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PH RESPONSIVE PALAM-G-PIPA MICROSPHERES - PREPARATION AND DRUG RELEASE

机译:PH响应性PALAM-G-PIPA微球-制备和药物释放

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Poly(N-isopropylacrylamide) (PIPA) was synthesized by radical polymerization with 2,2'-azobisisobutyronitrile (AIBN) as an initiator and 3-mercaptopropionic acid (MPA) as a chain-transfer reagent in methanol (MeOH) at 70 degrees C for 7 h. The resultant PIPA was grafted to polyallylamine hydrochloride (PAlAm.HCl) by amide formation under the influence of water-soluble carbodiimide 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC). The graft polymer was made into microspheres (MS) by chemical crosslinking. The pH-responsive drug release of the graft polymer microspheres was examined by releasing phenobarbital natrium (PN), which was carried on the microspheres by physical adsorption. A dynamic dialysis technique was used in the drug-release experiment and the drug-release-rate constants reflecting the drug release characteristic of polymer microspheres were obtained by constituting a mathematical model. The results indicated that the homopolymer PAlAm microspheres and the copolymer PAlAm-g-PIPA microspheres are both pH responsive to release PN and that in the neutral pH condition the release rate is the slowest. (C) 1995 John Wiley and Sons, Inc. [References: 15]
机译:聚(N-异丙基丙烯酰胺)(PIPA)是通过在70℃于甲醇(MeOH)中以2,2'-偶氮二异丁腈(AIBN)作为引发剂和3-巯基丙酸(MPA)作为链转移剂进行自由基聚合而合成的持续7小时。在水溶性碳二亚胺1-乙基-3-(3-二甲基氨基丙基)碳二亚胺盐酸盐(EDC)的影响下,通过酰胺的形成将所得的PIPA接枝到聚烯丙胺盐酸盐(PAlAm.HCl)上。通过化学交联将接枝聚合物制成微球(MS)。通过释放苯巴比妥钠(PN)来检查接枝聚合物微球的pH响应药物释放,该苯巴比妥钠是通过物理吸附携带在微球上的。在药物释放实验中采用了动态渗析技术,并通过建立数学模型获得了反映聚合物微球药物释放特性的药物释放速率常数。结果表明,均聚物PA1Am微球和共聚物PA1Am-g-PIPA微球均对释放的PN具有pH响应,并且在中性pH条件下,释放速率最慢。 (C)1995 John Wiley and Sons,Inc. [参考:15]

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