姜黄素漂浮片的研制与评价

Kishor A. Bellad, B. Nanjwade, Arindam Sarkar, T. Srichana, Roopali M. Shetake
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引用次数: 1

摘要

本研究首先采用热熔挤压机将抗炎药姜黄素与溶液配合,提高姜黄素的溶解度,并采用直接加压法制备浮片。以不同等级的羟丙基甲基纤维素(HPMC)聚合物和碳酸氢钠为气体发生剂配制片剂。进行了预配制和微粒试验。对所制备的浮片进行了理化性质、体外释放度、体内漂浮性能、药代动力学和稳定性研究。配方在厚度(5.11至5.27 mm)和硬度(4.4至4.8 kg/cm2)方面是均匀的。易碎度(0.27 ~ 0.53%)、重量变异度(1.28 ~ 1.89%)、药物含量(97.84 ~ 99.46%)。HPMC溶胀指数的大小顺序为K100M > K15M > K4M。发现碳酸氢钠浓度为16% w/w时足以获得浮力。浮力滞后时间均小于1分钟。不同配方的总漂浮时间在12 ~ 24小时之间。优化后的配方F4和F6在20和24 h时的释药率分别为98.85%和98.10%。体内漂浮研究通过x射线成像显示片剂在胃中漂浮。药代动力学研究表明,Cmax-260 ng/ml, Tmax-12 h, AUC -738.33 ng/hr/ml, Kel为0.061,t1/2为11.36 h。FT-IR, XRD和DSC研究表明药物与聚合物之间没有化学相互作用。在稳定期,所选片剂的漂浮行为和药物释放特性均稳定。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and Evaluation of Curcumin Floating Tablets
In the present study, curcumin an anti-inflammatory agent, was first complexed with the soluplus by hot melt extrusion machine to enhance the solubility of curcumin and was formulated into floating tablets by direct compression method. Tablets were formulated using various grades of Hydroxypropyl methylcellulose (HPMC) polymers and sodium bicarbonate as gas generating agent. Preformulation and micromeritic studies were performed. The floating tablets were evaluated for their physico-chemical properties, in-vitro release, in-vivo floating property, pharmacokinetic and stability studies. Formulations were found uniform with respect to thickness (5.11 to 5.27 mm) and hardness (4.4 to 4.8 kg/cm2). The friability (0.27 to 0.53 %), weight variation (1.28-1.89%) and Drug content (97.84 to 99.46 %). The order of swelling index of HPMC was found to be K100M > K15M > K4M. Sodium bicarbonate at the concentration of 16% w/w was found to be sufficient in attaining the buoyancy. The buoyancy lag time was found to be less than 1 minute for all the prepared tablets. The total floating time for different formulations was in the range of 12-24 hours. The optimized formulation F4, and F6 showed 98.85 and 98.10 % drug release at the end of 20 and 24 hrs respectively. The in-vivo floating study was carried out by X-ray imaging showed floating of the tablet in the stomach. The pharmacokinetic study showed, Cmax-260 ng/ml, Tmax-12 hrs, AUC -738.33 ng/hr/ml Kel as 0.061 and t1/2 was found to be 11.36 hrs. FT-IR, XRD and DSC studies revealed no chemical interaction between drug and polymers. During the stability period selected tablets were found to be stable with respect to floating behaviour and drug release characteristics.
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