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Dissolution Enhancement of Curcumin by Solid Dispersion with Polyethylene Glycol 6000 and Hydroxypropyl Methylcellulose

机译:用聚乙二醇6000和羟丙基甲基纤维素固体分散体溶出姜黄素

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Curcumin, a polyphenolic compound derived from Curcuma longa, possesses diverse pharmacologic effects such as anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. However, curcumin has poor bioavailability and low dissolution rate due to poor absorption, rapid metabolism, and rapid systemic elimination. The aim of the study was to improve the solubility and dissolution rate of curcumin by solid dispersions. Polyethylene glycol (PEG 6000) and swellable polymers such as hydroxylpropyl methylcelluloses (HPMCs) and polyethylene oxide (PEO), were applied to improve dissolution and oral absorption of curcumin. The solid dispersions (SDs) in different ratios were prepared by hot melting method. The dissolution rate of SDs was tested in simulated gastric fluid (buffer pH 1.2) and simulated intestinal fluid (buffer pH 6.8). Samples were collected at 10, 20,30, 60,90,120 minutes and replaced with an equivalent amount of fresh medium to maintain a constant dissolution volume. High-performance liquid chromatography (HPLC) method was used to determine concentration of curcumin after dissolution test The dissolution rate of curcumin was enhanced by the incorporation into hydrophilic carrier (e.g. PEG 6000, HPMC 4000, HPMC 6, and PEO). The best percentage of drug release was observed with curcumin: PEG 6000: HPMC 4000 in ratio 1:8:4. Through the selection of polymers with optimal ratio, the SDs could increase the dissolution rate of curcumin.
机译:姜黄素,从姜黄获得的多酚化合物,具有多样的药理作用,例如抗炎,抗氧化,抗增殖和抗血管生成活性。然而,姜黄素的生物利用度差且溶解速度由于吸收不良,快速代谢和快速全身消除。该研究的目的是提高通过固体分散体姜黄素的溶解度和溶出速率。聚乙二醇(PEG 6000)和可溶胀聚合物,例如羟丙基甲基纤维素(的HPMC)和聚环氧乙烷(PEO),分别适用于改进的溶解和姜黄素的口服吸收。以不同比例的固体分散体(SDS)通过热熔融法来制备。 SDS的溶出率在模拟胃液(缓冲液pH 1.2)和模拟肠液(缓冲液pH 6.8)进行了测试。将样品在10,20,30,60,90,120分钟收集并用,以保持恒定溶解体积的新鲜培养基的等量替换。使用高效液相色谱法(HPLC)法溶出试验姜黄素的溶解速率通过掺入亲水性载体(例如PEG 6000,HPMC 4000,HPMC 6,和PEO)增强后,以确定姜黄素浓度。观察到药物释放的百分比最好姜黄素:PEG 6000:HPMC 4000在比为1:8:4。通过聚合物的选择具有最佳比例,SDS可以增加姜黄素的溶解速率。

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