Research Journal of Pharmacy and Technology

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Preparation, Evaluation and Development Celecoxib Prolonged Release (Pr) Tablets by Using Cellulose Polyacrylic Acid – Based Polymers


Affiliations
1 Department of General Pharmaceutical and Biomedical Technology, Medical Institute, Peoples' Friendship University of Russia, Моscow,, Russian Federation
     

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The aim of this research was formulation of celecoxib prolonged release matrix tablets and studying the influence of different types and concentration of polymers on release of drug. Seven formulations F1 – F7 were manually designed using different proportions and amount of polymers. The formulations of matrix tablets (F1 – F6) were composed of different polymers such as, hydroxypropyl methylcellulose (HPMC-K100M), carboxymethyl cellulose (CMC), ethylcellulose (EC-10 cps), Carbopol-940, hydroxypropyl cellulose high viscosity (HPCh), whereas (F7) standard formulation without polymer contained microcrystalline cellulose (MCC), lactose monohydrate, sodium lauryl sulfate (SLS) and polyvinylpyrrolidone (PVP-K30). The MCC and PVP-K30 were used in a fixed quantity in all formulations except F9 in proportions, 21.66% and 3.33%, respectively. Dissolution test was performed in phosphate buffer of pH 7.4, because cellulose polymers are insoluble in gastric fluid and celecoxib is very slightly soluble in gastric fluid. Dissolution profiles indicated that formulations F1, F2 and F3 extended the drug release up to 16h. MS Excel was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Higuchi and Korsmeyer–Peppas models. Formulation (F1) containing HPMC–K100M as a matrix former showed drug release as highest correlation coefficient (R2) values obtained when higuchi-order model was applied (R2 = 0.9316). While formulation (F2) containing HPMC–K100M and EC showed the highest correlation coefficient (R2) values when first-order model was applied (R2 = 0.9534). Whereas, formulation (F3) containing HPMC – K100M and CMC as a matrix former showed concentration-independent drug release as highest linearity was observed when zero-order model was applied (R2 = 0.9869). Active substance was released from all formulations by Case II relaxation mechanism. The present study showed that cellulose polyacrylic acid – based polymers can be used successfully to develop prolonged release matrix tablet formulation.

Keywords

Celecoxib, HPMC, Ethylcellulose, Carboxymethyl cellulose, Prolonged release.
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  • Preparation, Evaluation and Development Celecoxib Prolonged Release (Pr) Tablets by Using Cellulose Polyacrylic Acid – Based Polymers

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Authors

Svetlana Suslina
Department of General Pharmaceutical and Biomedical Technology, Medical Institute, Peoples' Friendship University of Russia, Моscow,, Russian Federation
Аhmed Alkhodri
Department of General Pharmaceutical and Biomedical Technology, Medical Institute, Peoples' Friendship University of Russia, Моscow,, Russian Federation

Abstract


The aim of this research was formulation of celecoxib prolonged release matrix tablets and studying the influence of different types and concentration of polymers on release of drug. Seven formulations F1 – F7 were manually designed using different proportions and amount of polymers. The formulations of matrix tablets (F1 – F6) were composed of different polymers such as, hydroxypropyl methylcellulose (HPMC-K100M), carboxymethyl cellulose (CMC), ethylcellulose (EC-10 cps), Carbopol-940, hydroxypropyl cellulose high viscosity (HPCh), whereas (F7) standard formulation without polymer contained microcrystalline cellulose (MCC), lactose monohydrate, sodium lauryl sulfate (SLS) and polyvinylpyrrolidone (PVP-K30). The MCC and PVP-K30 were used in a fixed quantity in all formulations except F9 in proportions, 21.66% and 3.33%, respectively. Dissolution test was performed in phosphate buffer of pH 7.4, because cellulose polymers are insoluble in gastric fluid and celecoxib is very slightly soluble in gastric fluid. Dissolution profiles indicated that formulations F1, F2 and F3 extended the drug release up to 16h. MS Excel was used to analyze the dissolution profile data for drug release kinetics such as first order, Zero-order, Higuchi and Korsmeyer–Peppas models. Formulation (F1) containing HPMC–K100M as a matrix former showed drug release as highest correlation coefficient (R2) values obtained when higuchi-order model was applied (R2 = 0.9316). While formulation (F2) containing HPMC–K100M and EC showed the highest correlation coefficient (R2) values when first-order model was applied (R2 = 0.9534). Whereas, formulation (F3) containing HPMC – K100M and CMC as a matrix former showed concentration-independent drug release as highest linearity was observed when zero-order model was applied (R2 = 0.9869). Active substance was released from all formulations by Case II relaxation mechanism. The present study showed that cellulose polyacrylic acid – based polymers can be used successfully to develop prolonged release matrix tablet formulation.

Keywords


Celecoxib, HPMC, Ethylcellulose, Carboxymethyl cellulose, Prolonged release.

References