Research Article
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Optimization of HPMC Loaded Paroxetine HCl Controlled Release Matrix Tablet by Central Composite Design

Year 2024, , 289 - 305, 01.12.2024
https://doi.org/10.52794/hujpharm.1460738

Abstract

The main aim of the present study was to improve the release profile of Paroxetine (PXT) using Novel Drug Delivery System (NDDS). Therefore, Controlled Release Matrix tablet of PXT was prepared to extend the release of the drug from 8 hours to 12 hours. In the present research work, controlled release matrix tablet of paroxetine (PXT) was prepared by wet granulation method using various polymer grades of Hydroxypropyl methylcellulose (HPMC) and Polyvinylpyrrolidone (PVP) like HPMC K100M, HPMC K4M, HPMC K100M LV, and PVP K-30. Central Composite Design was applied to optimize the amount of polymers in the tablet. Infrared Spectroscopic analysis was done to check the interaction between drug and polymers. Results showed that all pre-compression and post-compression parameters were as per standard limits and not deviated when compared with the marketed formulation. The release profile of the tablet formulated using optimized batch was also improved significantly. Specifically, PXT matrix tablet released approximately 29.382%, 41.29%, and 93.47% of the drug at the second, fourth, and twelfth hours, respectively. In conclusion, the dissolution profile of the optimized batch aligns closely with the established USP guidelines for PXT extended-release formulations.

References

  • 1. Nokhodchi A, Raja S, Patel P, Asare-Addo K. The role of oral controlled release matrix tablets in drug delivery systems. BioImpact. 2012; 2(4):175-187. https://doi.org/10.5681%2Fbi.2012.027
  • 2. Agarwal P, Semimul A. A comprehensive review on sustained release matrix tablets: a promising dosage form. Universal J Pharm Res. 2018;3(6):49–54. https://doi.org/10.22270/ujpr.v3i6.222
  • 3. Yang Y, Huang Z, Zhang X, Li J, Huang Y, Chen W, Pan X, Wu C. Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 3² Factorial Design. Pharmaceutics. 2018;10(4): 243. https://doi.org/10.3390/pharmaceutics10040243
  • 4. Davis BA, Nagarajan A, Forrest LR, Singh S K. Mechanism of Paroxetine (Paxil) Inhibition of the Serotonin Transporter. Sci Report. 2016;6:23789. https://doi.org/10.1038/srep23789
  • 5. Rajesh HJ, Shashikiran YH, Anu PA, Priyanka RG. Review on Sustain Release Matrix Tablets. World J Pharm Pharm Sci. 2021;10(11):545-553
  • 6. Khan R, Ashraf MS, Afzal M, Kazmi I, Jahangir MA, Singh R. Formulation and evaluation of sustained release matrix tablet of rabeprazole using wet granulation technique. J Pharm Bioal Sci. 2014;6(3):180-184. https://doi.org/10.4103%2F0975-7406.130961
  • 7. Madgulkar AR, Bhalekar MR, Kolhe VJ, Kenjale YD. Formulation and optimization of sustained release tablets of venlafaxine resinates using response surface methodology. Indian J Pharm Sci. 2009;71(4):387-394. https://doi.org/10.4103%2F0250-474X.57287
  • 8. Mortazavi SA, Jafariazar Z, Ghadjahani Y, Mahmoodi H, Mehtarpour F. Formulation and In vitro Characterization of Sustained Release Matrix Type Ocular Timolol Maleate Mini-Tablet. Iranian J Pharm Res. 2014;13(1), 19–27
  • 9. Sheskey PJ, Robb RT, Moore RD, Boyce BM. Effects of lubricant level, method of mixing, and duration of mixing on a controlled-release matrix tablet containing hydroxypropyl methylcellulose. Drug Develop Ind Pharm. 1995;21(19):2151–2165. https://doi.org/10.3109/03639049509065898
  • 10. Bravo SA, Lamas MC, Salomón CJ. In vitro studies of diclofenac sodium controlled-release from biopolymeric hydrophilic matrices. J Pharm Pharm Sci. (2002); 5(3):213–219.
  • 11. Shah VP, Gurbarg M, Noory A, Dighe S, Skelly JP. Influence of higher rates of agitation on release patterns of immediate-release drug products. J Pharm Sci. 1992;81(6) 500–503. https://doi.org/10.1002/jps.2600810604
  • 12. Nair A, Gupta R, Vasanti S. In vitro controlled release of alfuzosin hydrochloride using HPMC-based matrix tablets and its comparison with marketed product. Pharm Develop Technol. 2007;12(6):621–625. https://doi.org/10.1080/10837450701563277
  • 13. Ravi PR, Kotreka UK, Saha RN. Controlled release matrix tablets of zidovudine: effect of formulation variables on the in vitro drug release kinetics. AAPS Pharm SciTech. 2008;9(1):302–313. https://doi.org/10.1208/s12249-007-9030-8
  • 14. Patel H, Panchal DR, Patel U, Brahmbhatt T, Suthar M. Matrix type drug delivery system: A review. J Pharm Sci Biosci Res. 2011; 1(3):143–151
  • 15. Bang LM, Keating GM. Paroxetine Controlled Release. CNS Drugs. 2004; 18, 355–364. https://doi.org/10.2165/00023210-200418060-00003
  • 16. Aulton ME. Aulton’s Pharmaceutics: The design and manufacture of medicine. 3rd Edition. Churchil livingstone, Elsevier, UK, 2008
  • 17. Lachman L, Liberman HA, Kanig JL. The theory and practice of industrial pharmacy. 3rd Edition. Varghese Publishing House, Bombay, India. 1991
  • 18. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52(12):1145–1149. https://doi.org/10.1002/jps.2600521210
  • 19. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15(1):25-35. https://doi.org/10.1016/0378-5173(83)90064-9
  • 20. Lieberman HA, Lachman L. Pharmaceutical Dosage Forms. In: Dekker M (ed) Tablet 1980.75-128
  • 21. Bushra R, Shoaib MH, Ali H, Zafar F, Naeem MI, Aslam N. Formulation design and optimization of aceclofenac tablets (100 mg) using central composite design with response surface methodology. Lat Am J Pharm. 2014;33(6):1009–1018
  • 22. Barsagade P, Khetade R, Nirwan K, Agrawal T, Gotafode S, Lade U. Review Article of Dissolution Test Method Development and Validation of Dosage Form by Using RP-HPLC. Int J Pharm Sci Rev Res. 2021; 70(1):28-38 https://dx.doi.org/10.47583/ijpsrr.2021.v70i01.005
  • 23. Kunamaneni P, Kovvasu SP, Janjanam KC. Formulation and optimization of controlled release paroxetine hydrochloride tablets using response surface methodology. J Global Trend Pharm Sci. 2016; 7(4):3520–3534
  • 24. Thirumaran M, Balakumar K, Vijaya Raghavan C, Thuvaragan S. Formulation and in vitro release kinetic study of an enteric coated paroxetine-controlled release tablets. Asian J Res Chem Pharm Sci. 2014; 2(2):63-73
  • 25. Avachat A, Kotwal V. Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulphate. AAPS Pharm SciTech. 2007; 8(4):51–56. https://doi.org/10.1208/pt0804088

