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十六烷基氯化吡啶生物黏附片的制剂与表征

Formulation and characterization of cetylpyridinium chloride bioadhesive tablets.

作者信息

Akbari Jafar, Saeedi Majid, Morteza-Semnani Katayoun, Kelidari Hamidreza, Lashkari Maryam

机构信息

Department of pharmaceutics, Faculty of pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

Department of medicinal chemistry, Faculty of pharmacy, Mazandaran University of Medical Sciences, Sari, Iran.

出版信息

Adv Pharm Bull. 2014 Dec;4(4):385-90. doi: 10.5681/apb.2014.057. Epub 2014 Aug 10.

Abstract

PURPOSE

Bioadhesive polymers play an important role in biomedical and drug delivery applications. The aim of this study is to develop a sustained- release tablet for local application of Cetylpyridinium Chloride (CPC). This delivery system would supply the drug at an effective level for a long period of time, and thereby overcome the problem of the short retention time of CPC and could be used for buccal delivery as a topical anti-infective agent.

METHODS

CPC bioadhesive tablets were directly prepared using 7 mm flat-faced punches on a hydraulic press. The materials for each tablet were weighted, introduced into the die and compacted at constant compression pressure. The dissolution tests were performed to the rotation paddle method and the bioadhesive strength of the tablets were measured.

RESULTS

The results showed that as the concentration of polymer increased, the drug release rate was decreased. Also the type and ratio of polymers altered the release kinetic of Cetylpyridinium Chloride from investigated tablets. The bioadhesion strength increased with increasing the concentration of polymer and maximum bioadhesion strength was observed with HPMC K100M.

CONCLUSION

The selected formulation of CPC bioadhesive tablet can be used as a suitable preparation for continuous release of CPC with appropriate bioadhesion strength.

摘要

目的

生物黏附性聚合物在生物医学和药物递送应用中发挥着重要作用。本研究的目的是开发一种用于局部应用西吡氯铵(CPC)的缓释片。该递送系统将在较长时间内以有效水平提供药物,从而克服CPC滞留时间短的问题,并可作为局部抗感染剂用于颊部给药。

方法

使用7毫米平面冲头在液压机上直接制备CPC生物黏附片。对每片的材料进行称重,放入模具中,并在恒定压缩压力下压制。采用旋转桨法进行溶出试验,并测量片剂的生物黏附强度。

结果

结果表明,随着聚合物浓度的增加,药物释放速率降低。聚合物的类型和比例也改变了所研究片剂中西吡氯铵的释放动力学。生物黏附强度随聚合物浓度的增加而增加,HPMC K100M的生物黏附强度最高。

结论

所选的CPC生物黏附片制剂可作为具有适当生物黏附强度的CPC持续释放的合适制剂。

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