Highly compressible paracetamol: I: crystallization and characterization

被引:64
作者
Garekani, HA [1 ]
Ford, JL [1 ]
Rubinstein, MH [1 ]
Rajabi-Siahboomi, AR [1 ]
机构
[1] Liverpool John Moores Univ, Sch Pharm & Chem, Liverpool L3 3AF, Merseyside, England
关键词
paracetamol; polyvinylpyrrolidone; crystallization; crystal habit; crystal structure; differential scanning calorimetry; X-ray powder diffraction;
D O I
10.1016/S0378-5173(00)00550-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
It was found that polyvinylpyrrolidone (PVP) is an effective additive during crystallization of paracetamol and significantly influenced the crystallization and crystal habit of paracetamol. These effects were attributed to adsorption of PVP onto the surfaces of growing crystals. It was found that the higher molecular weights of PVP (PVP 10 000 and PVP 50 000) were more effective additives than lower molecular weight PVP (PVP 2000). Paracetamol particles obtained in the presence of 0.5% w/v of PVP 10 000 or PVP 50 000 had near spherical structure and consisted of numerous rod-shaped microcrystals which had agglomerated together. Particles obtained in the presence of PVP 2000 consisted of fewer microcrystals. Differential scanning calorimetry (DSC) and X-ray powder diffraction (XPD) experiments showed that paracetamol particles, crystallized in the presence of PVP, did not undergo structural modifications. By increasing the molecular weight and/or the concentration of PVP in the crystallization medium the amount of PVP incorporated into the paracetamol particles increased. The maximum amount of PVP in the particles was 4.32% w/w. (C) 2000 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:87 / 99
页数:13
相关论文
共 25 条
[1]  
ABDELILLAH E, 1995, P 14 PHARM TECH C SP, V2, P368
[2]   MODIFICATION OF PHENYTOIN CRYSTALS - INFLUENCE OF 3-ACETOXYMETHYL-5,5-DIPHENYLHYDANTOIN ON SOLUTION-PHASE CRYSTALLIZATION AND RELATED CRYSTAL PROPERTIES [J].
CHOW, AHL ;
HSIA, CK .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 75 (2-3) :219-230
[3]   Modification of phenytoin crystals .3. Influence of 3-butanoyloxymethyl-5,5-diphenylhydantoin on solution-phase crystallization and related crystal properties [J].
Chow, AHL ;
Gordon, JD ;
Szeitz, A ;
Young, JWM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 126 (1-2) :11-19
[4]   MODIFICATION OF ACETAMINOPHEN CRYSTALS - INFLUENCE OF GROWTH IN AQUEOUS-SOLUTIONS CONTAINING PARA-ACETOXYACETANILIDE ON CRYSTAL PROPERTIES [J].
CHOW, AHL ;
CHOW, PKK ;
WANG, ZS ;
GRANT, DJW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1985, 24 (2-3) :239-258
[5]  
Davey J.R., 1982, IND CRYSTALLIZATION, P123
[6]   A new pure paracetamol for direct compression: The orthorhombic form [J].
DiMartino, P ;
GuyotHermann, AM ;
Conflant, P ;
Drache, M ;
Guyot, JC .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1996, 128 (1-2) :1-8
[7]  
ELSAID Y, 1995, STP PHARMA SCI, V5, P232
[8]   COMPRESSION ABILITY IMPROVEMENT BY SOLVATION DESOLVATION PROCESS - APPLICATION TO PARACETAMOL FOR DIRECT COMPRESSION [J].
FACHAUX, JM ;
HERMANN, AMG ;
GUYOT, JC ;
CONFLANT, P ;
DRACHE, M ;
HUVENNE, JP ;
BOUCHE, R .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 99 (2-3) :99-107
[9]  
FAIRBROTHER J E, 1979, Journal of Pharmacy and Pharmacology, V31, p27P
[10]   CRYSTAL HABIT MODIFICATION OF A TABLET LUBRICANT, ADIPIC ACID [J].
FAIRBROTHER, JE ;
GRANT, DJW .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1978, 30 :P19-P19