Synthesis and enzymatic degradation of epichlorohydrin cross-linked pectins

被引:12
作者
Semdé, R
Moës, AJ
Devleeschouwer, MJ
Amighi, K
机构
[1] Free Univ Brussels, Inst Pharm, Lab Pharmaceut & Biopharmaceut, B-1050 Brussels, Belgium
[2] Univ Ouagadougou, UFR SDS, Lab Pharmaceut & Biopharmaceut, Ouaga, Burkina Faso
[3] Free Univ Brussels, Inst Pharm, Lab Microbiol & Hyg, B-1050 Brussels, Belgium
关键词
epichlorohydrin; cross-linked pectins; colonic drug delivery; enzymatic degradation;
D O I
10.1081/DDC-120016728
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The water solubility of pectin was successfully decreased by cross-linking with increasing amounts of epichlorohydrin in the reaction media. The initial molar ratios of epichlorohydrin/galacturonic acid monomer in the reaction mixtures were 0, 0.37, 0.56, 0.74, 1.00, 1.47, and 2.44. The resulting epichlorohydrin cross-linked pectins were thus referred to as C-LP0, C-LP37, C-LP56, C-LP75, C-LP100, C-LP150, and C-LP250, respectively. Methoxylation degrees ranged from 60.5 +/- 0.9% to 68.0 +/- 0.6%, and the effective cross-linking degrees, determined by quantification of the hydroxyl anions consumed during the reaction, were 0, 17.8, 26.0, 38.3, 46.5, 53.5, and 58.7%, respectively. After incubating the different cross-linked pectins (0.5% w/v) in 25 mL of 0.05 M acetate-phosphate buffer (pH 4.5), containing 50 muL of Pectinex(R) Ultra SP-L (pectinolytic enzymes), between 60 and 80% of the pectin osidic bounds were broken in less than 1 hr. Moreover, increasing the cross-linking degree only resulted in a weak slowing on the enzymatic degradation velocity.
引用
收藏
页码:203 / 213
页数:11
相关论文
共 29 条
[1]   SPLITTING OF PECTIN CHAIN MOLECULES IN NEUTRAL SOLUTIONS [J].
ALBERSHEIM, P ;
NEUKOM, H ;
DEUEL, H .
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS, 1960, 90 (01) :46-51
[2]   AN EVALUATION OF PECTIN AS A CARRIER FOR DRUG TARGETING TO THE COLON [J].
ASHFORD, M ;
FELL, J ;
ATTWOOD, D ;
SHARMA, H ;
WOODHEAD, P .
JOURNAL OF CONTROLLED RELEASE, 1993, 26 (03) :213-220
[3]   STUDIES ON PECTIN FORMULATIONS FOR COLONIC DRUG-DELIVERY [J].
ASHFORD, M ;
FELL, J ;
ATTWOOD, D ;
SHARMA, H ;
WOODHEAD, P .
JOURNAL OF CONTROLLED RELEASE, 1994, 30 (03) :225-232
[4]   Cross-linked cellulose as a tablet excipient: A binding/disintegrating agent [J].
Chebli, C ;
Cartilier, L .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1998, 171 (01) :101-110
[5]   DIGESTION OF PECTIN IN THE HUMAN GUT AND ITS EFFECT ON CALCIUM-ABSORPTION AND LARGE BOWEL FUNCTION [J].
CUMMINGS, JH ;
SOUTHGATE, DAT ;
BRANCH, WJ ;
WIGGINS, HS ;
HOUSTON, H ;
JENKINS, DJA ;
JIVRAJ, T ;
HILL, MJ .
BRITISH JOURNAL OF NUTRITION, 1979, 41 (03) :477-485
[6]   CHROMATOGRAPHIE VON PEKTINEN MIT VERSCHIEDENER VERTEILUNG DER METHYLESTER-GRUPPEN AUF DEN FADENMOLEKELN .16. UBER IONENAUSTAUSCHER [J].
HERI, W ;
DEUEL, H ;
NEUKOM, H .
HELVETICA CHIMICA ACTA, 1961, 44 (07) :1945-&
[7]   Cross-linked high amylose starch for controlled release of drugs: recent advances [J].
Lenaerts, V ;
Moussa, I ;
Dumoulin, Y ;
Mebsout, F ;
Chouinard, F ;
Szabo, P ;
Mateescu, MA ;
Cartilier, L ;
Marchessault, R .
JOURNAL OF CONTROLLED RELEASE, 1998, 53 (1-3) :225-234
[8]   Studies on the physical properties of mixed pectin/ethylcellulose films intended for colonic drug delivery [J].
Macleod, GS ;
Fell, JT ;
Collett, JH .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1997, 157 (01) :53-60
[9]   INDUSTRIAL PECTINS - SOURCES, PRODUCTION AND APPLICATIONS [J].
MAY, CD .
CARBOHYDRATE POLYMERS, 1990, 12 (01) :79-99
[10]  
Nelson N, 1944, J BIOL CHEM, V153, P375