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以纤维素纳米纤维为赋形剂的悬浮聚合药物输送用医药丙烯酸珠。

Pharmaceutical acrylic beads obtained by suspension polymerization containing cellulose nanowhiskers as excipient for drug delivery.

机构信息

Universidade Federal de Minas Gerais - UFMG, Faculdade de Engenharia, Departamento de Engenharia Metalúrgica e de Materiais, Av. Antônio Carlos, 6627, sala 3551, Bloco 2, Pampulha, CEP: 31270-901, Belo Horizonte, MG, Brazil.

出版信息

Eur J Pharm Sci. 2011 Mar 18;42(4):406-15. doi: 10.1016/j.ejps.2011.01.005. Epub 2011 Jan 15.

Abstract

Direct compression is one of the most popular techniques to prepare tablets but only a few commercial excipients are well adapted for this process into controlled release formulations. In the last years, the introduction of new materials for drug delivery matrix tablets has become more important. This paper evaluated the physicochemical and flow properties of new polymeric excipient of ethyl acrylate, methyl methacrylate and butyl metacrylate, synthesized by suspension polymerization using cellulose nanowhiskers as co-stabilizer, to be used as direct compression for modified release tablets. Infrared spectroscopy (FTIR) confirmed the success of the copolymerization reaction. Scanning electron microscopy (SEM) showed that excipient was obtained how spherical beads. Thermal properties of the beads were characterized by thermogravimetric (TG) analysis. Particle size analysis of the beads with cellulose nanowhiskers (CNWB) indicated that the presence of the nanowhiskers led to a reduction of particle size and to a narrower size distribution. In vitro test showed that the nanowhiskers and beads produced are nontoxic. Parameters such as Hausner ratio, Carr's index and cotangent of angle α were employed to characterize the flow properties of CNWB beads. Furthermore, the beads are used to produce tablets by direct compression contained propranolol hydrochloride as model drug. Dissolution tests performed suggested that beads could be used as excipient in matrix tablets with a potential use in drug controlled release.

摘要

直接压缩是制备片剂最常用的技术之一,但只有少数商业赋形剂非常适合用于控释制剂的该工艺。在过去的几年中,用于药物传递基质片剂的新材料的引入变得更加重要。本文评估了通过悬浮聚合使用纤维素纳米纤维作为共稳定剂合成的新型丙烯酸乙酯、甲基丙烯酸甲酯和甲基丙烯酸丁酯的聚合赋形剂的物理化学和流动性能,用作控释片剂的直接压片。红外光谱(FTIR)证实了共聚反应的成功。扫描电子显微镜(SEM)显示赋形剂呈球形珠状。通过热重分析(TG)对珠的热性能进行了表征。带有纤维素纳米纤维(CNWB)的珠的粒径分析表明,纳米纤维的存在导致粒径减小和粒径分布变窄。体外试验表明纳米纤维和珠是无毒的。使用哈纳斯比、卡尔指数和角度正切的余切等参数来表征 CNWB 珠的流动性能。此外,还使用珠通过直接压缩来制备含有盐酸普萘洛尔作为模型药物的片剂。进行的溶出度试验表明,珠可用作基质片剂中的赋形剂,具有在药物控制释放中潜在的用途。

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