Preparation of alginate beads for floating drug delivery system:: effects of CO2 gas-forming agents

被引:216
作者
Choi, BY
Park, HJ [1 ]
Hwang, SJ
Park, JB
机构
[1] Korea Univ, Grad Sch Biotechnol, Seoul 136701, South Korea
[2] Chungnam Natl Univ, Coll Pharm, Taejon 305764, South Korea
[3] Sama Pharm Co Ltd, Uiwang 437821, Kyonggi, South Korea
关键词
alginate bead; floating bead; floating drug dosage system (FDDS); gas-forming agent; NaHCO3; CaCO3;
D O I
10.1016/S0378-5173(02)00054-6
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Floating beads were prepared from a sodium alginate solution containing CaCO3 or NaHCO3 as gas-forming agents. The solution was dropped to 1% CaCl2 solution containing 10% acetic acid for CO2 gas and gel formation. The effects of gas-forming agents on bead size and floating properties were investigated. As gas-forming agents increased, the size and floating properties increased. Bead porosity and volume average pore size, as well as the L surface and cross-sectional morphology of the beads were examined with Mercury porosimetry and Scanning Electron Microscopy. NaHCO3 significantly increased porosity and pore diameter than CaCO3. Incorporation of CaCO3 into alginate Solution resulted in smoother beads than those produced with NaHCO3. Gel strength analysis indicated that bead strength decreased with increasing gas-forming agent from 9 to 4 N. Beads incorporating CaCO3 exhibited significantly increased get strength over control and NaHCO3-containing samples. Release characteristics of riboflavin as a model drug were Studied in vitro. Release rate of riboflavin increased proportionally with addition of NaHCO3. However, increasing weight ratios of CaCO3 did not appreciably accelerate drug release. The results of these Studies indicate that CaCO3 is superior to NaHCO3 us a gas forming agent in alginate bead preparations. The enhanced buoyancy and sustained release properties of CaCO3-containing beads make them an excellent candidate for floating drug dosage systems (FDDS). (C) 2002 Published by Elsevier Science B.V.
引用
收藏
页码:81 / 91
页数:11
相关论文
共 32 条
[21]   Controlled release of clot-dissolving tissue-type plasminogen activator from a poly(L-glutamic acid) semi-interpenetrating polymer network hydrogel [J].
Park, YJ ;
Liang, JF ;
Yang, ZQ ;
Yang, VC .
JOURNAL OF CONTROLLED RELEASE, 2001, 75 (1-2) :37-44
[22]   Evaluation and comparison of dissolution data derived from different modified release dosage forms: an alternative method [J].
Pillay, V ;
Fassihi, R .
JOURNAL OF CONTROLLED RELEASE, 1998, 55 (01) :45-55
[23]   A physico-chemical approach to production of alginate beads by emulsification-internal ionotropic gelation [J].
Poncelet, D ;
Babak, V ;
Dulieu, C ;
Picot, A .
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS, 1999, 155 (2-3) :171-176
[24]  
Rouge N, 1998, Pharm Acta Helv, V73, P81, DOI 10.1016/S0031-6865(97)00050-2
[25]   Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery [J].
Rouge, N ;
Buri, P ;
Doelker, E .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1996, 136 (1-2) :117-139
[26]   Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention [J].
Singh, BN ;
Kim, KH .
JOURNAL OF CONTROLLED RELEASE, 2000, 63 (03) :235-259
[27]   EFFECT OF DIVALENT METALS ON PROPERTIES OF ALGINATE SOLUTIONS .I. CALCIUM IONS [J].
SMIDSROD, O ;
HAUG, A .
ACTA CHEMICA SCANDINAVICA, 1965, 19 (02) :329-&
[28]   Encapsulation of probiotic bacteria with alginate-starch and evaluation of survival in simulated gastrointestinal conditions and in yoghurt [J].
Sultana, K ;
Godward, G ;
Reynolds, N ;
Arumugaswamy, R ;
Peiris, P ;
Kailasapathy, K .
INTERNATIONAL JOURNAL OF FOOD MICROBIOLOGY, 2000, 62 (1-2) :47-55
[29]   ORAL SUSTAINED-RELEASE DRUG DELIVERY SYSTEMS USING POLYCARBONATE MICROSPHERES CAPABLE OF FLOATING ON THE GASTRIC FLUID [J].
THANOO, BC ;
SUNNY, MC ;
JAYAKRISHNAN, A .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1993, 45 (01) :21-24
[30]   FACTORS CONTROLLING THE BUOYANCY AND GASTRIC RETENTION CAPABILITIES OF FLOATING MATRIX CAPSULES - NEW DATA FOR RECONSIDERING THE CONTROVERSY [J].
TIMMERMANS, J ;
MOES, AJ .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1994, 83 (01) :18-24