GLASS-FORMATION OF 4''-O-(4-METHOXYPHENYL)ACETYLTYLOSIN AND PHYSICOCHEMICAL STABILITY OF THE AMORPHOUS SOLID

被引:25
作者
YAMAGUCHI, T
NISHIMURA, M
OKAMOTO, R
TAKEUCHI, T
YAMAMOTO, K
机构
[1] INST MICROBIAL CHEM,SHINAGAWA KU,TOKYO 141,JAPAN
[2] CHIBA UNIV,FAC PHARMACEUT SCI,INAGE KU,CHIBA 263,JAPAN
关键词
4''-O-(4-METHOXYPHENYL)ACETYLTYLOSIN; AMORPHOUS SOLID; SPRAY DRYING; GLASSY STATE; GLASS TRANSITION TEMPERATURE; RECRYSTALLIZATION TEMPERATURE; STABILITY;
D O I
10.1016/0378-5173(92)90137-Q
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Glass formation of 4"-O-(4-methoxyphenyl)acetyltylosin (MAT) and the physicochemical stability of amorphous MAT have been investigated. The amorphous form of MAT was prepared by spray drying of an MAT dichloromethane solution. The glassy state was confirmed by DSC and the glass transition temperature was observed to be 102-103-degrees-C. It was found that different kinds of the glassy state of MAT could be obtained by changing the inlet temperature of spray drying. Storage experiments on amorphous powders at 40-degrees-C and 75% RH revealed that the amorphous powders prepared at a temperature between the glass transition (T(g)) and recrystallization (T(c)) temperatures were the most stable. A correlation between the stability and the apparent density was observed.
引用
收藏
页码:87 / 96
页数:10
相关论文
共 20 条
[1]  
AOYAGI N, 1985, INT J CLIN PHARM TH, V23, P529
[2]  
AOYAGI N, 1985, INT J CLIN PHARM TH, V23, P469
[3]  
BABA K, 1990, CHEM PHARM BULL, V38, P2542
[4]  
BALLARD BE, 1962, J PHARMACOL EXP THER, V135, P120
[5]  
EGAWA H, 1992, CHEM PHARM BULL, V40, P819
[6]  
FUKUOKA E, 1986, CHEM PHARM BULL, V34, P4314
[7]  
FUKUOKA E, 1989, CHEM PHARM BULL, V37, P1047
[8]  
FUKUOKA E, 1989, CHEM PHARM BULL, V37, P2782
[9]  
GOLDSTEIN M, 1976, ANN NY ACAD SCI, V279
[10]   PHARMACEUTICAL APPLICATIONS OF POLYMORPHISM [J].
HALEBLIAN, J ;
MCCRONE, W .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1969, 58 (08) :911-+