Development of extended release matrices of rifampicin using hot melt extrusion technique.
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Date
2013-10
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Abstract
Tuberculosis has metamorphosized over the decades from drug resistant to multidrug resistant to the lethal
extensively drug resistant forms lately. With scarce newer anti-TB drugs emerging, there is a pressing need to
ameliorate the current treatment therapy by modulating the formulation approaches towards the first line
treatment drugs. In the present study an attempt has been made to formulate Rifampicin (RIF), the first line
treatment drug for TB as an extended release oral formulation using melt extrusion technique. The total dose of
RIF was divided into two components- Immediate release (IR) pellets of RIF as the loading dose (300mg) and
extended release tablet as the maintenance dose (150mg). Extrusion trials were conducted using various class of
extrudable polymers (cellulose, polyvinyl acetate, polyethylene oxide, poly(meth)acrylates). Based on the
preliminary findings, IR pellets were formulated using Eudragit EPO whereas hydroxylpropyl cellulose (HPC)
was further explored as the matrix former. The release rate was modified using addition of hydrophilic pH
independent release modifier. The formulation was characterized with respect to in vitro dissolution behavior,
thermal and chemical stability, miscibility, drug-polymer interactions and surface morphology followed by
stability studies. The loading dose could adequately release RIF initially whereas a combination of hydrophilic
pH independent polymer of varying viscosity could successfully control RIF release over 24 hours following zero
order release mechanism. The developed formulation exhibited content uniformity, physical and chemical
stability over a period of six months. The application of melt extrusion for developing extended release matrices
for anti-TB drugs like RIF was sought. Melt extrusion being a continuous manufacturing process could be scaled
up commercially thus enhancing the feasibility of the designed formulation.
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Keywords
Tuberculosis, Rifampicin, Extended release, Hot melt extrusion, Dissolution
Citation
Sharma Vanita J, Amin Purnima D. Development of extended release matrices of rifampicin using hot melt extrusion technique. Journal of Applied Pharmaceutical Science. 2013 Oct; 3(10): 30-38.