头孢呋辛酯鼻腔给药系统的配方开发、表征和评价

IF 0.4 Q4 PHARMACOLOGY & PHARMACY
S. Rajarajan
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引用次数: 0

摘要

目的:研制头孢呋辛酯(CA)鼻黏附微球,作为治疗呼吸道感染的一种替代剂型。材料与方法:以壳聚糖和β -环糊精为缓释聚合物,采用改性乳剂-冻干法制备CA微球。通过24因子设计对模型进行优化,并用方差分析对模型进行验证。评价CA微球的包封效率、体外黏附和药物释放率。对优化后的配方进行了傅里叶红外(FT-IR)分析、粒径、多分散性指数(PDI)和zeta电位、热分析、DSC和XRD、扫描电镜表面形貌以及体外和离体释放动力学研究。主要发现:包封效率为69.21 ~ 80.45%,粒径范围为12.55 ~ 17.22 μm,黏附范围为72.51 ~ 79.68%,药物释放范围为72.21 ~ 83.65%。FT-IR研究确保配方微球中没有药物-聚合物相互作用。测定了微球的PDI和zeta电位,微球的平均粒径和分布都在该范围内,表面形貌显示所有配方均为球形表面和由药物和聚合物组成的外壳包围的圆形腔体。DSC和XRD均可接受,6 h后微球制剂的体外和体外释放谱分别为80.25和76.28%。6个月的稳定性研究表明,优化后的制剂稳定,物理外观无变化。结论:鼻腔CA微球具有足够的给药潜力
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Formulation Development, Characterization, and Evaluation of Controlled Nasal Drug Delivery Systems for Cefuroxime Axetil
Objective: This current study objective is to develop cefuroxime axetil (CA) nasal mucoadhesive microspheres for an alternative utilization of dosage form for respiratory tract infections Materials and Methods: CA microspheres were prepared by modified emulsion-lyophilization method in which chitosan and beta-cyclodextrin were used as a release retardant polymer. The model is optimization by 24 factorial designs and validated using ANOVA. CA microspheres evaluated for entrapment efficiency, ex vivo mucoadhesion and % drug release. The optimized formulations were performed for its Fourier transform infrared (FT-IR) analysis, particle size and polydispersity index (PDI) and zeta potential, thermal analysis DSC and XRD, and surface morphology by scanning electron microscopy followed by in vitro and ex vivo release kinetic studies. Key Findings: Results of these evaluations showed that entrapment efficiency was found to be 69.21–80.45%, particle size in the range of 12.55–17.22 μm, mucoadhesion in the range of 72.51–79.68%, and drug release in the range of 72.21–83.65%. FT-IR studies ensured that no drug-polymer interaction in the formulated microspheres. PDI and zeta potential were measured and the mean particle size and distribution of microspheres were in the range and the surface topography revealed a spherical surface for all the formulations and a round cavity enclosed by an outer shell composed of the drug and polymer. DSC and XRD were found to be in fairly acceptable and in vitro and ex vivo release profile of microspheres formulation was found to be 80.25 and 76.28% at the end of 6 h. Stability studies for 6 months revealed that the optimized formulation was stable, no changes in physical appearance. Conclusion: Finally, it was concluded that the nasal microspheres of CA may have potential enough for effective drug delivery
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来源期刊
Asian Journal of  Pharmaceutics
Asian Journal of Pharmaceutics PHARMACOLOGY & PHARMACY-
自引率
0.00%
发文量
47
期刊介绍: Character of the publications: -Pharmaceutics and Pharmaceutical Technology -Formulation Design and Development -Drug Discovery and Development Interface -Manufacturing Science and Engineering -Pharmacokinetics, Pharmacodynamics, and Drug Metabolism -Clinical Pharmacology, General Medicine and Translational Research -Physical Pharmacy and Biopharmaceutics -Novel Drug delivery system -Biotechnology & Microbiological evaluations -Regulatory Sciences
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