３０．８ｎｍ，摩尔吸光系数ε＝１．６６×１０~４，ＲＳＤ为２．２％。用于测定制剂含量，结果与药典方法一致。     

Molecular Pharmacology of Topiramate: Managing Seizures and Preventing Migraine

Topiramate is a neuromodulatory compound with stabilizing properties that was initially introduced for the management of partial seizures. Topiramate has been demonstrated to modify several receptor-gated and voltage-sensitive ion channels, including voltage-activated Na⁺ and Ca²⁺ channels and non-NMDA receptors. These receptors have been implicated in the pathophysiology of both epilepsy and migraine. The pharmacological mechanisms of action for topiramate that may explain its antiepileptic and migraine preventive activities will be discussed in this review. In addition, the potential relationship between the molecular activities of topiramate and its efficacy in epilepsy and migraine prevention will be emphasized.