Salatin Sara, Tarzamani Mina, Farjami Afsaneh, Jelvehgari Mitra
Neurosciences Research Center (NSRC), Tabriz University of Medical Sciences, Tabriz, Iran.
Faculty of pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
Ther Deliv. 2022 Feb;13(2):95-108. doi: 10.4155/tde-2021-0069. Epub 2022 Feb 7.
Sumatriptan (ST) is used for the treatment of migraine and cluster headaches. However, it exhibits low oral bioavailability (15%) due to the high first-pass metabolism. The aim of this work was to formulate an ST rectal hydrogel. Hydrogels were formulated according to a Box-Behnken design using pluronic F-127 (PF-127) and chitosan as thermogelling and mucoadhesive agents, respectively. The rectal permeability was examined using a sheep rectal mucosa. Among all the formulations, the hydrogel S2 showed satisfactory drug content (4.50%), gelling temperature (32°C), pH (6.41), viscosity (105 cP) and strength (15.90 sec). Mucoadhesive strength was adequate to provide a prolonged residence time. The flux of hydrogel S2 was calculated to be 0.0003 μg/cm.min. The ST hydrogel can provide a potential opportunity to overcome the first pass metabolism and reduce drug dose.
舒马曲坦（ST）用于治疗偏头痛和丛集性头痛。然而，由于首过代谢率高，其口服生物利用度较低（15%）。本研究的目的是制备一种ST直肠水凝胶。采用Box-Behnken设计，分别以泊洛沙姆F-127（PF-127）和壳聚糖作为热凝胶剂和黏膜黏附剂来制备水凝胶。使用绵羊直肠黏膜检测直肠通透性。在所有制剂中，水凝胶S2显示出令人满意的药物含量（4.50%）、胶凝温度（32℃）、pH值（6.41）、粘度（105厘泊）和强度（15.90秒）。黏膜黏附强度足以提供较长的停留时间。计算得出水凝胶S2的通量为0.0003μg/cm·min。ST水凝胶可为克服首过代谢和降低药物剂量提供潜在机会。
