Artesunate-clindamycin multi-kinetics and site-specific oral delivery system for antimalaric combination products

作者：Strusi Orazio Luca; Barata Pedro; Traini Daniela; Young Paul M; Mercuri Salvatore; Colombo Gaia; Sonvico Fabio; Bettini Ruggero; Colombo Paolo^*

来源：Journal of Controlled Release, 2010, 146(1): 54-60.

DOI：10.1016/j.jconrel.2010.05.001

• Clindamycin
• Artesunate
• Malaria combination therapy
• Release module assemblage
• Floating dosage form

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 8h.
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.

• 出版日期2010-8-17