Document Detail


A kinetic study of the polymorphic transformation of nimodipine and indomethacin during high shear granulation.
MedLine Citation:
PMID:  21553164     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The objective of the present study was to investigate the mechanism, kinetics, and factors affecting the polymorphic transformation of nimodipine (NMD) and indomethacin (IMC) during high shear granulation. Granules containing active pharmaceutical ingredient, microcrystalline cellulose, and low-substituted hydroxypropylcellulose were prepared with ethanolic hydroxypropylcellulose solution, and the effects of independent process variables including impeller speed and granulating temperature were taken into consideration. Two polymorphs of the model drugs and granules were characterized by X-ray powder diffraction analysis and quantitatively determined by differential scanning calorimetry. A theoretical kinetic method of ten kinetic models was applied to analyze the polymorphic transformation of model drugs. The results obtained revealed that both the transformation of modification I to modification II of NMD and the transformation of the α form to the γ form of IMC followed a two-dimensional nuclei growth mechanism. The activation energy of transformation was calculated to be 7.933 and 56.09 kJ·mol(-1) from Arrhenius plot, respectively. Both the granulating temperature and the impeller speed affected the transformation rate of the drugs and, in particular, the high shear stress significantly accelerated the transformation process. By analyzing the growth mechanisms of granules in high-shear mixer, it was concluded that the polymorphic transformation of NMD and IMC took place in accordance with granule growth in a high-shear mixer.
Authors:
Zhen Guo; Mingxin Ma; Tianyi Wang; Di Chang; Tongying Jiang; Siling Wang
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Publication Detail:
Type:  Comparative Study; Journal Article; Research Support, Non-U.S. Gov't     Date:  2011-05-07
Journal Detail:
Title:  AAPS PharmSciTech     Volume:  12     ISSN:  1530-9932     ISO Abbreviation:  AAPS PharmSciTech     Publication Date:  2011 Jun 
Date Detail:
Created Date:  2011-07-13     Completed Date:  2012-05-16     Revised Date:  2013-06-30    
Medline Journal Info:
Nlm Unique ID:  100960111     Medline TA:  AAPS PharmSciTech     Country:  United States    
Other Details:
Languages:  eng     Pagination:  610-9     Citation Subset:  IM    
Affiliation:
School of Pharmacy, Shenyang Pharmaceutical University, People's Republic of China.
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MeSH Terms
Descriptor/Qualifier:
Cellulose / analogs & derivatives,  chemistry,  standards
Chemistry, Pharmaceutical / instrumentation,  methods*,  standards
Indomethacin / chemistry,  pharmacokinetics*,  standards
Nimodipine / chemistry,  pharmacokinetics*,  standards
Polymers / chemistry,  pharmacokinetics*,  standards
Shear Strength*
X-Ray Diffraction / instrumentation,  methods,  standards
Chemical
Reg. No./Substance:
0/Polymers; 0/microcrystalline cellulose; 53-86-1/Indomethacin; 66085-59-4/Nimodipine; 9004-34-6/Cellulose; 9004-64-2/hydroxypropylcellulose
Comments/Corrections

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