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以拉伸性能和溶化时间为指标筛选处方,制备了以聚乙烯醇(PVA)和玉米淀粉为成膜材料的苯甲酸利扎曲普坦速溶膜剂,并进行体内外评价。采用不同方法测定溶化时间,结果均表明其体外溶化迅速,并在Beagle犬口中能在20 s内完全溶化。使用桨法和漏槽式溶出仪法测定其体外溶出特性,结果均显示40~45 s时的溶出率达80%以上,1 min内完全溶解。鉴于膜剂的独特性质,以溶出度来评价速溶膜的溶化性能更为科学,其中漏槽式溶出仪法重现性更好、区分力更大,适合膜剂体外溶出性能的评价。Beagle犬体内药动学试验结果表明,口服自制速溶膜剂与灌胃同剂量的苯甲酸利扎曲普坦溶液具有相似的药动学性质,本品的相对生物利用度为(97.5±11.4)%。
Tensile properties and dissolution time were used as indexes to screen the prescription. The instant film of rizatriptan benzoate with polyvinyl alcohol (PVA) and corn starch as film-forming materials was prepared and evaluated in vitro and in vivo. Different methods were used to determine the melting time, the results show that the dissolution in vitro quickly, and Beagle dog mouth in 20 s completely dissolved. In vitro dissolution characteristics were determined by paddle method and leaking trough dissolution method. The results showed that the dissolution rate was more than 80% at 40-45 s and completely dissolved within 1 min. In view of the unique nature of the film, it is more scientific to evaluate the dissolution performance of the instant film by the dissolution rate, in which the reproducibility of the grooved dissolution method is better and the distinction is greater, which is suitable for evaluating the dissolution performance of the film in vitro. Beagle dog pharmacokinetic test results show that oral self-made instant film and gavage with the same dose of rizatriptan benzoate solution has similar pharmacokinetic properties, the relative bioavailability of this product was (97.5 ± 11.4) %.