Research Journal of Pharmacy and Technology

Open Access Open Access  Restricted Access Subscription Access
Open Access Open Access Open Access  Restricted Access Restricted Access Subscription Access

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
     

   Subscribe/Renew Journal


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.
Subscription Login to verify subscription
User
Notifications
Font Size


  • Adilakshmi, D. et al. Simultaneous Formulation, Estimation and Evaluation of Allopurinol Sustained Release Tablets using various suitable Excipients. Asian Journal of Pharmaceutical Analysis. 2016; 6(3), 155-166. DOI: 10.5958/2231-5675.2016.00025.9

  • James, H. P. et al. Smart polymers for the controlled delivery of drugs–a concise overview. Acta Pharmaceutica Sinica B. 2014; 4(2), 120-127. doi: 10.1016/j.apsb.2014.02.005

  • Salve, P. et al. Development and Evaluation of Sustained Release Dosage Form using Hydrophilic and Hydrophobic Materials. Research Journal of Pharmacy and Technology. 2016; 9(5), 481-489. DOI: 10.5958/0974-360X.2016.00089.5

  • Ismail, R. et al. Formulation and in vitro evaluation of once-daily methyldopa sustained release matrix tablets. Research Journal of Pharmacy and Technology. 2015; 8(2), 161-166. DOI: 10.5958/0974-360X.2015.00029.3

  • Madhukar, G. A. et al. Optimization of Various Grades of HPMC for Development of Sustained Release Matrix Tablets of Theophylline. Asian Journal of Pharmacy and Technology. 2017; 7(1), 19-26. DOI: 10.5958/2231-5713.2017.00004.6

  • Qi, X. et al. Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. International Journal of Pharmaceutics. 2015; 489(1-2), 210-217. doi: 10.1016/j.ijpharm.2015.05.007

  • Abdulhameed, K. A. A., & Salih, N. A. Controlled Release of Cefixime using Sodium Carboxymethyl Cellulose Polymer. Research Journal of Pharmacy and Technology. 2019; 12(9), 4073-4079. DOI: 10.5958/0974-360X.2019.00701.7

  • Perez-Marcos, B. et al. Mechanical and drug-release properties of atenolol-carbomer hydrophilic matrix tablets. Journal of Controlled Release. 1991; 17(3), 267-276. doi: 10.1016/0168-3659(91)90145-4

  • World health organization (WHO). Musculoskeletal conditions. Available at: https://www.who.int/news-room/fact-sheets/detail/musculoskeletal-conditions (дата обращения – 08.02.2021) 10. Thimmasetty, J. et al. Solubility parameter estimation of celecoxib by current methods. Asian Journal of Research in Chemistry. 2009; 2(2), 188-195.

  • Terse, P., and Mallya, R. Formulation and Evaluation of Celecoxib loaded colon Targeted Microsponges. Asian Journal of Research in Pharmaceutical Science. 2020; 10(2), 73-78. DOI: 10.5958/2231-5659.2020.00014.4

  • Paulson, S. K. et al. Pharmacokinetics of celecoxib after oral administration in dogs and humans: effect of food and site of absorption. Journal of Pharmacology and Experimental Therapeutics. 2001; 297(2), 638-645.

  • Gong, L. et al. Celecoxib pathways: pharmacokinetics and pharmacodynamics. Pharmacogenetics and Genomics. 2012; 22(4), 310-318. doi: 10.1097/FPC.0b013e32834f94cb

  • USP 41- NF36 (2018) The United States Pharmacopeial Convention, USA.

  • Mathur N. et al. Evaluation of quality control parameters on various brands of paracetamol tablet formulation. World J Pharm Pharmaceut Sci. 2015; 4(7):976–984.

  • Ravi, G. et al. Development and Evaluation of oral controlled release tablets of oxybutynin using various polymers. Research Journal of Pharmacy and Technology. 2020; 13(8), 3854-3860. DOI: 10.5958/0974-360X.2020.00682.4

  • Saha, R. N. et al. Determination of celecoxib in pharmaceutical formulations using UV spectrophotometry and liquid chromatography. Journal of Pharmaceutical and Biomedical Analysis. 2002; 28(3-4), 741-751. doi: 10.1016/S0731-7085(01)00678-1

  • Mandale, T. R. et al Development and validation of analytical method for simultaneous estimation of amlodipine besylate and celecoxib in pure and combined dosage form. Research Journal of Pharmacy and Technology. 2020; 13(9), 4280-4284. DOI: 10.5958/0974-360X.2020.00756.8

  • Hamed, R., and Omran, H. Development of dual–release pellets of the non-steroidal anti–inflammatory drug celecoxib. Journal of Drug Delivery Science and Technology. 2020; 55. doi: 10.1016/j.jddst.2019.101419

  • Biswas, B. K. et al. In vitro release kinetic study of esomeprazole magnesium from methocel K15M and methocel K100 LVCR matrix tablets. Dhaka University Journal of Pharmaceutical Sciences. 2008; 7(1), 39-45. doi.org/10.3329/dujps.v7i1.1216

  • Wise DL. Handbook of Pharmaceutical Controlled Release Technology. UK: CRC press, (2000). 902 P. ISBN 9780824703691

  • Tiwari, S.B. et al. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmSciTech. 2003; 4, 18–23. doi: 10.1208/pt040331

  • Sawant, V. A. et al. In-Vitro Release Kinetic Study of Mosapride Citrate Dihydrate from Sustained Release Matrix Tablet Containing Two Different Viscosity Grades of HPMC. Research Journal of Pharmaceutical Dosage Forms and Technology. 2009; 1(3), 207-212.

  • Iwata, M., & Ueda, H. Dissolution properties of glibenclamide in combinations with polyvinylpyrrolidone. Drug Development and Industrial Pharmacy. 1996; 22(11), 1161-1165. doi: 10.3109/03639049609065953

  • Ejikeme, P.M. Investigation of the physicochemical properties of microcrystalline cellulose from agricultural wastes I: orange mesocarp. Cellulose. 2008; 15, 141–147. doi: 10.1007/s10570-007-9147-7

  • Saeio, K. et al. Factors influencing drug dissolution characteristic from hydrophilic polymer matrix tablet. Scientia Pharmaceutica. 2007; 75(4), 147-164. doi: 10.3797/scipharm.2007.75.147

  • Maharjan, S. et al. Formulation and Evaluation of sustained release Sodium Alginate beads of Indomethacin. Asian Journal of Pharmacy and Technology. 2019; 9(3), 165-172. DOI: 10.5958/2231-5713.2019.00028.X

  • Sareen, R. et al. Meloxicam carbopol-based gels: characterization and evaluation. Current Drug Delivery. 2011; 8(4), 407-415.

  • Mostafavi, A. et al. Development of a prolonged-release gastroretentive tablet formulation of ciprofloxacin hydrochloride: Pharmacokinetic characterization in healthy human volunteers. International Journal of Pharmaceutics. 2011; 409(1-2), 128-136. doi: 10.1016/j.ijpharm. 2011.02. 035


Abstract Views: 276

PDF Views: 0




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

Abstract Views: 276  |  PDF Views: 0

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