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采用压制包衣技术研制含阿托伐他汀/氯吡格雷/阿司匹林的具有粘膜粘附核心的压缩包衣复方药丸。

DEVELOPMENT OF COMPRESSED COATED POLYPILL WITH MUCOADHESIVE CORE COMPRISING OF ATORVASTATIN/CLOPIDOGREL/ASPIRIN USING COMPRESSION COATING TECHNIQUE.

作者信息

Shahid Nabeel, Adnan Sherjeel, Farooq Muhammad, Ali Sajid, Shabbir Maryam, Masood Zeeshan, Waqar Kiran, Saleem Hamad, Gill Shoaib Ali, Ali Tabish

出版信息

Acta Pol Pharm. 2017 Mar;74(2):477-487.

Abstract

The study was conducted to formulate and assess a novel polypill comprising of atorvastatin calci- um (ATVC), clopidogrel bisulfate (CLB) and aspirin (ASP) which, after in vivo correlation, can be intended for use in hyperlipidemic chronic heart disease patients. Polypill was made by the compression coating technique (CCT) with multiple active ingredients along with different concentrations of mucoadhesive and sustained release polymers, i.e., Carbopol 934 (CAB), Methocel k15 (MTH) and sodium carboxymethyl cellulose (NaCMC). The effect of different concentration of polymers on physical properties, wash off time, mucoadhe- sion strength, swelling behavior, surface pH and drug release kinetics were investigated. In vitro drug release studies showed that combination of CAB-NaCMC (1 : 1) retarded drug release up to 96.7 ± 1.15%, while com- bination of CAB-MTH and MTH-NaCMC retarded drug release up to 81.9 ± 1.5% and 101.4 ± 1.3%, respec- tively, at the same polymer concentration. Core enteric coated tablet of ATVC (K 11) was compressed over with CLB and ASP granules with the help of CCT and produced the desired results with zero order release rate thus indicating successful formulation of proposed polypill.

摘要

本研究旨在制备并评估一种新型复方制剂,其由阿托伐他汀钙(ATVC)、硫酸氢氯吡格雷(CLB)和阿司匹林(ASP)组成,经体内相关性研究后,可用于高脂血症慢性心脏病患者。该复方制剂采用压制包衣技术(CCT)制备,包含多种活性成分以及不同浓度的黏膜黏附聚合物和缓释聚合物,即卡波姆934(CAB)、羟丙甲纤维素k15(MTH)和羧甲基纤维素钠(NaCMC)。研究了不同浓度聚合物对物理性质、洗脱时间、黏膜黏附强度、溶胀行为、表面pH值和药物释放动力学的影响。体外药物释放研究表明,在相同聚合物浓度下,CAB - NaCMC(1:1)组合使药物释放延迟高达96.7±1.15%,而CAB - MTH和MTH - NaCMC组合分别使药物释放延迟高达81.9±1.5%和101.4±1.3%。借助CCT将ATVC的肠溶包衣片芯(K 11)与CLB和ASP颗粒压制在一起,得到了零级释放速率的理想结果,从而表明所提出的复方制剂成功制备。

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