盐酸头孢吡肟缓释微球的制备与工艺优化

来源期刊:中南大学学报(自然科学版)2013年第3期

论文作者:彭东明 王春燕 刘艳飞 李永欣 苏小爱 帅海涛 盛毓

文章页码:907 - 913

关键词:盐酸头孢吡肟;O-羧甲基壳聚糖;星点设计-效应面法;缓释微球

Key words:cefepime dihydrochloride; O-carboxymethylchitosan; central composite design-response surface methodology; controlled release microspheres

摘    要:以O-羧甲基壳聚糖(OCMC)为载体、戊二醛(GA)为交联剂,采用乳化交联法制备包覆盐酸头孢吡肟(CD)的药物缓释微球。以OCMC质量分数、CD与OCMC质量比(m(CD)/m(OCMC))、交联剂用量(V(GA)/m(OCMC))及油相乳化剂Span80质量分数为自变量,以载药量和包封率为因变量,采用星点设计-效应面法优化制备工艺,并对优化后的工艺进行验证。所得最优制备条件如下:OCMC质量分数为2.7%,m(CD)/m(OCMC)为0.665,交联剂用量V(GA)/m(OCMC)为8 mL/g,Span80质量分数为4%;在最优工艺条件下制备的微球外观圆整,平均粒径为7 μm,粒度跨距为1.52,载药量和包封率分别为(21.4±0.5)%和(42.3±0.7)%,缓释时间达到10 d以上;星点设计-效应面法预测性良好。

Abstract: O-carboxymethylchitosan (OCMC) microspheres containing an antibiotic drug cefepime dihydrochloride (CD) were prepared by emulsion crosslinking using glutaraldehyde (GA). The central composite design-response surface methodology was used to optimize process variables and the optimized formulation was validated. The OCMC concentration in the aqueous phase, mass ratio of CD to OCMC (m(CD)/m(OCMC)), the dosage of crosslinker (V(GA)/m(OCMC)) and the Span80 concentration in the organic phase were listed as independent variables and the dependent variables were drug-loading and encapsulation efficiency. The results show that the optimal values are as follows: the OCMC concentration is 2.7%, m(CD)/m(OCMC) is 0.665, the dosage of crosslinker (V(GA)/m(OCMC)) is 8 mL/g, the Span80 concentration is 4%. According to these conditions, the microspheres are spherical in shape. The mean diameter of the microspheres is 7 μm and the span is 1.52. The drug loading and drug encapsulation efficiency of CD-loaded microspheres are (21.4±0.5)% and (42.3±0.7)%, respectively. The microspheres are proved to be successful in prolonging drug release up to 10 d or more. The central composite design-response surface methodology has good prediction ability.

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