Huanbutta Kampanart, Sittikijyothin Wancheng
Faculty of Pharmaceutical Sciences, Burapha University, 169, Saensook, Muang, Chonburi 20131, Thailand.
Faculty of Engineering, Department of Chemical Engineering, Burapha University, 169, Saensook, Muang, Chonburi 20131, Thailand.
Asian J Pharm Sci. 2018 Sep;13(5):398-408. doi: 10.1016/j.ajps.2018.02.006. Epub 2018 Mar 26.
Most seed gums have been widely used in oral and topical pharmaceutical formulations, cosmetics, and food products because of their hydrophilic properties. Gums from and seeds were chemically modified by carboxymethylation to improve their functionalities. The objective of the present study was to characterize and evaluate crude and carboxymethylated gums from and seeds to achieve the controlled-release of diclofenac sodium (DS) in matrix tablet form. Both crude and carboxymethylated gums were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy. The results revealed that the gums were successfully modified by carboxymethylation and that the modified gums were amorphous in structure and had better flow properties. The carboxymethylated gums from both plant seeds did not exhibit cytotoxicity at concentrations lower than 0.5 mg/ml. All gum samples used as polymeric controlled-release agents were formulated into DS matrix tablets. Hardness and thickness tests were conducted as in-process tests. Drug content estimation and drug release studies were carried out to evaluate the matrix tablets. Increasing the concentration of gums increased compression time and hardness while it reduced the thickness. Furthermore, the results fitted well with the Korsmeyer-Peppas model. Moreover, the DS tablets were found to release the drug by super case II transport (relaxation). In summary, the carboxymethylated gum from and seeds is an excellent, naturally sourced gum with high physicochemical and functional qualities, and can potentially be used in pharmaceutical applications as a disintegrant, diluent, and drug release-controlling agent.
由于其亲水性,大多数种子胶已广泛应用于口服和局部用药物制剂、化妆品及食品中。对[具体植物1]和[具体植物2]种子胶进行了羧甲基化化学改性以改善其功能。本研究的目的是对[具体植物1]和[具体植物2]种子的粗胶和羧甲基化胶进行表征和评价,以实现双氯芬酸钠(DS)在基质片剂中的控释。通过傅里叶变换红外光谱、X射线衍射和扫描电子显微镜对粗胶和羧甲基化胶进行了表征。结果表明,胶通过羧甲基化成功改性,改性后的胶结构为无定形,具有更好的流动性能。两种植物种子的羧甲基化胶在浓度低于0.5mg/ml时均未表现出细胞毒性。所有用作聚合物控释剂的胶样品均制成DS基质片剂。进行硬度和厚度测试作为过程中测试。进行药物含量测定和药物释放研究以评价基质片剂。增加胶的浓度会增加压制时间和硬度,同时减小厚度。此外,结果与Korsmeyer-Peppas模型拟合良好。此外,发现DS片剂通过超Ⅱ型转运(松弛)释放药物。总之,[具体植物1]和[具体植物2]种子的羧甲基化胶是一种优良的天然来源胶,具有高理化和功能品质,有潜力在药物应用中用作崩解剂、稀释剂和药物释放控制剂。