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加工变量对以洋常春藤胶为控释辅料的曲马多基质片的机械性能和释放特性的影响。

The effect of processing variables on the mechanical and release properties of tramadol matrix tablets incorporating Cissus populnea gum as controlled release excipient.

作者信息

Adeleye Olutayo Ademola, Femi-Oyewo Mbang Nyong, Odeniyi Michael Ayodele

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, Olabisi Onabanjo University, Ago-Iwoye, Ogun State, Nigeria.

Department of Pharmaceutics and Industrial Pharmacy, University of Ibadan, Ibadan, Oyo State, Nigeria.

出版信息

Polim Med. 2014 Oct-Dec;44(4):209-20.

Abstract

BACKGROUND

Natural gums are polymers widely used as excipients in drug formulation. Polymer extraction and formulation processing methods could significantly affect formulation characteristics.

OBJECTIVES

To evaluate different methods of gum extraction and the effect of different compression methods on the mechanical and release properties of tramadol hydrochloride matrix tablets incorporating cissus gum as controlled release polymer.

MATERIAL AND METHODS

Water (CW) and acetone (CA) extracts of cissus gum were obtained from Cissus populea stem and two methods - wet granulation and direct compression - were used to compress the tablet and compare it with xanthan gum (X) formulations. Crushing strength and friability were used to assess mechanical properties while dissolution rate were used to assess release properties. Data were analysed using t-test and ANOVA at p < 0.05.

RESULTS

The crushing strength of tramadol tablets has increased together with the increase in polymer concentration in all formulations, while friability has decreased for both methods. Tablets made by wet granulation had higher crushing strength than those made by direct compression method. The release mechanism for both direct compression and wet granulation methods was Fickian and non-Fickian respectively. The rank order for t25, t50 and t75 for all formulations was X > CA > CW. Generally, wet granulation method decreased the rate of tramadol release more than direct compression method, indicating a higher drug retarding ability.

CONCLUSIONS

Incorporation of cissus gum controlled the release of tramadol hydrochloride from the matrix tablets. Extraction method and formulation variables influenced mechanical and release properties of the tablets. Cissus gum acetone extract had comparable release properties with xanthan gum and could serve as a cheaper alternative in controlled release tablet formulations.

摘要

背景

天然胶是广泛用作药物制剂辅料的聚合物。聚合物提取和制剂加工方法会显著影响制剂特性。

目的

评估不同的胶提取方法以及不同压片方法对以西番莲胶作为控释聚合物的盐酸曲马多基质片的机械性能和释放性能的影响。

材料与方法

从西番莲茎中获得西番莲胶水提取物(CW)和丙酮提取物(CA),并采用湿法制粒和直接压片两种方法压制片剂,并与黄原胶(X)制剂进行比较。用抗压强度和脆碎度评估机械性能,用溶出速率评估释放性能。采用t检验和方差分析对p < 0.05的数据进行分析。

结果

在所有制剂中,盐酸曲马多片的抗压强度随聚合物浓度的增加而增加,而两种方法的脆碎度均降低。湿法制粒制备的片剂比直接压片法制备的片剂具有更高的抗压强度。直接压片法和湿法制粒法的释放机制分别为菲克扩散和非菲克扩散。所有制剂的t25、t50和t75的排序为X > CA > CW。一般来说,湿法制粒法比直接压片法更能降低盐酸曲马多的释放速率,表明其药物缓释能力更强。

结论

加入西番莲胶可控制盐酸曲马多从基质片中的释放。提取方法和制剂变量影响片剂的机械性能和释放性能。西番莲胶丙酮提取物与黄原胶具有相当的释放性能,可作为控释片剂制剂中更便宜的替代品。

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