Formulation and in vivo evaluation of chlorhexidine buccal tablets prepared using drug-loaded chitosan microspheres

被引:115
作者
Giunchedi, P
Juliano, C
Gavini, E
Cossu, M
Sorrenti, M
机构
[1] Univ Sassari, Dipartimento Sci Farmaco, I-07100 Sassari, Italy
[2] Univ Pavia, Dipartimento Chim Farmaceut, I-27100 Pavia, Italy
关键词
chitosan microspheres; chlorhexidine; spray-drying; buccal tablets;
D O I
10.1016/S0939-6411(01)00237-5
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
This investigation deals with the development Of buccal formulations (tablets) based on chitosan microspheres containing chlorhexidine diacetate. The microparticles were prepared by a spray-drying technique, their morphological characteristics were studied by scanning electron microscopy and the in vitro release behaviour v,,as investigated in pH 7.0 USP buffer. Chlorhexidine in the chitosan microspheres dissolves more quickly in vitro than does chlorhexidine powder. The anti-microbial activity of the microparticles was investigated as minimum inhibitory concentration. minimum bacterial concentration and killing,, time. The loading of chlorhexidine into chitosan is able to maintain or improve the anti-microbial activity of the drug. The improvement is particularly high against Candida albicans. This is important for a formulation whose potential use is against buccal infections. Drug-empty microparticles have an anti-microbial activity due to the polymer itself. Buccal tablets were prepared by direct compression of the microparticles with mannitol alone or with sodium alginate, After their in vivo administration the determination of chlorhexidine in saliva showed the capacity of these formulations to give a prolonged release of the drug in the buccal cavity. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:233 / 239
页数:7
相关论文
共 24 条
[1]   THE EFFECTS OF THE INCORPORATION OF CHLORHEXIDINE ACETATE ON SOME PHYSICAL-PROPERTIES OF POLYMERIZED AND PLASTICIZED ACRYLICS [J].
ADDY, M ;
HANDLEY, R .
JOURNAL OF ORAL REHABILITATION, 1981, 8 (02) :155-163
[2]  
Edmundson I C, 1967, Adv Pharm Sci, V2, P95
[3]   Topical use of chitosan in ophthalmology: tolerance assessment and evaluation of precorneal retention [J].
Felt, O ;
Furrer, P ;
Mayer, JM ;
Plazonnet, B ;
Buri, P ;
Gurny, R .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 180 (02) :185-193
[4]   Chitosan microspheres with hydrocortisone and hydrocortisone-hydroxypropyl-β-cyclodextrin inclusion complex [J].
Filipovic-Grcic, J ;
Voinovich, D ;
Moneghini, M ;
Becirevic-Lacan, M ;
Magarotto, L ;
Jalsenjak, I .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2000, 9 (04) :373-379
[5]  
GENTA I, 1995, STP PHARMA SCI, V5, P202
[6]  
Giunchedi P, 2000, J MICROENCAPSUL, V17, P711
[7]  
GIUNCHEDI P, 1995, STP PHARMA SCI, V5, P276
[8]  
Giunchedi Paolo, 2000, Pharmacy and Pharmacology Communications, V6, P149
[9]   Chitosan microspheres prepared by spray drying [J].
He, P ;
Davis, SS ;
Illum, L .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1999, 187 (01) :53-65
[10]  
He P, 1999, J MICROENCAPSUL, V16, P343