Artesunate-clindamycin multi-kinetics and site-specific oral delivery system for antimalaric combination products.
The aim of this work was to study a multi-kinetics and site-specific oral antimalaria drug delivery system (MKS_DDS), containing artesunate and clindamycin, based on the Dome Matrix module assembly technology. The MKS_DDS assembled system comprises of four modules, i.e., two controlled release (CR) modules for delivery of 160 mg of clindamycin phosphate, one immediate release module containing 50 mg of artesunate and one immediate release module containing 80 mg of clindamycin phosphate. These modules have been assembled in stacked and void configurations. The void configuration is able to float and showed gastro-retentive behavior. The MKS_DDS was investigated for its mechanical characteristics, system behavior during release, drug release rate and mechanism. A bioavailability study (dogs) showed that the clindamycin plasma curve of the MKS_DDS system exhibited a quasi constant release rate, up to 8 h. The MKS_DDS system containing clindamycin and artesunate allows the use of one tablet containing one immediate release dose of artesunate and of clindamycin and a portion of clindamycin released over a prolonged time, by exploiting the gastro-retentive properties of a floating system.
Strusi
Orazio Luca
OL
BioPharmaNet, Department of Pharmacy, University of Parma, Viale G.P. Usberti 27/A, Parma, Italy.
Barata
Pedro
P
Traini
Daniela
D
Young
Paul M
PM
Mercuri
Salvatore
S
Colombo
Gaia
G
Sonvico
Fabio
F
Bettini
Ruggero
R
Colombo
Paolo
P
D000284:Administration, Oral; D000818:Animals; D000962:Antimalarials / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D037621:Artemisinins / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000077332:Artesunate; D001682:Biological Availability; D002981:Clindamycin / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D004285:Dogs; D004338:Drug Combinations; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D005753:Gastric Mucosa / Q000378:metabolism; D012995:Solubility
D000962:Antimalarials; D037621:Artemisinins; D003692:Delayed-Action Preparations; D004338:Drug Combinations; D002981:Clindamycin; D000077332:Artesunate