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Supercritical antisolvent coprecipitation in the pharmaceutical field: Different polymeric carriers for different drug releases
The Canadian Journal of Chemical Engineering ( IF 2.1 ) Pub Date : 2020-04-28 , DOI: 10.1002/cjce.23759
Paola Franco 1 , Iolanda De Marco 1
Affiliation  

The supercritical antisolvent process (SAS) was employed to obtain polymer/drug coprecipitated powders. Indeed, processes based on the use of supercritical fluids allow us to obtain polymer/active drug coprecipitated microparticles with tunable bioavailability. In this work, two different biocompatible polymers were selected to be used as carriers for obtaining drug microparticles with different releases for different applications: polyvinylpyrrolidone (PVP) was coprecipitated with ketoprofen to obtain a rapid drug release and zein was coprecipitated with ampicillin to obtain a controlled drug release. The experiments were performed both on a bench‐scale and a pilot‐scale plant. Ketoprofen is one of the most prescribed non‐steroidal anti‐inflammatory drugs. It is poorly soluble in water and, to overcome this inconvenience, in this work, it was coprecipitated with PVP. In correspondence with the optimized polymer/drug ratio, the dissolution rate of the active principle in the coprecipitated particles was about three times higher than the one of the unprocessed ketoprofen. The second model drug under study in this paper is ampicillin, a semi‐synthetic penicillin that is one of the most commonly prescribed broad‐spectrum antibiotics. Prolonging the release of the drug would imply a reduction in the number of administrations and, therefore, of the side effects associated with too high dosages. For this purpose, in this work, ampicillin was coprecipitated with zein. Zein/ampicillin microparticles were produced up to a polymer/drug ratio of 5/1 w/w; in this case, the antibiotic coprecipitated with zein reaches 90% of its dissolution in about 14 hours, while the unprocessed antibiotic takes about 3 hours to dissolve.

中文翻译:

制药领域的超临界抗溶剂共沉淀:用于不同药物释放的不同聚合物载体

采用超临界抗溶剂法(SAS)获得聚合物/药物共沉淀粉末。实际上,基于使用超临界流体的方法使我们能够获得具有可调生物利用度的聚合物/活性药物共沉淀微粒。在这项工作中,选择了两种不同的生物相容性聚合物作为载体,以获取具有不同用途的不同释放的药物微粒:聚乙烯吡咯烷酮(PVP)与酮洛芬共沉淀以获得快速药物释放,玉米蛋白与氨苄青霉素共沉淀以获得可控的药物释放。实验在实验室规模和中试规模上进行。酮洛芬是最处方的非甾体类抗炎药之一。它难溶于水,为了克服这种不便,在这项工作中,它与PVP共沉淀。与最佳的聚合物/药物比率相对应,活性成分在共沉淀颗粒中的溶解速率比未处理的酮洛芬之一高约三倍。本文研究的第二种模型药物是氨苄青霉素,一种半合成的青霉素,是最常用的广谱抗生素之一。延长药物的释放将减少给药次数,并因此减少与剂量过高有关的副作用。为此,在这项工作中,氨苄青霉素与玉米醇溶蛋白共沉淀。产生了玉米蛋白/氨苄青霉素微粒,其聚合物/药物比率为5/1 w / w;在这种情况下,与玉米醇溶蛋白共沉淀的抗生素在大约14小时内达到其溶出度的90%,
更新日期:2020-04-28
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