含有抗病毒药物的浮动给药系统(fdds)的制备与评估

Teena Mohan, Mariya Sunny, Manju Maria Mathews, B. R
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摘要

抗病毒药物阿昔洛韦的口服生物利用度较低,约为 15-30%。它在上消化道的吸收率更高。研究的主要目的是评估海藻酸浮珠作为阿昔洛韦药物载体的潜力,以延长药物在胃吸收窗口的停留时间。浮珠由含有 CaCO3 作为气体形成剂的海藻酸钠溶液通过离子凝胶法制备而成。为了克服制备过程中药物浸出的限制,并改善持续释放特性,在制备海藻酸钠珠时添加了羟丙基甲基纤维素(HPMC K4M)、Eudragit RL 100 和黄原胶等聚合物。还使用含有交联溶液的果胶(聚电解质)制备了珠子。通过傅立叶变换红外光谱研究证实了药物与聚合物的相容性。为了了解在海藻酸盐溶液中添加这些聚合物和在交联溶液中添加果胶的效果,对制备的珠子进行了药物负载百分比、夹持效率、表面形态和体外释放特性评估。用黄原胶和果胶制备的果胶处理珠不仅显示出更高的药物负载百分比,而且在 pH 值为 1.2 时显示出持续的药物释放。因此,这些海藻酸浮珠可以作为阿昔洛韦的载体,提高其口服生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Preparation and evaluation of floating drug delivery system (fdds) containing an antiviral drug
Acyclovir, an antiviral drug has low oral bioavailability of about 15-30%. It shows more absorption in the upper gastro intestinal tract. The main objective is to evaluate the potential of floating alginate beads as a drug carrier for acyclovir to prolong gastric residence time of drug in its absorption window. Floating beads were prepared from sodium alginate solution containing CaCO3 as gas-forming agent using Ionotropic gelation method. To overcome the limitation of drug leaching during preparation and to have improved sustained release characteristics, alginate beads were prepared with the addition of polymers like Hydroxy propyl methyl cellulose (HPMC K4M), Eudragit RL 100 and Xanthan gum. Beads were also prepared by using Pectin (polyelectrolyte) containing cross linking solution. The compatibility of drug with the polymer was confirmed through the FT-IR studies. The prepared beads were evaluated for percentage drug loading, entrapment efficiency, surface morphology and in vitro release characteristics to know the effect of addition of these polymers to alginate solution and the addition of Pectin to cross linking solution. Pectin treated beads prepared with Xanthan gum & Pectin not only showed improved percentage drug loading but also exhibited sustained drug release in the pH 1.2. So these floating alginate beads may act as a promising carrier for acyclovir to improve its oral bioavailability.
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