布地奈德4种直肠给药制剂体外释放和流变学特征研究

China Pharmacist(2022)

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Abstract
目的:评价布地奈德4种直肠给药制剂的体外释放和流变学特性,预测布地奈德脂质体温敏凝胶的体内释放行为.方法:采用乙醚注入法制备脂质体,以泊洛沙姆407、泊洛沙姆188和HPMC制备布地奈德脂质体温敏凝胶,并制备布地奈德的普通灌肠剂、脂质体制剂、温敏凝胶制剂;采用改良Franz扩散池法,测定4种直肠给药制剂的体外释放参数并绘制累计释放曲线;以旋转黏度计测定不同条件下温敏凝胶和脂质体温敏凝胶的静态流变学的变化规律.结果:布地奈德脂质体温敏凝胶释药性能最好,温敏凝胶次之,脂质体和普通灌肠液释药性能较差且无显著差别;在常温下,温敏凝胶和脂质体温敏凝胶均为牛顿流体,在30~35℃时发生相变黏度上升,在体内温度、pH、电解质等条件下脂质体温敏凝胶表现更佳.结论:布地奈德脂质体温敏凝胶可充分发挥直接直肠给药的优势,可快速贴附于直肠黏膜释药,为布地奈德新型直肠用制剂的研究提供参考.
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