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低熔点药物酮洛芬和布洛芬与交联聚维酮的粉末固体分散体的流动性和压片特性

Fluidity and tableting characteristics of a powder solid dispersion of the low melting drugs ketoprofen and ibuprofen with crospovidone.

作者信息

Shibata Yusuke, Fujii Makiko, Noda Shinobu, Kokudai Makiko, Okada Hideko, Kondoh Masuo, Watanabe Yoshiteru

机构信息

Showa Pharmaceutical University, 3-3165 Higashi-Tamagawagakuen, Machida, Tokyo, 194-8543, Japan.

出版信息

Drug Dev Ind Pharm. 2006 Apr;32(4):449-56. doi: 10.1080/03639040500529127.

Abstract

A powder solid dispersion system (SD) of ketoprofen (KP) or ibuprofen (IP), which possess low melting points, plus crospovidone (CrosPVP), have good fluidity characteristics and can be used to formulate tablets. Tablets of KP or IP in the SD of adequate hardness within a narrow weight range can be prepared by direct compression. Addition of microcrystalline cellulose (MCC) resulted in greater hardness characteristics and less variation in tablet weight. Forces during the tableting process were measured with a tableting process analyzer (TabAll) equipped with a single-punch for determining capping and sticking properties during the tableting process. Pressure transmission ratio from the upper to the lower punch and die wall force were increased by adding 1% magnesium stearate (MS) to the SD. Ejection force decreased when MS was added to the SD. When tablets of the IP SD were prepared without excipient, scraper pressure (SP) was large, resulting in sticking. However, addition of 1% MS, lowered the SP value and eliminated sticking. Thus, an SD of compounds with a low melting point such as KP or IP is suitable for tablet manufacture by direct compression with the addition of 1% MS.

摘要

酮洛芬(KP)或布洛芬(IP)的粉末固体分散体系统(SD),它们具有低熔点,加上交联聚维酮(CrosPVP),具有良好的流动性特征,可用于制备片剂。通过直接压片可以制备出硬度足够、重量范围狭窄的SD中KP或IP片剂。添加微晶纤维素(MCC)可获得更大的硬度特征,且片剂重量变化更小。使用配备单冲头的压片过程分析仪(TabAll)测量压片过程中的力,以确定压片过程中的裂片和黏附特性。向SD中添加1%硬脂酸镁(MS)可提高上冲头与下冲头之间的压力传递率以及冲模壁力。向SD中添加MS时,顶出力降低。在不添加辅料制备IP SD片剂时,刮刀压力(SP)较大,导致黏附。然而,添加1% MS可降低SP值并消除黏附。因此,KP或IP等低熔点化合物的SD适合通过添加1% MS直接压片来制造片剂。

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