Department of Chemistry, Faculty of Science, Chulalongkorn University, 254 Phayathai Road, Bangkok 10330, Thailand.
Mar Drugs. 2011;9(9):1649-1663. doi: 10.3390/md9091649. Epub 2011 Sep 23.
The controlled release of diclofenac sodium (DFNa) from a chitosan-oxidized konjac glucomannan (CTS-OKG) polymer film was studied. Konjac glucomannan (KGM) was initially oxidized by sodium periodate and then cross-linked to CTS via imine bonds (-C=N-) to form the new CTS-OKG copolymer. The DFNa loaded CTS-OKG polymers were characterized by Fourier transformed infrared spectroscopy (FT-IR) and X-ray diffractometry (XRD). Finally, the release profiles of DFNa from the CTS-OKG polymer matrices were evaluated in a simulated gastrointestinal fluid system comprised of two hours in simulated gastric fluid (SGF; pH 1.2) followed by 24 h in simulated intestinal fluid (SIF; pH 7.4). A 1:2:1 (w/w/w) ratio of CTS:OKG:DFNa prepared at room temperature for 3 hours gave the highest % encapsulation efficiency (EE) of 95.6 ± 0.6 and resulted in a minimal release of DFNa (<1% over 2 h) in SGF (pH 1.2) and a significantly improved sustained release in SIF (pH 7.4) with ~6% and 19% release over 8 and 24 h, respectively), some 15- and five-fold lower than that of the two commercial DFNa preparations, Diclosian and Voltaren. This formulation may be used for further study as a long term intestine controlled release drug model (at least 3 days).
本文研究了将双氯芬酸钠(DFNa)从壳聚糖氧化魔芋葡甘聚糖(CTS-OKG)聚合物薄膜中控制释放。首先用高碘酸钠氧化魔芋葡甘聚糖(KGM),然后通过亚胺键(-C=N-)将其交联到 CTS 上,形成新的 CTS-OKG 共聚物。用傅里叶变换红外光谱(FT-IR)和 X 射线衍射(XRD)对负载 DFNa 的 CTS-OKG 聚合物进行了表征。最后,在由两小时模拟胃液(SGF;pH 1.2)和 24 小时模拟肠液(SIF;pH 7.4)组成的模拟胃肠道流体系统中评估了 CTS-OKG 聚合物基质中 DFNa 的释放曲线。在室温下制备的 CTS:OKG:DFNa 比例为 1:2:1(w/w/w),反应 3 小时,得到最高的包封效率(EE)为 95.6±0.6%,在 SGF(pH 1.2)中 DFNa 的释放最小(<1%,2 小时内),在 SIF(pH 7.4)中显著改善了持续释放,分别在 8 小时和 24 小时时释放约 6%和 19%,比两种市售的 DFNa 制剂 Diclosian 和 Voltaren 分别低 15 倍和 5 倍。该制剂可用作进一步研究的长期肠道控制释放药物模型(至少 3 天)。