兰索拉唑中有机溶剂残留量的毛细管GC测定

建立了毛细管气相色谱法测定兰索拉唑中甲醇、丙酮、乙腈、氯仿的残留量.采用RTX-50毛细管柱,程序升温.各溶剂检测限分别为18、50.4、1.46和0.4ng,平均回收率分别为102.3%、100.4%、101.8%和1013%.     

Treatment of erosive reflux esophagitis resistant to H2-receptor antagonist therapy

Fifty-four patients with endoscopically documented therapy-resistant erosive reflux esophagitis were treated with lansoprazole, a new proton pump inhibitor, for up to 12 weeks. Prior to entry, all had remained unhealed after treatment with at least two histamine₂-receptor antagonists, at therapeutic doses or higher, for at least 12 weeks. Patients were randomized to receive either 30 or 60 mg lansoprazole once daily. Endoscopy was performed and symptoms assessed at weeks 2, 4, 6, 8, and 12. Fifty-nine percent of the 50 evaluable patients were healed (ie, no evidence of erosions) after only two weeks of lansoprazole. Cumulative endoscopic healing rates were 82% and 92% by week 4 and week 8, respectively, and the two doses were equally effective in healing. The 30- and 60-mg doses effected a decrease in the overall symptom score from 5.30 and 4.85 to 2.35 and 1.67, respectively, by the final treatment visit (P=0.001). No clinically significant adverse events or changes in laboratory parameters were observed, and no patients withdrew prematurely from the study. This study demonstrates that lansoprazole therapy is highly effective in healing erosive reflux esophagitis resistant to therapy with histamine H₂-receptor antagonists.Supported by a grant from TAP Pharmaceuticals Inc., Deerfield, Illinois.     

Effect of lansoprazole on DNA integrity of human spermatozoa and activity of seminal creatine kinase

Although lansoprazole (brand name Prevacid) is a commonly used dug to manage various acid-related gastrointestinal diseases, little is known about its effects on human semen quality and sperm parameters. Here, we aimed to investigate the effect of lansoprazole on DNA integrity of human spermatozoa and activity of seminal creatine kinase. DNA integrity of human spermatozoa was assessed by the Apo-Direct™ kit followed by flow cytometry. The activity of creatine kinase was measured by kinetic spectrophotometric method using commercially available kits following the International Federation of Clinical Chemistry recommendations. Lansoprazole at 3 µg/ml, after 1-hr incubation period, did not show any significant increase in fluorescein isothiocyanate fluorescence (p > .05) and hence on the content of DNA breaks of human spermatozoa. In addition, there was no significant change (p = .8113) in the activity of seminal creatine kinase by the effect of lansoprazole. In conclusion, lansoprazole at 3 µg/ml did not alter DNA integrity of human spermatozoa or activity of seminal creatine kinase after 1-hr incubation period.     

Influence of lansoprazole,famotidine, roxatidine and rebamipide administration on the urea breath test for the diagnosis of Helicobacter pylori infection

BACKGROUND AND AIM: The sensitivity of the urea breath test (UBT) has been reported to be influenced by the administration of omeprazole, lansoprazole and ranitidine. However, it is unclear whether other H2 receptor antagonists (H2RA), except ranitidine, and rebamipide, a mucosal protective agent, affect UBT sensitivity. The aim of this study is to clarify the effects of lansoprazole, famotidine, roxatidine and rebamipide administration on UBT sensitivity. METHODS: Subjects comprised 30 volunteers with Helicobacter pylori infection. All subjects were examined by the 13C-UBT on four occasions: (i) without medication (control); (ii) after the administration of 30 mg lansoprazole (u.i.d) for 14 days; (iii) after the administration of 100 mg rebamipide (t.i.d) for 14 days; and (iv) after the administration of 20 mg famotidine or 75 mg roxatidine (b.i.d) for 14 days. In the H2RA study, individuals were randomized into two groups of 15 subjects and were administered either famotidine or roxatidine. RESULTS: Five of the 30 cases administered lansoprazole and one of the 15 cases given roxatidine gave a false-negative UBT result. No negative UBT results were observed in patients administered famotidine or rebamipide. CONCLUSION: Patients showing negative UBT results during the administration of proton pump inhibitors and H2RA should be re-examined after the cessation of these drugs to confirm the true negativity of H. pylori infection.     

