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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >A novel once daily microparticulate dosage form comprising lansoprazole to prevent nocturnal acid breakthrough in the case of gastro-esophageal reflux disease: preparation, pharmacokinetic and pharmacodynamic evaluation
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A novel once daily microparticulate dosage form comprising lansoprazole to prevent nocturnal acid breakthrough in the case of gastro-esophageal reflux disease: preparation, pharmacokinetic and pharmacodynamic evaluation

机译：包含兰索拉唑的新型每日一次微粒剂型，在胃食管反流疾病中可防止夜酸突破：制剂，药代动力学和药效学评价

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摘要

The objective of this study was to formulate and evaluate the lansoprazole (LPZ)-loaded microparticles to prevent nocturnal acid breakthrough in the case of gastro-esophageal reflux disease (GERD). The micropaniculate delivery system was prepared by solvent evaporation method using Eudragit RS100 as a matrix polymer followed by enteric coated with Eudragit S100 and hydroxypropyl methylcellulose phthalate HP55 using spray drying method. The enteric coated microparticles were stable in gastric pH condition. In vivo pharmacokinetic and pharmacodynamic studies in male Wistar rats demonstrated that enteric coated microparticles sustained release of LPZ and promoted ulcer healing activity. In other words, the microparticulate dosage form provided effective drug concentration for a longer period as compared to conventional extended release dosage form, and showed sufficient anti-acid secretion activity to treat acid related disorders including the enrichment of nocturnal acid breakthrough event based on a once daily administration.
机译：这项研究的目的是配制和评估载有兰索拉唑（LPZ）的微粒，以防止在胃食管反流病（GERD）情况下夜间酸突破。通过溶剂蒸发法，使用Eudragit RS100作为基质聚合物，然后通过喷雾干燥法，用Eudragit S100和羟丙基甲基纤维素邻苯二甲酸酯HP55进行肠溶衣，制备微颗粒递送系统。肠溶包衣的微粒在胃pH条件下是稳定的。对雄性Wistar大鼠的体内药代动力学和药效学研究表明，肠溶衣微粒可持久释放LPZ并促进溃疡愈合活性。换句话说，与常规的延长释放剂型相比，微粒剂型提供了更长的有效药物浓度，并且显示了足够的抗酸分泌活性以治疗与酸有关的疾病，包括基于一次的夜间酸突破事件的富集。日常管理。

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