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布洛芬、微晶纤维素和气相二氧化硅熔融分散后颗粒重排、压缩行为及溶解性能的研究。

Study of particle rearrangement, compression behavior and dissolution properties after melt dispersion of ibuprofen, Avicel and Aerosil.

作者信息

Mallick Subrata, Kumar Pradhan Saroj, Chandran Muronia, Acharya Manoj, Digdarsini Tanmayee, Mohapatra Rajaram

机构信息

Department of Pharmaceutics, School of Pharmaceutical Sciences, Siksha 'O' Anusandhan University, Kalinganagar, Bhubaneswar 751003, Orissa, India.

Department of Pharmaceutics, College of Pharmaceutical Sciences, Berhampur, Mohuda, Orissa, India.

出版信息

Results Pharma Sci. 2011 May 17;1(1):1-10. doi: 10.1016/j.rinphs.2011.05.003. eCollection 2011 May.

Abstract

Particle rearrangements, compaction under pressure and in vitro dissolution have been evaluated after melt dispersion of ibuprofen, Avicel and Aerosil. The Cooper-Eaton and Kuno equations were utilized for the determination of particle rearrangement and compression behavior from tap density and compact data. Particle rearrangement could be divided into two stages as primary and secondary rearrangement. Transitional tapping between the stages was found to be 20-25 taps in ibuprofen crystalline powder, which was increased up to 45 taps with all formulated powders. Compaction in the rearrangement stages was increased in all the formulations with respect to pure ibuprofen. Significantly increased compaction of ibuprofen under pressure can be achieved using Avicel by melt dispersion technique, which could be beneficial in ibuprofen tablet manufacturing by direct compression. SEM, FTIR and DSC have been utilized for physicochemical characterization of the melt dispersion powder materials. Dissolution of ibuprofen from compacted tablet of physical mixture and melt dispersion particles has also been improved greatly in the following order: Ibc<Ibsmd1<Ibsmd2<Ibsmp10<Ibsmd5<Ibsmd10.

摘要

对布洛芬、微晶纤维素(Avicel)和气相二氧化硅(Aerosil)进行熔融分散后,评估了颗粒重排、压力下压实以及体外溶出情况。利用库珀 - 伊顿方程和库诺方程,根据振实密度和压片数据来确定颗粒重排和压缩行为。颗粒重排可分为初级重排和次级重排两个阶段。在布洛芬结晶粉末中,发现两个阶段之间的过渡振实为20 - 25次,而在所有配方粉末中,该次数增加到了45次。与纯布洛芬相比,所有配方在重排阶段的压实程度均有所增加。通过熔融分散技术使用微晶纤维素,可显著提高布洛芬在压力下的压实程度,这对于布洛芬片剂的直接压片制造可能有益。扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)已用于对熔融分散粉末材料进行物理化学表征。布洛芬从物理混合物压片和熔融分散颗粒压片中的溶出情况也有了极大改善,顺序如下:Ibc < Ibsmd1 < Ibsmd2 < Ibsmp10 < Ibsmd5 < Ibsmd10。

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