秋葵胶固体分散体对阿托伐他汀溶解度影响的体内外评估

Raja Y. Alghadi, Abdel Kareem M. Abdel Kareem, Alaa Balla Suliman Abuelrakha, Mohammed O. Alqamar, Banan A. Ibrahim
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引用次数: 0

摘要

背景阿托伐他汀是 BCS 二类药物,属于降血脂药物。秋葵胶(OKG)取自秋葵的荚果,是一种天然产品,含有聚合物,与合成聚合物相比,它具有安全、化学惰性、无刺激性、可生物降解等优点,而且不需要进行毒理学研究。目的:本研究旨在评估秋葵胶固体分散体对阿托伐他汀溶解度的影响。方法:采用热水提取法提取秋葵胶:采用热水提取法提取秋葵胶,并对干提取物的实用率、流动性、pH 值和傅立叶变换红外光谱进行评估。然后用溶剂蒸发法从 OKG 和羟丙基甲基纤维素(HPMC)中制备不同药物与聚合物比例的固体分散体。对制备的固体分散体、物理混合物和阿托伐他汀进行饱和溶解度测试。用饱和溶解度最高的固体分散体制备片剂,然后对片剂进行测试和评估。最后,使用瑞士白化小鼠进行体内试验,并使用单向 Anova 检验和 T 检验对数据进行分析。结果阿托伐他汀在所制备的固体分散体中的含量为 99.9%-100.1%,片剂显示出令人满意的理化特性,如片剂重量变化的 RSD 为 1.29%,崩解时间为 24 分钟,硬度为 5.24±0.457,OKGSD 片剂显示出持续释放方式,87% 的药物在 6 小时内释放。血脂分析结果显示,使用 OKGSD 片剂后,总胆固醇水平明显下降,低密度脂蛋白也明显下降。结论结论认为,OKG 是一种很有前景的辅料,可用于剂型配方中以提高低溶解度药物的溶解度。
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In vitro and In vivo Assessment of the Effect of Okra Gum Solid Dispersion in Atorvastatin Solubility
Background: Atorvastatin is BCS class II drug; it is lipid-lowering medication. Okra gum (OKG), from the pods of Abelmoschus esculentus, is natural product contain polymers having advantages over synthetic ones as it is safe, chemically inert, nonirritant, biodegradable, and does not require toxicological studies. Aim: This study aimed to assess the effect of okra gum solid dispersion in atorvastatin solubility. Method: The gum was extracted by hot water extraction and the dry extract was evaluated for percentage practical yield, flow properties, pH values and FTIR spectroscopy. Then solid dispersions with different drug to polymer ratios were prepared from OKG, and hydroxy propyl methyl cellulose (HPMC) by solvent evaporation method. Saturation solubility was tested for the solid dispersions prepared, the physical mixtures and atorvastatin. Tablets were prepared from solid dispersions with the highest saturation solubility, then tablets were tested and evaluated. Finally, in vivo test was done using Swiss albino mice and data were analyzed using one way Anova test followed by T test. Results: The content percent of atorvastatin in the solid dispersion prepared were 99,9- 100.1%, the tablets showed satisfactory physicochemical properties as 1.29% RSD in tablet weight variation, 24 min disintegration time, 5.24±0.457 Hardness and OKGSD tablets showed sustained release manner and 87% of drug released in 6 hrs. Lipid profile results showed significant decrease in total cholesterol level with marked decrease in LDL when using OKGSD tablets. Conclusion: It was concluded that OKG is promising excipient that can be used in dosage forms formulation to enhance solubility of low soluble drugs.
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