Solid-state β-cyclodextrin complexes containing indomethacin, ammonia and water.: II.: Solubility studies

被引:26
作者
Casella, R
Williams, DA
Jambhekar, SS
机构
[1] Zeneca Inc, Zeneca Pharmaceut, Wilmington, DE 19850 USA
[2] Massachusetts Coll Pharm & Allied Hlth Sci, Div Pharmaceut Sci, Boston, MA 02115 USA
关键词
beta-cyclodextrin; indomethacin; solubility; dissolution; binding constant; crystallinity; enthalpy;
D O I
10.1016/S0378-5173(98)00003-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In a previous report five unique complexes were prepared and characterized containing beta-cyclodextrin, indomethacin, ammonia and water. In this study the solubility, dissolution behavior, complex-binding constant, crystallinity and enthalpy were assessed. The results show indomethacin solubility was improved by complex formation with beta-cyclodextrin. There was little difference among the various complex solubilities. Indomethacin dissolution was improved by complex formation with the exception of one complex. Indomethacin dissolution profiles were found to differ and were unrelated to either the complexed indomethacin content or binding constant. Indomethacin dissolution profiles were found to be related to the complex crystallinity and enthalpy. The complex-binding constants were found to support a theory reported previously that beta-cyclodextrin ring cavity solvation was the predominant factor responsible for complex formation. (C) 1998 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:15 / 22
页数:8
相关论文
共 15 条
[1]  
[Anonymous], 1990, US PHARM
[2]   ESTIMATION OF DEGREE OF CRYSTALLINITY IN DIGOXIN BY X-RAY AND IR METHODS [J].
BLACK, DB ;
LOVERING, EG .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1977, 29 (11) :684-687
[3]   Solid-state β-cyclodextrin complexes containing indomethacin, ammonia and water.: I.: Formation studies [J].
Casella, R ;
Williams, DA ;
Jambhekar, SS .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1998, 165 (01) :1-14
[4]  
Connors K. A., 1987, BINDING CONSTANTS, P261
[5]  
Cullity B. D., 1978, ELEMENTS XRAY DIFFRA, pp13
[6]  
Higuchi T., 1965, Interscience, New York, V4, P117
[7]  
IMAI T, 1988, CHEM PHARM BULL, V36, P354
[8]  
LACHMAN L, 1986, THEORY PRACTICE IND, P176
[9]  
MURTHY NS, 1982, AM LAB, V14, P70
[10]  
SEO H, 1983, CHEM PHARM BULL, V31, P286