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Optimization of Sustained Release Paliperidone Matrix Tablet

Basavaraj K. Nanjwade, Ritesh Udhani, Jatin Popat

Department of Pharmaceutics, KLE University’s College of Pharmacy, JN Medical College, Belgaum, Karnataka, India

Corresponding author: Dr. Basavaraj K. Nanjwade, Department of Pharmaceutics, KLE University’s College of Pharmacy JNMC Campus, Belgaum-590010 Karnataka (India), e-mail: bknanjwade@yahoo.com

The purpose of the study was to formulate paliperidone sustained release matrix tablet using hydrophilic polymers. The effect of hydroxypropylmethylcellulose (HPMC) and polyethylene oxide (PEO) on drug release was investigated. A 3² full factorial design was designed to optimize the drug release profile and to study the effect of independent variables, amount of hydroxypropylmethylcellulose (X1) and amount of polyethylene oxide (X2) on dependent variables, i. e. percentage drug release after 2 h (Y1), after 6 h (Y2), and after 10 h (Y3). A mathematical model was generated after each response parameter. The mathematical model allowed to plot response surface curves and to determine optimal preparation conditions. Hydrophilic matrix of HPMC and PEO in combination sustained the drug release effectively for more than 12 h. The results of regression analysis showed that all the coefficients bear a different sign, which indicate that both the polymers show different effects on the release of drug. The drug release profiles were characterized by initial burst effect of release and then sustaining the release for up to 12 h. The in vitro release profiles of the drug from the optimized formulation could be best expressed by Higuchi’s equation, as the plots showed high linearity (R² = 0.980). From the Peppas model, however, the n value appeared small, which indicated a coupling of diffusion and erosion mechanisms, so called anomalous diffusion.

Key words Anomalous diffusion • 3² Full factorial design • Paliperidone • Regression analysis • Response surface curves