RP—HPLC法测定人血浆中兰索拉唑浓度

目的:建立 RP-HPLC 法测定人血浆中兰索拉唑浓度。方法:1 mL 血浆样品以奥美拉唑为内标,加入0.5 mL Na_2HPO_4溶液(0.5 mol·L~(-1),pH 9.05)碱化,用5 mL 乙醚-二氯甲烷(7:3,v/v)混合液振荡萃取,分取有机相空气流下吹干。残渣用200μL甲醇-0.1 mol·L~(-1)碳酸钠(50:50,v/v)混合液溶解,40 μL进样。采用 NUCLEOSIL C_(18)分析柱(250 mm×4.6 mm,5μm),以0.025 mol·L~(-1)磷酸二氢钠-乙腈(60:40,v/v)为流动相,流速为1 mL·min~(-1),柱温为30℃,于285 nm 波长下检测。结果:兰索拉唑在20～2400μg·L~(-1)范围内线性关系良好(r=0.9996),最低检测浓度为20μg·L~(-1)。血浆中低、中、高3种浓度的萃取回收率(n=5)分别为69.9%,64.0%,58.8%;RSD(n=5)分别为7.94%,5.33%,5.39%;方法回收率(n=5)分别为98.6%,106.3%,101.9%;日内和日间精密度均小于10%。结论:该法操作简单,灵敏,准确,重现性好,适用于该药的临床药代动力学研究。     

注射用兰索拉唑与常用输液的配伍稳定性

目的：研究注射用兰索拉唑与4种常用输液配伍的稳定性。方法：采用HPLC法考察与4种输液按临床应用配伍，干室温条件下，考察12h内pH值，外观和含量的变化情况。结果：在室温条件下，与生理氯化钠溶液配伍后，6h内基本稳定，与10％葡萄糖，5％葡萄糖氯化钠和5％葡萄糖配伍后，随时间延长，含量分别降至97．5％，97．6％．98．0％。结论：注射用兰索拉唑可与生理氯化钠溶液配伍使用，但是应在4h内用完。     

HPLC测定注射用兰索拉唑中兰索拉唑的含量和有关物质

 目的采用高效液相色谱法建立注射用兰索拉唑有关物质检查及其含量测定方法。方法Diamonsil-C₁₈柱(4.6 mm×200 mm,5μm),以甲醇-水-三乙胺-磷酸(640∶360∶5∶1.5,pH为7.3)为流动相,检测波长为284 nm。结果制剂中辅料对主药测定无干扰,兰索拉唑与有关物质完全分离。在10.0～400.0 mg·L^-1内峰面积与浓度呈良好的线性关系。精密度(RSD=0.13%)良好。平均回收率为99.6%。结论本方法简便,迅速,准确,专属性强。     

兰索拉唑口服治疗消化性溃疡急性大出血

目的：观察兰索拉唑口服治疗消化性溃疡急性大出血的疗效。方法：３０例消化性溃疡急性大出血病人（男性２４例，女性６例，年龄４８±ｓ１６ａ）予兰索拉唑３０ｍｇ，ｐｏ，ｑｄ×（１０～１４ｄ），并酌情输液、输血。结果：兰索拉唑３０例（１００％）止血成功，住院天数为１４．１±２．１ｄ；输血量为０。未见药物不良反应。结论：兰索拉唑口服对消化性溃疡急性大出血有良好疗效。     

兰索拉唑对消化溃疡的疗效和药物动力学及生物利用度

目的：观察兰索拉唑对消化性溃疡的疗效和患者体内药物动力学及生物利用度。方法：３１例消化性溃疡患者随机分成两组,分别ＰＯ两组兰索拉唑制剂３０ｍｇ．ｑｄ,连续服用１ｍｏ后观察儿,并用ＨＰＬＣ法测定单剂量ＰＯ后的血药浓度,模拟房室模型度计算药物动力学参数及利用度。结果：国产和进口制剂用药后５ｄ内腹痛消失的病人均约占７０％,总有效率为１００％,组间无明显差别（Ｐ〉０．０５）;单剂量ＰＯ后的经浓度时间曲线均