...
首页> 外文期刊>International Journal of Pharmaceutical Sciences Review and Research >Formulation and Evaluation of Floating Alginate Microbeads of Hydralazine Hydrochloride
【24h】

Formulation and Evaluation of Floating Alginate Microbeads of Hydralazine Hydrochloride

机译:盐酸盐河盐藻酸盐微珠的制定与评价

获取原文

摘要

Hydralazine is a direct-acting vasodilator and has a short biological half-life (2-4 hours) due to significant first-pass metabolism with poor oral bioavailability.The aim of the current research is to reduce the frequency of dosing and enhance bioavailability to improve patient compliance by developing and systematically evaluating the sustained release of Floating alginate microbeads of Hydralazine hydrochloride.Using sodium alginate as the hydrophilic carrier in combination with different viscosity grades of HPMC such as HPMC K4M, HPMC K15M and HPMC K100M as drug release modifiers for the preparation of floating alginate microbeads of Hydralazine Hydrochloride by ionotropic gelation and cross-linking technique.Prepared beads were evaluated for percentage yield, particle size, micromeritic properties, drug entrapment efficiency, drug loading capacity, swelling ratio, in-vitro buoyancy studies, in-vitro release (in acidic buffer pH 1.2) and in-vitro release kinetic study.No significant drug-polymer interactions were observed from FT-IR studies.In fixed concentration of sodium alginate and calcium chloride and increases in the coating polymer concentration results increases in diameter of microbeads and also decrease the swelling ratio of beads.With the increase in coating polymer ratio, drug entrapment efficiency has been improved.All the formulations (F1 to F9) floated immediately or with a very short lag time and remained floating up to 12 hours.From the result of in-vitro dissolution studies reveals that the formulation F9 gave sustained release pattern of drug upto 12 hours (99.75%) and exhibited zero order kinetic followed by non-fickian diffusion transport of mechanism.Hence the formulated HPMC K100M coated sodium alginate beads can be used as an alternative and cheaper carrier for the oral controlled delivery of Hydralazine hydrochloride, especially for the treatment of congestive heart failure.
机译:氢氮嗪是一种直接作用的血管脱胆剂,并且由于具有差的口腔生物利用度的重要的首发代谢而具有短的生物半衰期(2-4小时)。目前研究的目的是降低给药频率并提高生物利用度通过开发和系统地评估盐酸盐盐藻酸盐微珠的持续释放来改善患者的顺应性。用藻酸钠与亲水载体组合的HPMC K4M,HPMC K15M和HPMC K100M相结合,作为药物释放改性剂通过离子型凝胶化和交联技术制备盐酸盐酸盐藻酸盐微珠及交联技术。评价较准备的珠粒率百分比产率,粒度,微晶特性,药物夹带效率,药物负载能力,溶胀比,体外浮力研究, - 体外释放(在酸性缓冲液pH 1.2中)和体外释放动力学研究。Noimitalan从FT-IR研究中观察到药物 - 聚合物相互作用。固定浓度的藻酸钠和氯化钙的浓度增加,涂层聚合物浓度的增加导致微珠的直径增加,并且还降低了珠粒的溶胀比。涂层聚合物的增加比例,药物滞留效率已经得到改善。所有的制剂(F1至F9)立即漂浮或具有非常短的滞后时间,并且保持漂浮至12小时。从体外溶出的结果表明,制剂F9持续存在释放药物的药物可高达12小时(99.75%)并显示出零级动力学,然后出现零级动力学,然后进行非Fickian扩散传输。因此,配制的HPMC K100M涂覆的海藻酸钠珠粒可用作口腔控制递送的替代和更便宜的载体盐酸盐,尤其是治疗充血性心力衰竭。

著录项

获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号