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使用 pH 响应型溶胀聚合物制备和评价漂浮型、脉冲型、多颗粒制剂。

Formulation and evaluation of floating, pulsatile, multiparticulates using pH-dependent swellable polymers.

机构信息

Department of Pharmaceutics, R.C. Patel College of Pharmacy, Karvand Naka, Shirpur-425405, Maharashtra, India.

出版信息

Pharm Dev Technol. 2010 Mar-Apr;15(2):209-16. doi: 10.1080/10837450903095334.

Abstract

The objective of this study was to develop a floating, pulsatile, multiparticulate drug delivery system intended for chronopharmacotherapy of arthritis. The floating pulsatile drug delivery has the advantage that a drug can be released in the upper gastrointestinal tract after a definite time period of no drug release, i.e. lag time. Cross-linked beads were prepared using low methoxylated pectin (LM104AS), sodium alginate, and low methoxylated pectin (LM104AS) along with sodium alginate by acid- base reaction during ionotropic gelation. Beads were dried in oven at 50 degrees C for 4 h. Aceclofenac was used as a model drug for encapsulation. Drug loaded multiparticulates were subjected to various characterization and evaluation parameters like entrapment efficiency, surface topography, size analysis and in vitro release study. It was found that calcium pectinate beads show maximum drug entrapment. Hence, pectin containing formulation was further studied for buoyancy, DSC and radio imaging study. Drug release study was performed in acidic environment using pH 1.2 buffer solution for 6 h and then at 7.4 pH for 60 min. The total drug release ranges from 5-10% and 90-94% in acidic and basic media, respectively.

摘要

本研究旨在开发一种用于关节炎时辰治疗的漂浮型脉冲式多颗粒给药系统。漂浮型脉冲式给药系统的优点在于,药物可以在上消化道在一定的无药物释放时间(即滞后时间)后释放。通过酸碱反应,使用低甲氧基果胶(LM104AS)、海藻酸钠和低甲氧基果胶(LM104AS)制备交联珠。珠体在 50°C 的烘箱中干燥 4 小时。醋氯芬酸被用作包封的模型药物。将载药多颗粒进行各种特性和评价参数的研究,如包封效率、表面形貌、粒径分析和体外释放研究。结果发现,果胶钙珠显示出最大的药物包封效率。因此,进一步研究了含有果胶的制剂的漂浮性、DSC 和放射性成像研究。在酸性环境中(使用 pH 1.2 缓冲溶液)进行 6 小时的药物释放研究,然后在 7.4 pH 下进行 60 分钟的药物释放研究。在酸性和碱性介质中,总药物释放范围分别为 5-10%和 90-94%。

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