Preparation and evaluation of oral capsules containing apigenin nanocrystals prepared by ultrasonication

Mahmood A. Haiss, Nidhal K. Maraie
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引用次数: 1

Abstract

This work aims to enhance dissolution rate, increase absorption and bioavailability of Apigenin by formulating it as nanocrystal suspension employing ultrasonic technology. Two different diluents; (5%, 10%) microcrystalline cellulose (MCC) and (2%, 3%) anhydrous lactose were used to prepare hard gelatin capsules for two optimum types for apigenin nanocrystals prepared in our laboratory utilizing ultrasonication technique using 1% tween 80 (F6) and 2% poloxamer 188 (F20). The results showed that the marketed capsules (containing MCC) had about half the dissolution rate than all the prepared nanocrystals capsules formulas, and the nanocrystals prepared with poloxamer gave 90% release within 20 minutes and 100% release with 2 hours with excellent flow properties with no effect of the added diluents while the addition of diluents improved significantly the release of nanocrystals capsules (F6) with 1% tween 80 with good flow properties. The results suggested that utilizing apigenin nanocrystals prepared by ultrasonication technique may improve drug absorption and bioavailability with a reduced required dose.
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超声法制备芹菜素纳米晶口服胶囊的制备与评价
本研究旨在利用超声技术制备芹菜素纳米晶悬浮液,提高芹菜素的溶出率、吸收率和生物利用度。两种不同的稀释剂;采用(5%,10%)微晶纤维素(MCC)和(2%,3%)无水乳糖制备硬明胶胶囊,以1%的tween 80 (F6)和2%的poloxam188 (F20)为超声技术制备了两种最佳类型的芹菜素纳米晶体。结果表明,市售微胶囊(含MCC)的溶出率约为所有制备的纳米晶胶囊配方的一半;波洛沙姆制备的纳米晶在20分钟内释放90%,2小时内释放100%,具有良好的流动性能,不受稀释剂的影响;而稀释剂的加入显著提高了1% tween 80的纳米晶胶囊(F6)的释放度,具有良好的流动性能。结果表明,利用超声技术制备的芹菜素纳米晶体可以提高药物的吸收和生物利用度,同时降低所需剂量。
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