加替沙星软胶囊健康志愿者体内药动学和生物等效性研究

目的:评价两种加替沙星制剂的人体生物等效性。方法:采用两制剂双周期交叉试验设计。18名健康志愿者分别单剂量口服受试制剂加替沙星软胶囊或参比制剂加替沙星片400 mg,采用高效液相色谱法(HPLC)测定血液中药物浓度。结果:受试制剂与参比制剂的Tmax分别为(1.85±0.60)和(2.08±0.65)h,Cmax分别为(3.556±0.904)和(3.575±0.908)μg.mL-1,t1/2分别为(7.76±1.27)和(7.91±1.26)h,AUC0~t分别为(29.71±7.10)和(32.00±7.67)μg.h.mL-1,AUC0~∞分别为(30.91±7.53)和(33.32±8.04)μg.h.mL-1。各药动学参数无显著性统计学差异(P>0.05),加替沙星软胶囊相对生物利用度F为(95.1±16.7)%。结论:2种加替沙星制剂具有生物等效性。     

加替沙星治疗期间发生精神障碍

1例75岁女性患者,于胆囊切除术后给予加替沙星0.4g溶入5%葡萄糖注射液500ml静脉滴注。第2天静脉滴注结束后约5.5h,患者出现幻视、幻觉,兴奋、躁动及迫害妄想。12h后症状逐渐缓解。第3天停用加替沙星,精神症状未再出现。     

加替沙星治疗社区获得性肺炎的成本-效果分析

目的:对加替沙星治疗敏感菌所致的社区获得性肺炎的3种给药方案进行药物经济学分析。方法:A组方案为静脉滴注加替沙星注射液,B组方案为静脉滴注加替沙星注射液与口服序贯疗法;C组为口服加替沙星片剂。采用成本-效果分析法对3种方案进行回顾性分析。结果:采用序贯疗法的B组方案成本-效果比较低,且每增加一个效果单位,B组费用最低。结论:从药物经济学的角度,B组方案较佳。     

加替沙星引起血糖异常不良反应分析

通过对国内外文献和病例报告数据库的系统分析，旨在了解加替沙星引起血糖异常不良反应的发生情况、影响因素和发生特征，并提出风险管理的初步意见。     

甲磺酸加替沙星与加替沙星的药物代谢动力学比较

目的甲磺酸加替沙星(GATM)和加替沙星(GAT)是喹诺酮类抗感染药物的新型制剂,对改变酸根的甲磺酸加替沙星在大鼠体内的药物代谢动力学规律和特点进行了考察并和加替沙星进行比较。方法以SD大鼠为研究对象,单剂量口服等克分子剂量(0.0497 mmol.kg-1)GATM和GAT后,采用高效液相色谱法(HPLC)检测血清中GAT的含量,采用3p97程序软件计算二者在大鼠体内的药代动力学参数。结果大鼠单次口服GATM(23.43 mg.kg-1)和GAT(20 mg.kg-1)后,二者的血药浓度经时变化符合一级消除动力学特征,药时曲线拟合为二房室模型,其中GATM的药代动力学参数为:血浆消除半衰期(T12β)9.13 h,药时曲线下面积(AUC)15.05 mg.L-1.h,血药峰浓度(Cm ax)4.41mg.L-1,达峰时间(Tm ax)0.5 h;而GAT的药代参数分别为:T12β10.70 h,AUC 13.84 mg.L-1.h,Cm ax4.25 mg.L-1,Tm ax0.5 h。结论在上述剂量条件下GATM与GAT的吸收(Tm ax、Cm ax、AUC)、分布(V/F)和消除(T12β、CL)参数差异未见显著性,二者的血药浓度经时变化相似,药代动力学规律基本一致。     

注射用加替沙星和替硝唑注射液配伍稳定性研究

目的考察注射用加替沙星和替硝唑注射液配伍稳定性。方法采用高效液相色谱法测定配伍前后两种药物的含量，并观察和测定外观性状、pH值变化。结果注射用加替沙星和替硝唑注射液配伍后在室温及350C放置24h，配伍溶液外观性状、pH值及2种组分的含量均无明显变化。结论注射用加替沙星与替硝唑注射液配伍后至少24h稳定，可配伍使用。     

双氯灭痛滴眼液的研制

 拟定了双氯灭痛滴眼液的处方及其制备工艺，并制定了质量控制标准。用紫外分光光度法测定双氯灭痛的含量，结果于２７６ｎｍ处有最大吸收。同时对眼刺激性和溶液稳定性进行了试验，表明双氯灭痛滴眼液对眼无刺激，其有效期为２．６年。     

Levocabastine eyedrops in comparison with cromoglycate in the treatment of conjunctivitis in children with birch pollinosis

During the season 65 children, 7–19) yours old, with conjunctivitis due to birch pollinosis were treated with eyedrops, either levocabastine b. i. d. (+ placebo b. i. d.) ( n =32), or cromoglycate q. i. d. ( n = 33). Beclomethasone was given to children with rhinitis. Symptoms of conjunctivitis and sedation as well as pollen counts were assessed daily. Blood was drawn before and at the end of the treatment. When mean weekly scores for symptoms of conjunctivitis or sedation were evaluated there were no significant differences between the treatments. A dynamic statistical method correlating symptoms with pollen counts on the same and previous days was applied showing that the children treated with levocabastine had a quicker reduction of their conjunctivis symptoms after a pollen peak (p < 0.05) but were tired for a longer period (p < 0.01). Other side effects were few and similar in the groups. No significant changes were seen in the blood safety data. The differences between the groups were small, and from a clinical point of view the conclusion is that levocabastine taken twice daily is as effective and as free of side effects as cromoglycate taken 4 times a day.