Bioavailability of norfloxacin from PEG 6000 solid dispersion and cyclodextrin inclusion complexes in rabbits

被引:23
作者
Fawaz, F [1 ]
Bonini, F [1 ]
Guyot, M [1 ]
Bildet, J [1 ]
Maury, M [1 ]
Lagueny, AM [1 ]
机构
[1] CREAPHARM,F-33186 LE HAILLAN,FRANCE
关键词
norfloxacin; beta-cyclodextrin; hydroxypropyl-alpha-cyclodextrin; PEG; 6000; solid dispersion; bioavailability;
D O I
10.1016/0378-5173(95)04387-X
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
A comparative bioavailability study was carried out in rabbits on pure powder of norfloxacin and its formulations: aqueous solution, polyethyleneglycol 6000 solid dispersions (PEG 6000 SD), beta-cyclodextrin (beta-CD) and hydroxypropyl-beta cyclodextrin (HP-beta-CD) complexes. Norfloxacin plasma concentrations were measured by HPLC method with a fluorimetric detection. Estimation of t(1/2) and k(e) proved that PEG 6000 SD and CD complexes did not modify the elimination characteristics of norfloxacin. Data from plasma concentration profiles indicated that absorption of norfloxacin from of SD and inclusion complexes was markedly accelerated when compared with powder of pure drug. The extent of absorption was significantly smaller with powder of norfloxacin than with its formulations. Bioavailability was improved and significantly higher with CD and complexes SD than with powder, but the improvement was lower than expected.
引用
收藏
页码:271 / 275
页数:5
相关论文
共 10 条
[1]   FORMULATION AND INVITRO-INVIVO CHARACTERIZATION OF SOLID DISPERSIONS OF PIROXICAM [J].
BHATTACHARYYA, M ;
BASU, SK ;
GUPTA, BK ;
GHOSAL, SK ;
MANDAL, SC ;
CHATTARAJ, SC .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1993, 19 (06) :739-747
[2]   DISSOLUTION, BIOAVAILABILITY AND ULCEROGENIC STUDIES ON SOLID DISPERSIONS OF INDOMETHACIN IN WATER-SOLUBLE CELLULOSE POLYMERS [J].
CHOWDARY, KPR ;
BABU, KVVS .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1994, 20 (05) :799-813
[3]   PREPARATION, CHARACTERIZATION AND DISSOLUTION OF CIPROFLOXACIN PEG-6000 BINARY-SYSTEMS [J].
FRANCES, C ;
VEIGA, MD ;
ESPANOL, OM ;
CADORNIGA, R .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1991, 77 (2-3) :193-198
[4]   PHYSICOCHEMICAL CHARACTERIZATION AND DISSOLUTION OF NORFLOXACIN/CYCLODEXTRIN INCLUSION-COMPOUNDS AND PEG SOLID DISPERSIONS [J].
GUYOT, M ;
FAWAZ, F ;
BILDET, J ;
BONINI, F ;
LAGUENY, AM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 123 (01) :53-63
[5]   BIOAVAILABILITY STUDY OF TOLBUTAMIDE BETA-CYCLODEXTRIN INCLUSION-COMPOUNDS, SOLID DISPERSIONS AND BULK POWDER [J].
KEDZIEREWICZ, F ;
ZINUTTI, C ;
HOFFMAN, M ;
MAINCENT, P .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 94 (1-3) :69-74
[6]   HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHY OF CIPROFLOXACIN AND ITS METABOLITES IN SERUM, URINE AND SPUTUM [J].
MYERS, CM ;
BLUMER, JL .
JOURNAL OF CHROMATOGRAPHY-BIOMEDICAL APPLICATIONS, 1987, 422 :153-164
[7]  
OTEROESPINAR FJ, 1991, INT J PHARM, V5, P37
[8]   BIOAVAILABILITY OF A POORLY WATER-SOLUBLE DRUG FROM TABLET AND SOLID DISPERSION IN HUMANS [J].
SHEEN, PC ;
KIM, SI ;
PETILLO, JJ ;
SERAJUDDIN, ATM .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1991, 80 (07) :712-714
[9]  
Szejtli J., 1988, CYCLODEXTRIN TECHNOL
[10]  
YAZAN Y, 1994, STP PHARMA SCI, V4, P128