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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Formulation, In vitro and In vivo Analysis of Cyclodextrin Complexed Albendazole Composites for Enhanced Solubility
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Formulation, In vitro and In vivo Analysis of Cyclodextrin Complexed Albendazole Composites for Enhanced Solubility

机译:环糊精复合阿苯达唑复合物的配方,体外体内分析以提高溶解度

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Albendazole is a low water soluble benzimidazole carbonate drug, extensively used against instestinal parasites due to its broad spectrum activity, good tolerance and low cost. The drug has a disadvantage of poor bioavailability due to very low solubility in water. The main objective of the study was to increase the solubility and dissolution rate by complexing with cyclodextrins by kneading method and to compare the solubility between hydroxypropyl beta cyclodextrin and beta cyclodextrin. Solid state characterization was done by Fourier Transform Infrared (FTIR) and thermo gravimetric analysis. Increased solubility was obtained when more substituted cyclodextrins were used instead of non-substituted cyclodextrins. High oral dose of albendazole is required for treating systemic helminthiasis which can lead to liver impairment, so the main aim of the study was to analyze liver enzymes using albino wistar rats. For enzyme determination, blood samples were collected from each rat after 48 h of drug administration via retro-orbital puncture method and allowed to clot. From the studies it was found that elevation in liver enzymes is less in case of ABZ-HPβCD complex suspensions than the other formulations. Drug release studies and kinetic profiles help to find out the release of drug from cyclodextrins and it was found out that ABZ-HPβCD suspension having better release profile than the ABZ-βCD.
机译:阿苯达唑是一种低水溶性碳酸苯并咪唑药物,由于其广谱活性,良好的耐受性和低成本而被广泛用于抵抗肠道寄生虫。该药物由于在水中的溶解度非常低而具有生物利用度差的缺点。该研究的主要目的是通过捏合方法与环糊精复合来提高溶解度和溶解度,并比较羟丙基β-环糊精和β-环糊精的溶解度。固态表征通过傅立叶变换红外(FTIR)和热重分析完成。当使用更多取代的环糊精代替未取代的环糊精时,溶解度增加。治疗系统性蠕虫病可能导致肝功能损害,需要口服高剂量的阿苯达唑,因此该研究的主要目的是使用白化病wistar大鼠分析肝酶。为了测定酶,在给药48小时后通过眼眶后穿刺法从每只大鼠收集血样并凝结。从研究中发现,ABZ-HPβCD复合物悬浮液的肝酶升高低于其他制剂。药物释放研究和动力学特征有助于找出药物从环糊精中的释放,并且发现ABZ-HPβCD悬浮液的释放特征比ABZ-βCD更好。

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