一种新型瑞舒伐他汀钙牛酥油组分双形配合物:配方表征与评价

Q2 Pharmacology, Toxicology and Pharmaceutics Drug Delivery Letters Pub Date : 2021-08-31 DOI:10.2174/2210303111666210831170312
V. Suryawanshi, K. Sarwa, S. N. Sakarkar, C. Kaur
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引用次数: 0

摘要

瑞舒伐他汀钙是一类他汀类药物,其口服生物利用度有限,约为20%。这个问题可以通过使用牛酥油部分作为生物利用度增强剂来制造双形复合物来克服。采用精密的热分离技术从牛酥油中分离出不同的脂肪酸。收集的级分根据脂肪酸报告的参数进行表征。LC-MS和FTIR证实了收集的馏分中的含量变化。以一定比例的药物和牛酥油为原料,采用融合法制备了双歧杆菌复合物。对制备的配合物进行FTIR、DSC和LC-MS研究,以确认化学组成特征。还进行了药物含量、体外和离体渗透研究。使用卡拉胶爪诱导的水肿大鼠模型测量抗炎反应。还使用ELISA特异性试剂盒进行了降脂作用和炎症标志物分析。在30ºC下用热组分制备的牛酥油双形复合物显示出最高的体外和离体渗透性。双型复合物F1的抗炎反应高于具有显著的降脂和脂蛋白降低特性的其他测试制剂。本研究证实,热分离法能够根据牛酥油的脂肪酸含量对其进行分离。瑞舒伐他汀钙与牛酥油热组分的外观提高了口服生物利用度,随后具有抗炎和降脂活性。
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A novel rosuvastatin calcium cow ghee fraction biform complex: formulation characterization and evaluation
Rosuvastatin calcium is a statin class of drug having limited oral bioavailability of about 20%. This problem might be overcome by making the biform complex using cow ghee fraction as a bioavailability enhancer. A precise thermal fractionation technique was adopted to separate different fatty acids from cow ghee. Collected fractions were subjected to characterization over parameters reported for fatty acids. LC-MS and FTIR confirm the content variation in the collected fraction. Biform complex was prepared by fusion method with a constant ratio of drug and cow ghee fraction. The prepared complex was subjected to FTIR, DSC, and LC-MS study to confirm chemical composition characteristics. Drug content, in-vitro and ex-vivo permeation studies were also performed. The anti-inflammatory response was measured using the carrageenan paw-induced edema rat model. Lipid-lowering effect and inflammation marker analysis was also performed using ELISA specific kit. The biform complex prepared with a thermal fraction at 30ºC of cow ghee show the highest in-vitro and ex-vivo permeation. The anti-inflammation response of the biform complex F1 was higher than other tested formulations with considerable lipid and lipoprotein lowering properties. This study confirms that the thermal fractionation method abled to separate cow ghee as per their fatty acid content. The complexion of rosuvastatin calcium with cow ghee thermal fraction enhances oral bioavailability followed by the anti-inflammatory and lipid-lowering activity.
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来源期刊
Drug Delivery Letters
Drug Delivery Letters Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.70
自引率
0.00%
发文量
30
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