采用直接加压技术制备尼扎替丁胃保留漂浮型生物黏附给药系统

Sravya V, S. P, Jagannath Patro V, S. Ch
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摘要

尼扎替丁是一种生物半衰期短、吸收窗窄的胃保护药物。本研究以K4M、K15M、卡波波尔934P、海藻酸钠、羧甲基纤维素钠等不同粘度的HPMC为原料,制备尼扎替丁漂浮片。直接压片的硬度、厚度、重量均匀性好,尼扎替丁均匀分布于基质浮片内。浮力研究表明,片剂的浮力可达12 h以上。其中,以HPMC K15M与Carbopol 934P比例为3:1的F12配方为理想,其浮力滞后时间小于5min,浮力持续时间大于12 h。释药时间长达12小时,具有良好的生物粘附强度。所有处方均表现出零级释放动力学,药物释放遵循非菲克扩散机制。
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Formulate gastroretentive floating bioadhesive drug delivery system of nizatidine by direct compression technique
Nizatidine is a gastroprotective drug with a short biological half-life and narrow absorption window. This study aimed at developing floating tablets of nizatidine using various HPMC viscosity grades, namely K4M, K15M, Carbopol 934P, Sodium alginate and sodium carboxy methyl cellulose. Directly compressed tablets revealed an excellent uniformity in hardness, thickness and weight and nizatidine was evenly distributed within the matrix floating tablets. Buoyancy study revealed the tablets remain buoyant for more than 12 h. Among all the formulations, F12 formulation containing 3:1 ratio of HPMC K15M and Carbopol 934P was found to be promising, which showed a floating lag time less than 5min and floating duration of more than 12 hours. It showed constant drug release up to 12 hours and good bio adhesion strength. All the designed formulations displayed zero order release kinetics and drug release follows non-Fickian diffusion mechanism.
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