Ferron Geraldine M, Ku Sherry, Abell Madelyn, Unruh Mary, Getsy John, Mayer Philip R, Paul Jeffrey
Clinical Pharmacokinetics, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA.
Am J Health Syst Pharm. 2003 Jul 1;60(13):1324-9. doi: 10.1093/ajhp/60.13.1324.
The bioavailability of pantoprazole when administered as a suspension in sodium bicarbonate solution and as the oral tablet was studied. In an open-label, randomized, two-period crossover study, healthy fasting subjects received either one enteric-coated 40-mg pantoprazole tablet by mouth with 240 mL of water or 20 mL of a suspension prepared from one crushed pantoprazole tablet and 840 mg of sodium bicarbonate solution and administered via a nasogastric tube. Treatments were separated by a 48-hour washout period. Blood samples were collected at intervals up to 24 hours after drug administration for measurement of pantoprazole concentration by high-performance liquid chromatography (HPLC) and estimation of pharmacokinetic values. A separate study was conducted to determine pantoprazole's stability in the suspension for up to three months at 25, 5, and -20 degrees C; concentrations were measured by HPLC. Twelve subjects completed the study. The suspension yielded pantoprazole Cmax values similar to those of the tablet formulation, but the drug was 25% less bioavailable. There was no lag time for the suspension. The suspension was stable for up to two weeks at 5 degrees C and up to three months at -20 degrees C. A suspension of pantoprazole in sodium bicarbonate solution yielded a Cmax similar to that of the tablet formulation, and the drug was quickly absorbed. However, bio-availability was slightly lower with the suspension than with the tablet.
研究了泮托拉唑以碳酸氢钠溶液混悬液和口服片剂形式给药时的生物利用度。在一项开放标签、随机、两阶段交叉研究中，健康的空腹受试者口服一片40毫克肠溶泮托拉唑片剂并饮用240毫升水，或者通过鼻胃管服用由一片碾碎的泮托拉唑片剂和840毫克碳酸氢钠溶液制成的20毫升混悬液。治疗间隔48小时洗脱期。给药后24小时内定期采集血样，通过高效液相色谱法（HPLC）测定泮托拉唑浓度并估算药代动力学值。还进行了一项单独研究，以确定泮托拉唑在25℃、5℃和-20℃下在混悬液中的稳定性，长达三个月；浓度通过HPLC测定。12名受试者完成了研究。混悬液产生的泮托拉唑Cmax值与片剂制剂相似，但药物的生物利用度低25%。混悬液没有滞后时间。混悬液在5℃下最多稳定两周，在-20℃下最多稳定三个月。泮托拉唑在碳酸氢钠溶液中的混悬液产生的Cmax与片剂制剂相似，药物吸收迅速。然而，混悬液的生物利用度略低于片剂。
