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聚合活化剂在用于热触发释放萘普生钠的N-异丙基丙烯酰胺衍生物合成过程中的应用。

Application of Polymerization Activator in the Course of Synthesis of N-Isopropylacrylamide Derivatives for Thermally Triggered Release of Naproxen Sodium.

作者信息

Gasztych Monika, Kotowska Anna, Musiał Witold

机构信息

Department of Physical Chemistry, Faculty of Pharmacy, Wroclaw Medical University, 50-556 Wroclaw, Poland.

出版信息

Materials (Basel). 2018 Feb 8;11(2):261. doi: 10.3390/ma11020261.

DOI:10.3390/ma11020261
PMID:29419767
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5848958/
Abstract

Poly--isopropylacrylamide (polyNIPA) is an extensively studied polymer in the field of controlled drug delivery. PolyNIPA contains carbonyl and amide groups along a hydrophobic chain. In an aqueous environment, crosslinked polyNIPA forms a gel characterized by a reversible volume phase transition temperature (VPTT), in response to changes in the external environment excited by the temperature factor. NIPA-based polymers were synthesized by a surfactant-free precipitation polymerization (SFPP) method at a temperature of 70 °C using the free radical initiator potassium persulfate (KPS) and at 35 °C using redox initiator system KPS with ,,','-tetramethylethylenediamine (TEMED). The synthesized products were evaluated via dynamic light scattering (DLS), nuclear magnetic resonance (NMR) and Fourier-transform infrared spectroscopy (FTIR). The chemical structure, molecular mass, and hydrodynamic diameter of obtained particles, as well as the effects of synthesized polymers on the release of the active substance, naproxen sodium (NS), from hydroxypropyl methyl cellulose (HPMC)-based hydrogels were assessed. The use of the TEMED activator affected the particle size, as well as the release kinetics of NS. The insertion of TEMED into reactant mixtures may be applied to modify the release kinetics of NS from hydrogel preparations.

摘要

聚异丙基丙烯酰胺(聚NIPA)是药物控释领域中一种被广泛研究的聚合物。聚NIPA在疏水链上含有羰基和酰胺基团。在水性环境中,交联的聚NIPA形成一种具有可逆体积相变温度(VPTT)的凝胶,以响应由温度因素激发的外部环境变化。基于NIPA的聚合物通过无表面活性剂沉淀聚合(SFPP)方法合成,在70℃使用自由基引发剂过硫酸钾(KPS),在35℃使用氧化还原引发剂体系KPS与N,N,N',N'-四甲基乙二胺(TEMED)。通过动态光散射(DLS)、核磁共振(NMR)和傅里叶变换红外光谱(FTIR)对合成产物进行评估。评估了所得颗粒的化学结构、分子量和流体动力学直径,以及合成聚合物对活性物质萘普生钠(NS)从羟丙基甲基纤维素(HPMC)基水凝胶中的释放的影响。TEMED活化剂的使用影响了颗粒大小以及NS的释放动力学。将TEMED插入反应物混合物中可用于改变NS从水凝胶制剂中的释放动力学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/e9d008e6be1c/materials-11-00261-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/273b3ff7599c/materials-11-00261-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/05890f637708/materials-11-00261-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/8b4752987581/materials-11-00261-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/dcfc3e535748/materials-11-00261-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/19618e51036c/materials-11-00261-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/e9d008e6be1c/materials-11-00261-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/273b3ff7599c/materials-11-00261-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/05890f637708/materials-11-00261-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/8b4752987581/materials-11-00261-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/dcfc3e535748/materials-11-00261-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/19618e51036c/materials-11-00261-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2615/5848958/e9d008e6be1c/materials-11-00261-g006.jpg

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