天然高分子外用凝胶的体外评价

L. Kumar, R. Verma
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引用次数: 133

摘要

尼美舒利是第二代非甾体类抗炎药,广泛用于类风湿性关节炎的长期治疗,减轻疼痛和炎症。但是它的半衰期很短(只有3-4小时),所以它会引起更多的波动。口服尼美舒利后引起心脏灼热、恶心、运动松弛、瘙痒等。本研究基于尼美舒利生物黏附外用凝胶的制备,以避免所有的胃部副作用。采用天然高分子凝胶法制备外用生物胶。生物胶粘剂聚合物是增加制剂与生物膜接触,避免制剂波动,表现为缓释制剂的药剂。本研究通过药物含量、铺展性、挤压性、溶胀指数、体外药物扩散研究、体外药物释放动力学研究和离体生物黏附测量等参数对制备的生物黏附外用凝胶进行评价。通过体外药物扩散研究和凝胶的离体生物黏附性能测定,我们认为天然高分子凝胶蜜瓜是制备生物黏附缓释外用凝胶的最佳聚合物。关键词:外用凝胶;辅料;天然聚合物
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In vitro evaluation of topical gel prepared using natural polymer
Nimesulide is a second generation non–steroidal anti–inflammatory agent, which is widely used in the long term therapy of rheumatoid arthritis, in alleviating pain and inflammation. But its short half-life (only 3–4 hr), so its causes more fluctuation. After oral administration Nimesulide causes to produces heart burn, nausea, loose motions, pruritus, etc. The present study based on the preparation of bioadhesive topical gel of Nimesulide, so as to avoid all gastric side effects. For the preparation of bioadhesive topical gel natural polymer aegel marmelos (plant Bale) was used. Bioadhesive polymers are the agents which increases the contact between the formulation and biological membrane, so as to avoid the fluctuation of formulation and behave as a sustained release formulation. In the present study, prepared bioadhesive topical gel was evaluated with the help of different parameters like drug content, spreadability, extrudability, swelling index study, in–vitro drug diffusion study, in-vitro drug release kinetic study and ex–vivo bioadhesive measurement. On the basis of in–vitro drug diffusion study and ex–vivo bioadhesive measurement property of gel, we have concluded that natural polymer aegel marmelos is the best polymer for the preparation of sustained release bioadhesive topical gel. Keywords: Topical gel; Bioadhesion; Natural polymer
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