Kittipongpatana Ornanong S, Kittipongpatana Nisit
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai 50200, Thailand.
Lanna Rice Research Center, Chiang Mai University, Chiang Mai 50100, Thailand.
Polymers (Basel). 2022 Mar 23;14(7):1298. doi: 10.3390/polym14071298.
Starch extracted from KJ CMU-107 rice, with amylose content of 13.4%, was modified to yield pre-gelatinized starch (PGS), carboxymethyl starch (CMS), crosslinked carboxymethyl starch (CLCMS), crosslinked starch (CLS), and hydroxypropyl starch (HPS). Their physicochemical properties were assessed in comparison with the native starch (NS), and their functional properties were then evaluated for potential use as pharmaceutical excipients. Scanning electron microscopic (SEM) images and X-ray diffraction (XRD) patterns showed that granules of all but one of the modified starches retained the native character and crystalline arrangement. The exception, PGS, exhibited extensive granular rupture, which correlated with the loss of crystallinity suggested by the amorphous halo in XRD. Energy-dispersive X-ray (EDX) data confirmed the modification by the presence of related elements. Carboxymethylation increased solubility in unheated water, while crosslinking improved swelling. All modified starches displayed improved oil absorption capacity by 17-64%, while CMS and CLCMS also exhibited significant moisture sorption at above 75% RH PGS and HPS exhibited lower gelatinization temperature (Tg) and enthalpic change (ΔH), while CLS showed higher Tg and ΔH. CMS, CLCMS, and CLS showed adequate powder flow and compactibility, qualifying as potential tablet excipients. The 5% / solutions of CMS, CLMS, and HPS also formed intact films with suitable tensile strength. Overall, modified starches derived from KJ CMU-107 could potentially be developed into new pharmaceutical excipients.
从直链淀粉含量为13.4%的KJ CMU - 107大米中提取的淀粉，被改性制成预糊化淀粉（PGS）、羧甲基淀粉（CMS）、交联羧甲基淀粉（CLCMS）、交联淀粉（CLS）和羟丙基淀粉（HPS）。将它们的理化性质与天然淀粉（NS）进行比较评估，然后评估它们作为药物赋形剂的潜在功能性质。扫描电子显微镜（SEM）图像和X射线衍射（XRD）图谱显示，除一种改性淀粉外，其他改性淀粉颗粒均保留了天然特性和晶体排列。例外的是PGS，其颗粒出现大量破裂，这与XRD中非晶晕所表明的结晶度丧失相关。能量色散X射线（EDX）数据通过相关元素的存在证实了改性。羧甲基化提高了在未加热水中的溶解度，而交联改善了膨胀性。所有改性淀粉的吸油能力提高了17 - 64%，而CMS和CLCMS在相对湿度高于75%时也表现出显著的吸湿作用。PGS和HPS的糊化温度（Tg）和焓变（ΔH）较低，而CLS的Tg和ΔH较高。CMS、CLCMS和CLS表现出足够的粉末流动性和可压性，有资格作为潜在的片剂赋形剂。CMS、CLMS和HPS的5%溶液也形成了具有合适拉伸强度的完整薄膜。总体而言，源自KJ CMU - 107的改性淀粉有可能被开发成新型药物赋形剂。
