体外药物模型中阿托伐他汀在壳聚糖上的吸附研究

IF 0.8 Q4 MATERIALS SCIENCE, BIOMATERIALS
J. Meler, B. Grimling, M. Szcześniak, B. Karolewicz, Paweł Biernat
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引用次数: 0

摘要

在特定疾病的药理学治疗过程中,使用的药物与其他制剂或食物可以建立联系,在许多情况下改变甚至阻断其作用。另一方面,使用不合适的聚合物作为赋形剂可能导致药物-聚合物不相容。相互作用主要由吸附现象的发生和降低药物作用的复杂键的形成组成,这是特别重要的。本研究的目的是调查活性物质阿托伐他汀是否与含有壳聚糖的膳食补充剂不相容。使用药物胃肠道的静态模型,在通常以单剂量摄入的浓度范围内检查药物的吸附现象。结合药物量测定结果确定平均吸附药物剂量百分比。研究结果证明,抗胆碱酯酶药物在使用的pH范围内是吸附在壳聚糖上的,并且结合能力取决于壳聚糖的品种,间接影响反应的环境。结果表明,不同壳聚糖的平均吸附量在38% ~ 86%之间。壳聚糖的化学性质可以解释其在pH 6.4时的最低吸附值,壳聚糖仅在pH >6.7时才显示电荷。在这种条件下,与弱酸的愈合物质有关的静电吸附现象可能发生。当pH值高于7.6时,壳聚糖的平均吸收率为38% ~ 86%,与肠液填充的肠道相对应。当pH值从7.6增加到8.0时,抗胆碱酯酶药物在聚合物上的吸附量增加,这可以解释为壳聚糖的溶胀特性随着pH值的增加而增加,从而使聚合物的比表面积和吸附能力增加。基于以上考虑,可以得出结论,所研究的药物与聚合物之间存在拮抗相互作用,这涉及到从该基团中吸附药物在聚合物(壳聚糖)上并降低其生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
ATORVASTATIN ADSORPTION STUDIES ON CHITOSANS IN AN in vitro PHARMACEUTICAL MODEL
During the pharmacological therapy of specific diseases, drugs are used which, with other preparations or foods, can create connections, in many cases changing or even blocking their action. On the other hand, the use of unsuitable polymers as excipients may result in drug-polymer incompatibilities. Interactions consisting mainly of the occurrence of the adsorption phenomenon and on the formation of complex bonds that reduce the effect of the drugs are of particular importance. The aim of the study was to investigate whether the active substance atorvastatin is incompatible with dietary supplements containing chitosan. The phenomenon of the adsorption of the drug was examined using a static model of a pharmaceutical gastrointestinal tract, in the concentration range generally ingested in a single dose. Measurement results of the amount of bound drug were used to determine the average percentage of adsorbed drug dose. The results of the study prove that the anticholinesterase drug is adsorbed on chitosan in the pH ranges used, and that the binding capacity depends on the chitosan variety, which indirectly affects the reaction of the environment. It was observed that the average size of sorption depending on the chitosan variety ranged from 38% to 86%. The fact that the lowest value of adsorption was at pH 6.4 can be explained by the chemical properties of chitosan, which shows a charge only at pH >6.7. Under such conditions, the phenomenon of electrostatic adsorption may occur in relation to the healing substances of weak acids. At a pH above 7.6, corresponding to the intestinal fluid-filled intestine, the mean sorption for the highest dose of chitosan was from 38–86%. The increase in the adsorbed amount of anticholinesterase drugs on the polymer along with the increase in pH from 7.6 to 8.0 can be explained by the chitosan swelling properties, which increase with an increase in the pH. As a result, the specific surface area of the polymer and its sorption capacity increase. Based on the above considerations, it can be concluded that there is an antagonistic interaction between the drug and the polymer studied, which involves the adsorption of a drug from this group on the polymer (chitosan) and a decrease in its bioavailability.
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来源期刊
CiteScore
1.10
自引率
16.70%
发文量
19
期刊介绍: Progress in the Chemistry and Application of Chitin and its Derivatives is an annual journal focused on all aspects of production, modification, enzymology and application of chitin and its many derivatives, including chitosan. The journal publishes full-length papers as well as invited reviews. To be considered, papers must present original research that has not been published or accepted for publication elsewhere. The language of the journal will be English.
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