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一种具有自增强作用的新型亲水性黏附基质,用于药物经大鼠皮肤的透皮渗透。

A novel hydrophilic adhesive matrix with self-enhancement for drug percutaneous permeation through rat skin.

作者信息

Zhang Jianhua, Liu Zhipeng, Du Hai, Zeng Yong, Deng Liandong, Xing Jinfeng, Dong Anjie

机构信息

School of Material Science and Engineering, Tianjin University, Tianjin, China.

出版信息

Pharm Res. 2009 Jun;26(6):1398-406. doi: 10.1007/s11095-009-9850-1. Epub 2009 Feb 19.

Abstract

PURPOSE

In transdermal drug delivery system (TDDS), chemical enhancers and crystallization inhibitors added into the adhesive matrixes to improve drug permeation and formulation stability often result in some negative effect on adhesive properties and dressing performance. The aim of this paper is to develop a hydrophilic pressure sensitive adhesive (PSA) for TDDS without using additional chemical enhancers and crystallization inhibitors.

METHODS

A quaternary blend (PDGW) composed of polyvinyl pyrrolidone, D,L-lactic acid oligomers, glycerol and water was prepared. The adhesive strength, drug loading capacity, drug state and stability of PDGW were characterized by using ibuprofen (IBU) and salicylic acid (SA) as model drugs. Moreover, In vitro and in vivo drug permeation through rat skin from PDGW patch in comparison to acrylate adhesive (ACA) and nature rubber adhesive (NRA) was investigated.

RESULTS

PDGW performs excellent drug loading and crystallization inhibition capacity. Furthermore, the accumulative amount for 24 h in vitro from PDGW patch is far higher than that from ACA and NRA patch. And the plasma concentration of drugs in vivo from PDGW patch is bigger than that from ACA patch.

CONCLUSIONS

PDGW possesses excellent PSA properties and self-enhancement for drug percutaneous permeation, which can be used to develop new formulation of TDDS.

摘要

目的

在透皮给药系统(TDDS)中,添加到黏附基质中的化学促进剂和结晶抑制剂在改善药物渗透和制剂稳定性的同时,常常会对黏附性能和敷料性能产生一些负面影响。本文旨在开发一种无需使用额外化学促进剂和结晶抑制剂的用于TDDS的亲水性压敏胶(PSA)。

方法

制备了一种由聚乙烯吡咯烷酮、D,L-乳酸低聚物、甘油和水组成的四元共混物(PDGW)。以布洛芬(IBU)和水杨酸(SA)作为模型药物,对PDGW的黏附强度、载药量、药物状态和稳定性进行了表征。此外,研究了与丙烯酸酯黏合剂(ACA)和天然橡胶黏合剂(NRA)相比,PDGW贴剂中药物经大鼠皮肤进行的体外和体内渗透。

结果

PDGW具有优异的载药和抑制结晶能力。此外,PDGW贴剂的体外24小时累积量远高于ACA和NRA贴剂。并且,PDGW贴剂的药物体内血浆浓度高于ACA贴剂。

结论

PDGW具有优异的PSA性能和药物经皮渗透的自增强作用,可用于开发TDDS的新制剂。

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