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壳聚糖共晶体包埋的海藻酸钠微球用于提高醋氯芬酸的溶解度和生物利用度。

Chitosan cocrystals embedded alginate beads for enhancing the solubility and bioavailability of aceclofenac.

作者信息

Ganesh Mani, Jeon Ung Jin, Ubaidulla Udhumansha, Hemalatha Pushparaj, Saravanakumar Arthanari, Peng Mei Mei, Jang Hyun Tae

机构信息

Department of Chemical Engineering, Hanseo University, 360 Daegok-ri, Haemi-myun, Seoson-Si 356706, Chungcheongnam-do, Republic of Korea.

Department of Chemical Engineering, Hanseo University, 360 Daegok-ri, Haemi-myun, Seoson-Si 356706, Chungcheongnam-do, Republic of Korea.

出版信息

Int J Biol Macromol. 2015 Mar;74:310-7. doi: 10.1016/j.ijbiomac.2014.12.038. Epub 2014 Dec 31.

Abstract

Enhanced oral bioavailability of aceclofenac has been achieved using chitosan cocrystals of aceclofenac and its entrapment into alginate matrix a super saturated drug delivery system (SDDS). Prepared SDDS were evaluated by various physiochemical and pharmacological methods. The result revealed that the primary cocrystals enhanced the solubility of the drug and the thick gelled polymer matrix that formed from swelling of calcium alginate beads makes it to release the drug in continuous and sustained manner by supersaturated drug diffusion. The Cmax, Tmax and relative bioavailability for aceclofenac cocrystal and aceclofenac SDDS were 2.06±0.42 μg/ml, 1 h, 159.72±10.84 and 2.01 μg/ml, 1 h, 352.76±12.91, respectively. Anti-inflammatory activity of aceclofenac was significantly improved with the SDDS. With respect to the results, it revealed that the SDDS described herein might be a promising tool for the oral sustained release of aceclofenac and likely for that of various other poorly soluble drugs.

摘要

通过醋氯芬酸壳聚糖共晶体及其包封于藻酸盐基质(一种超饱和药物递送系统,SDDS)中,已实现醋氯芬酸口服生物利用度的提高。通过各种物理化学和药理学方法对制备的SDDS进行了评估。结果表明,初级共晶体提高了药物的溶解度,由海藻酸钙珠粒溶胀形成的厚凝胶聚合物基质使其通过超饱和药物扩散以持续和缓释的方式释放药物。醋氯芬酸共晶体和醋氯芬酸SDDS的Cmax、Tmax和相对生物利用度分别为2.06±0.42μg/ml、1小时、159.72±10.84和2.01μg/ml、1小时、352.76±12.91。SDDS显著提高了醋氯芬酸的抗炎活性。根据结果,本文所述的SDDS可能是醋氯芬酸口服缓释以及其他各种难溶性药物口服缓释的一种有前景的工具。

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