Satishbabu B K, Sandeep V R, Ravi R B, Shrutinag R
Department of Pharmaceutics, National College of Pharmacy, Balraj Urs Road, Shimoga - 577 201, India.
Indian J Pharm Sci. 2010 Nov;72(6):738-44. doi: 10.4103/0250-474X.84583.
A multiple unit oral floating drug delivery system of famotidine was developed to prolong gastric residence time, target stomach mucosa and increase drug bioavailability. Drug and polymer compatibility was studied by subjecting physical mixtures of drug and polymers to differential scanning calorimetry. Cod liver oil entrapped calcium alginate beads containing famotidine, capable of floating in the gastric condition were formulated and evaluated. The gel beads were prepared by emulsion gelation method by employing sodium alginate alone and mixture of sodium alginate and hydrophilic copolymers such as carbopol 934P and hydroxypropylmethylcellulose K15M grade in three different ratios. The effect of selected factors, such as percentage of oil and amount of copolymers on floating properties was investigated. The beads were evaluated for percent drug loading, drug entrapment efficiency, buoyancy and in vitro drug release. The in vitro drug release study of the beads was carried out in simulated gastric media employing a modified Rosette-Rice test apparatus. Wherein, the apparatus was further modified by incorporating a water jacket to the apparatus to circulate hot water to maintain 37±2° for throughout the release study. All the oil entrapped calcium alginate beads floated if a sufficient amount of oil was used. Beads formulated employing sodium alginate alone could not sustain the drug release up to 8 h, whereas beads formulated with mixture of sodium alginate and copolymers demonstrated sustained release of famotidine up to 8 h. The results suggested that cod liver oil entrapped calcium alginate beads were promising as a carrier for intragastric floating drug delivery of famotidine.
开发了一种法莫替丁的多单元口服漂浮药物递送系统，以延长胃滞留时间、靶向胃黏膜并提高药物生物利用度。通过对药物和聚合物的物理混合物进行差示扫描量热法研究药物与聚合物的相容性。制备并评估了包载法莫替丁且能够在胃部环境中漂浮的鱼肝油包封海藻酸钙珠。凝胶珠通过乳液凝胶法制备，分别单独使用海藻酸钠以及将海藻酸钠与亲水性共聚物（如卡波姆934P和羟丙基甲基纤维素K15M级）按三种不同比例混合。研究了所选因素（如油的百分比和共聚物的用量）对漂浮性能的影响。对珠子的载药量百分比、药物包封率、浮力和体外药物释放进行了评估。珠子的体外药物释放研究在模拟胃液介质中使用改良的玫瑰花瓣 - 赖斯试验装置进行。其中，该装置通过在其内部加入水套来循环热水以在整个释放研究过程中保持37±2℃而进一步改进。如果使用足够量的油，所有包油的海藻酸钙珠都会漂浮。单独使用海藻酸钠制备的珠子不能将药物释放维持8小时，而用海藻酸钠和共聚物混合物制备的珠子显示法莫替丁可持续释放长达8小时。结果表明，鱼肝油包封的海藻酸钙珠有望作为法莫替丁胃内漂浮药物递送的载体。
