两种超崩解剂对异烟肼与利福平联合分散片口服治疗肺结核的影响

V. Shukla, F. Manvi
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引用次数: 7

摘要

口服给药途径被广泛接受,占总药物形式的50-60%。快速崩解给药系统具有起效快、美观大方、给药方便等优点。为了提高抗结核药物异烟肼利福平快速崩解片的生物利用度,本研究尝试采用直接压缩法制备异烟肼利福平快速崩解片。这些配方具有足够的硬度,可以用常用的设备制造。在配方前,对预压缩参数进行流动特性表征,并对制备的配方进行理化参数、x射线粉末晶体学、扫描电镜和体内生物利用度评估。4种配方均具有良好的崩解性能,总崩解时间为25 ~ 40秒。考察了不同的超崩解剂和工艺参数对药物释放曲线和崩解性能的影响,结果表明不同的超崩解剂如Ac-di sol和Polyplastadone XL对药物释放效果更好。所有制剂在口腔内迅速崩解,并具有良好的抗结核性能。扫描电镜显示,配方的机械强度影响压缩后的形态变化。因此,从本研究中可以明显看出,快速分散片可能是异烟肼、利福平的一种很有前途的给药系统,它们的联合使用具有良好的口腔感觉和改善的药物可用性,并且患者的依从性更好。关键词:异烟肼;利福平;Superdisintegrants;直接压缩法;生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Effect of two different superdisintegrants on combinaion dispersible tablets of isoniazid and rifampicin for oral treatment of tuberculosis
Oral route of administration have wide acceptance up to 50-60% to total drug forms. Fast disintegrating drug delivery system has number of advantage such as faster onset of action, attractive elegance, ease of administration. In this study, an attempt has been made to study direct compression method, for formulation of fast disintegrating tablets of Isoniazid and Rifampicin, an anti-tubercular drug in view of enhancing bioavailability. These formulations have sufficient hardness and can be manufactured by commonly used equipment. Prior to formulation the pre-compression parameters were characterized for flow properties and prepared formulations were evaluated for physico-chemical parameters, X-ray powder crystallography, SEM and in-vivo bioavailability. All four formulations possessed good disintegration properties with total disintegration time of 25 to 40 seconds. The effects of different superdisintegrants and process variables on drug release profile and disintegration property were evaluated and results revealed the better drug release with different superdisintegrants such as Ac-di sol and Polyplastadone XL. All formulations are rapidly disintegrated in oral cavity as well as all formulations possess good anti-tubercular properties. SEM Showed the mechanical strength of the formulations affected the morphological changes after compression. Hence, it is evident from this study that fast dispersible tablets could be a promising delivery system for Isoniazid, Rifampicin and their combination with good mouth feel and improved drug availability with better patient compliance. Keywords: Isoniazid; Rifampicin; Superdisintegrants; Direct compression method; Bioavailability.
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