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从壳聚糖和氧化魔芋葡甘露聚糖的基质聚合物中控制释放双氯芬酸。

Controlled release of diclofenac from matrix polymer of chitosan and oxidized konjac glucomannan.

机构信息

Department of Chemistry, Faculty of Science, Chulalongkorn University, 254 Phayathai Road, Bangkok 10330, Thailand.

出版信息

Mar Drugs. 2011;9(9):1649-1663. doi: 10.3390/md9091649. Epub 2011 Sep 23.

DOI:10.3390/md9091649
PMID:22131963
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3225940/
Abstract

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).

摘要

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）。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6da5/3225940/9feb45690dd8/marinedrugs-09-01649f7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6da5/3225940/ed0c5d681758/marinedrugs-09-01649f8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6da5/3225940/e3ceb9221205/marinedrugs-09-01649f9.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6da5/3225940/733d77451d66/marinedrugs-09-01649f12.jpg

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