替代淀粉的特性及其对含有低溶解度药物(布洛芬和硝苯地平)的胶囊体外溶解的影响

Starch Pub Date : 2024-08-14 DOI:10.1002/star.202400075
Aníbal de Freitas Santos Júnior, Carlos Magno Ramos Carvalho Junior, Gilmar Antônio Carvalho Teles Júnior, Vagner Cardoso da Silva
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引用次数: 0

摘要

研究了替代淀粉(ASs)的生物制药应用,将其作为含有低溶解度药物(硝苯地平和布洛芬)的胶囊的赋形剂,替代淀粉来自面包果(Artocarpus altilis)、红竹(Syzygium malaccense)、千层塔(Artocarpus heterophyllus Lam.)、鳄梨(Persea americana)和山药(Dioscorea spp.)的种子。通过显微镜、热和 X 射线衍射(XRD)分析对 AS 进行了表征。对溶解曲线进行了追踪,并与正式淀粉(来自玉米)进行了比较--可溶于热水、颗粒大小(2-32 微米)和直链淀粉/支链淀粉比率(0.29-0.33)。显微镜分析显示,AS 颗粒呈四面体和球形/圆形(平均大小为 21.45 微米)。AS的直链淀粉/支链淀粉比率分别为:面包果(0.29-0.37)、红竹(0.25-0.29)、千层塔(0.28-0.37)、鳄梨(0.33-0.43)和山药根茎(0.37-0.47)。热分析表明,脱水时的质量损失为 303 和 373 K(30 和 100 °C),降解时的质量损失为 525 和 626 K(252 和 353 °C)。硝苯地平(≥80%,20 分钟内)和布洛芬(≥60%,30 分钟内)的释放与玉米淀粉相似或更佳。只有从鳄梨种子中提取的 AS 无法释放硝苯地平。这项研究有助于药品和替代生物制品的质量控制。
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Characterization of Alternative Starches and Its Effects on the In Vitro Dissolution of Capsules Containing Low Solubility Drugs (Ibuprofen and Nifedipine)
Biopharmaceutical applications of alternative starches (ASs), as excipients in capsules containing low solubility drugs (nifedipine and ibuprofen), from seeds of breadfruit (Artocarpus altilis), red‐jambo (Syzygium malaccense), jackfruit (Artocarpus heterophyllus Lam.), avocado (Persea americana), and yam rhizomes (Dioscorea spp.), are investigated. ASs are characterized by microscopic, thermal, and X‐ray diffraction (XRD) analysis. Dissolution profiles are traced and compared to the official starch (from corn) – soluble in hot water, particle size (2–32 µm) and amylose/amylopectin ratio (0.29–0.33). Microscopy analysis shows AS granules with tetrahedral and spherical/rounded shapes (average size of 21.45 µm). The amylose/amylopectin ratios of AS are: breadfruit (0.29–0.37), red‐jambo (0.25–0.29), jackfruit (0.28–0.37), avocado (0.33–0.43), and yam rhizomes (0.37–0.47). AS presents crystallinity patterns of types A, B, and C. Thermal analysis shows mass loss with dehydration – 303 and 373 K (30 and 100 °C) and degradation 525 and 626 K (252 and 353 °C). The release of nifedipine (≥80%, in 20 min) and ibuprofen (≥60%, in 30 min) are similar or superior to corn starch. Only AS obtained from avocado seeds fails to release nifedipine. This study contributes to the quality control of medicine and alternative bioproducts.
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