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通过中心复合设计评估不同的速熔崩解剂。

Evaluation of different fast melting disintegrants by means of a central composite design.

作者信息

Di Martino Piera, Martelli Sante, Wehrlé Pascal

机构信息

Laboratorio di Tecnica Farmaceutica, Dipartimento di Scienze Chimiche, Via S Agostino, 62032 Camerino, Italy.

出版信息

Drug Dev Ind Pharm. 2005 Jan;31(1):109-21. doi: 10.1081/ddc-44233.

Abstract

Fast-disintegration technologies have encountered increased interest from industries in the past decades. In order to orientate the formulators to the choice of the best disintegrating agent, the most common disintegrants were selected and their ability to quickly disintegrate direct compressed tablets was evaluated. For this study, a central composite design was used. The main factors included were the concentration of disintegrant (X1) and the compression force (X2). These factors were studied for tablets containing either Zeparox or Pearlitol 200 as soluble diluents and six different disintegrants: L-HPC LH11 and LH31, Lycatab PGS, Vivasol, Kollidon CL, and Explotab. Their micromeritics properties were previously determined. The response variables were disintegration time (Y1), tensile strength (Y2), and porosity (Y3). Whatever the diluent, the longest disintegration time is obtained with Vivasol as the disintegrant, while Kollidon CL leads to the shortest disintegration times. Exception for Lycatab PGS and L-HPC LH11, formulations with Pearlitol 200 disintegrate faster. Almost the same results are obtained with porosity: no relevant effect of disintegrant concentration is observed, since porosity is mainly correlated to the compression force. In particular, highest values are obtained with Zeparox as the diluent when compared to Pearlitol 200 and, as the type of disintegrant is concerned, no difference is observed. Tensile strength models have been all statistically validated and are all highly dependent on the compression force. Lycatab PGS concentration does not affect disintegration time, mainly increased by the increase of compression pressure. When Pearlitol 200 is used with Vivasol, disintegration time is more influenced by the disintegrant concentration than by the compression pressure, an increase in concentration leading to a significant and relevant increase of the disintegration time. With Zeparox, the interaction between the two controlled variables is more complex: there is no effect of compression force on the disintegration time for a small amount of disintegrant, but a significant increase for higher concentrations. With Kollidon CL, the main factor influencing the disintegration time is the compression force, rather than the disintegrant concentration. Increasing both the compression force and the disintegrant concentration leads to an increase of the disintegration time. For lower Kollidon CL percentages, the compression pressure increases dramatically the tablet disintegration. With the Explotab, whatever the increase of compression force, the disintegrant concentration leads to an increase of the disintegration time. According to Student's t-test, only the compression force significantly and strongly influences the disintegration time when Pearlitol 200 is used. A slight interaction and some trends nevertheless appear: above 150 MPa, increasing the disintegrant concentration leads to a shortened disintegration time, below this limit the opposite effect is observed.

摘要

在过去几十年中,速崩解技术越来越受到各行业的关注。为了帮助配方设计师选择最佳崩解剂,我们挑选了最常用的崩解剂,并评估了它们使直接压片快速崩解的能力。在本研究中,采用了中心复合设计。主要因素包括崩解剂浓度(X1)和压片力(X2)。针对含有Zeparox或Pearlitol 200作为可溶性稀释剂以及六种不同崩解剂(L-HPC LH11和LH31、Lycatab PGS、Vivasol、Kollidon CL和Explotab)的片剂对这些因素进行了研究。之前已测定了它们的粉体学性质。响应变量为崩解时间(Y1)、抗张强度(Y2)和孔隙率(Y3)。无论使用何种稀释剂,以Vivasol作为崩解剂时崩解时间最长,而Kollidon CL导致的崩解时间最短。除了Lycatab PGS和L-HPC LH11外,含有Pearlitol 200的制剂崩解更快。孔隙率方面得到了几乎相同的结果:未观察到崩解剂浓度的相关影响,因为孔隙率主要与压片力相关。特别是,与Pearlitol 200相比,以Zeparox作为稀释剂时孔隙率最高值,并且就崩解剂类型而言,未观察到差异。抗张强度模型均经过统计学验证,并且都高度依赖于压片力。Lycatab PGS的浓度不影响崩解时间,崩解时间主要因压片压力的增加而延长。当Pearlitol 200与Vivasol一起使用时,崩解时间受崩解剂浓度的影响大于压片压力,浓度增加会导致崩解时间显著且相关地增加。对于Zeparox,两个控制变量之间的相互作用更为复杂:对于少量崩解剂,压片力对崩解时间没有影响,但对于较高浓度则有显著增加。对于Kollidon CL,影响崩解时间的主要因素是压片力,而不是崩解剂浓度。压片力和崩解剂浓度的增加都会导致崩解时间增加。对于较低的Kollidon CL百分比,压片压力会显著增加片剂的崩解。对于Explotab,无论压片力如何增加,崩解剂浓度都会导致崩解时间增加。根据学生t检验,当使用Pearlitol 200时,只有压片力对崩解时间有显著且强烈的影响。不过仍出现了轻微的相互作用和一些趋势:在150 MPa以上,崩解剂浓度增加会导致崩解时间缩短,低于此限度则观察到相反的效果。

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