Abstract Praziquantel is the drug of first choice for the treatment of the human schistosomiasis. It is administered orally, requiring high doses to overcome adverse biopharmaceutical properties, including high lipophilia and intense hepatic first pass metabolism. According to its biopharmaceutical profile, praziquantel has very low water solubility and high permeability. Therefore, dissolution is the limiting factor for absorption in the gastrointestinal tract. Improvement of the aqueous solubility of the drug would reduce the currently high oral doses. Meanwhile, montmorillonite and sepiolite are clay minerals, with a high adsorption and swelling properties, potentially useful as a low-cost nanocarrier to design praziquantel delivery systems. In this work, the interactions between the drug and clay minerals are studied experimentally, with the aim of improving the biopharmaceutical profile of the drug. The results showed the effective loading of the drug in the clay minerals as well as the significant increase of the dissolution rate and the dissolved amount of praziquantel, potentially improving the bioavailability of the drug.

中文翻译：

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通过与蒙脱石和海泡石相互作用改善吡喹酮的生物制药

摘要 吡喹酮是治疗人血吸虫病的首选药物。它是口服给药，需要高剂量以克服不利的生物制药特性，包括高亲脂性和强烈的肝脏首过代谢。根据其生物制药特性，吡喹酮具有极低的水溶性和高渗透性。因此，溶解是胃肠道吸收的限制因素。药物水溶性的改善将减少目前的高口服剂量。同时，蒙脱石和海泡石是粘土矿物，具有高吸附性和溶胀性，可用作设计吡喹酮递送系统的低成本纳米载体。在这项工作中，通过实验研究了药物与粘土矿物之间的相互作用，目的是改善药物的生物制药特性。结果表明药物在粘土矿物中的有效负载以及溶解速率和吡喹酮的溶解量显着增加，潜在地提高了药物的生物利用度。