Spray-dried lactose composite particles containing an ion complex of alginate-chitosan for designing a dry-coated tablet having a time-controlled releasing function.
OBJECTIVE
The properties of novel spray-dried lactose composite particles suitable for the coating filler of a dry-coated tablet having a long induction period in drug release were investigated.


METHODS
To prepare spray-dried composite particles containing alginate-chitosan complex (SD(L/AL-CS)), an aqueous solution of lactose and sodium alginate and the acetic acid solution of chitosan were concomitantly fed into the rotary atomizer of a spray-dryer. The formation of the alginate-chitosan complex was confirmed by measuring the weight of insoluble portion in the mixture of sodium alginate and chitosan solutions. The dissolution properties of the dry-coated tablet were measured with the JP specified paddle method.


RESULTS
The micromeritic properties of SD(L/AL-CS) were compared to those of the SD composite particles of lactose-sodium alginate, having a good compacting property. The drug release profiles of dry-coated tablet with SD(L/AL-CS) contained a long induction period followed by a rapid drug release phase in the artificial intestinal fluid. The induction period for drug release to occur was increased with an increase in the degree of deacetylation of chitosan and in the amount of chitosan in the formulation. The prolongation of induction period was attributed to the formation of an insoluble ion complex between sodium alginate and chitosan in the composite particles, which could form a rigid gel structure on the tablet surface.


CONCLUSIONS
A time-controlled release tablet was designed with the composite particles of lactose containing the alginate-chitosan ion complex. The induction period of the dry-coated tablet could be prolonged in order to deliver the drug to the colon by controlling the type and amount of chitosan formulated in the composite particles.
Takeuchi
H
H
Gifu Pharmaceutical University, Japan.
Yasuji
T
T
Yamamoto
H
H
Kawashima
Y
Y
D000464:Alginates / Q000494:pharmacology*; D002686:Chitin / Q000031:analogs & derivatives* / Q000494:pharmacology; D048271:Chitosan; D003106:Colon / Q000378:metabolism; D016503:Drug Delivery Systems; D020723:Glucuronic Acid; D006603:Hexuronic Acids; D007785:Lactose / Q000494:pharmacology*; D013607:Tablets
D000464:Alginates; D006603:Hexuronic Acids; D013607:Tablets; D002686:Chitin; D020723:Glucuronic Acid; D048271:Chitosan; D007785:Lactose