Abstract:
In Part 1, we have introduced expandable gastroretentive fibrous dosage forms for prolonged delivery of sparingly-soluble tyrosine kinase inhibitors. The expansion rate, post-expansion mechanical strength, and drug release rate were modeled for a dosage form containing 200 mg nilotinib. In the present part, the dosage form was prepared and tested in vitro to validate the models. Upon immersing in a dissolution fluid, the fibrous dosage form expanded at a constant rate to a normalized radial expansion of 0.5 by 4 h, and then formed an expanded viscoelastic mass of high strength. The drug was released at a constant rate over a day. For comparison, a particle-filled gelatin capsule with the same amount of nilotinib disintegrated almost immediately, and released eighty percent of the drug content in just 10 min. The experimental data validate the theoretical models of Part 1 reasonably.
摘要:
在第1部分中,我们介绍了可扩展的胃滞留纤维剂型,用于延长微溶的酪氨酸激酶抑制剂的递送。膨胀率,膨胀后机械强度,对含有200mg尼洛替尼的剂型的药物释放速率进行建模。在本部分,制备剂型并进行体外测试以验证模型。浸入溶解液中后,纤维剂型以恒定速率膨胀到0.5x4h的归一化径向膨胀,然后形成高强度的膨胀粘弹性块。药物在一天内以恒定速率释放。为了比较,含有等量尼洛替尼的颗粒填充明胶胶囊几乎立即崩解,并在短短10分钟内释放了80%的药物含量。实验数据合理地验证了第一部分的理论模型。