Formulation Development of Floating Microspheres of Cefditoren Pivoxel by 32 Factorial Design and in Vitro Characterization

Formulation Development of Floating Microspheres of Cefditoren Pivoxel by 32 Factorial Design and in Vitro Characterization
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头孢托仑 Pivoxel 漂浮微球的 32 因子设计和体外表征的制剂开发

DOI:
10.22377/ajp.v10i1.546
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发表时间:
2016
影响因子:
0.4
通讯作者:
Swathi Chilukala
Swathi Chilukala
中科院分区:
--
文献类型:
--
作者:
Swathi Chilukala

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目的:本研究工作的主要目的是开发头孢妥仑羟氨苄(CP)的漂浮微球,以提供药物的持续速率。材料与方法:以羟丙基甲基纤维素(HPMC)K4 M和乙基纤维素为控速聚合物,采用溶剂挥发法制备CP漂浮微球。通过32因子设计进行处方优化,使用两个因素;聚合物的总量(X1)和乙基纤维素的浓度(X2)作为自变量。通过产率、粒径、包封率、体外释药、浮力、表面形貌(扫描电镜分析)等指标对微球进行表征。结果与讨论:优化处方(F6)12 h释药率为91.5 ± 1.35%,包封率为75 ± 0.92%。所有制剂均具有良好的浮力,其在溶解介质中漂浮超过12小时。结论:结果表明,以羟丙甲纤维素、乙基纤维素为控速聚合物,成功地制备了CP漂浮微球。
Aim: The main objective of the present research work was to develop floating microspheres of cefditoren pivoxel (CP) to provide the delivery of the drug at a sustained rate. Materials and Methods: Floating microspheres of CP were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC) K4M and ethyl cellulose as the rate controlling polymers. The optimization of formulation was carried out by 32 factorial design using two factors; a total amount of polymer (X1) and concentration of ethyl cellulose (X2) as independent variables. The formulated floating microspheres were characterized by evaluating its yield, particle size, encapsulation efficiency, in vitro drug release, buoyancy, surface morphology (scanning electron microscopy analysis). Results and Discussion: The optimized formulation (F6) showed 91.5 ± 1.35% of drug release after 12 h and 75 ± 0.92% of entrapment efficiency. All the formulations have good buoyancy which was floated over 12 h in the dissolution medium. Conclusion: It can be concluded from the study that floating microspheres of CP can be prepared successfully using HPMC K4M and ethyl cellulose as the rate controlling polymers.