Optimization of HPMC Loaded Paroxetine HCl Controlled Release Matrix Tablet by Central Composite Design

Year 2024, , 289 - 305, 01.12.2024
https://doi.org/10.52794/hujpharm.1460738

Abstract

The main aim of the present study was to improve the release profile of Paroxetine (PXT) using Novel Drug Delivery System (NDDS). Therefore, Controlled Release Matrix tablet of PXT was prepared to extend the release of the drug from 8 hours to 12 hours. In the present research work, controlled release matrix tablet of paroxetine (PXT) was prepared by wet granulation method using various polymer grades of Hydroxypropyl methylcellulose (HPMC) and Polyvinylpyrrolidone (PVP) like HPMC K100M, HPMC K4M, HPMC K100M LV, and PVP K-30. Central Composite Design was applied to optimize the amount of polymers in the tablet. Infrared Spectroscopic analysis was done to check the interaction between drug and polymers. Results showed that all pre-compression and post-compression parameters were as per standard limits and not deviated when compared with the marketed formulation. The release profile of the tablet formulated using optimized batch was also improved significantly. Specifically, PXT matrix tablet released approximately 29.382%, 41.29%, and 93.47% of the drug at the second, fourth, and twelfth hours, respectively. In conclusion, the dissolution profile of the optimized batch aligns closely with the established USP guidelines for PXT extended-release formulations.

Ethical Statement

NO ETHICAL COMMITTEE APPROVAL IS REQUIRED FOR THE PRESENT STUDY.

Supporting Institution

Dharmsinh Desai University, Nadiad (Gujarat) India

References

  • 1. Nokhodchi A, Raja S, Patel P, Asare-Addo K. The role of oral controlled release matrix tablets in drug delivery systems. BioImpact. 2012; 2(4):175-187. https://doi.org/10.5681%2Fbi.2012.027
  • 2. Agarwal P, Semimul A. A comprehensive review on sustained release matrix tablets: a promising dosage form. Universal J Pharm Res. 2018;3(6):49–54. https://doi.org/10.22270/ujpr.v3i6.222
  • 3. Yang Y, Huang Z, Zhang X, Li J, Huang Y, Chen W, Pan X, Wu C. Development of Paroxetine Hydrochloride Single Layer Controlled-Release Tablets Based on 3² Factorial Design. Pharmaceutics. 2018;10(4): 243. https://doi.org/10.3390/pharmaceutics10040243
  • 4. Davis BA, Nagarajan A, Forrest LR, Singh S K. Mechanism of Paroxetine (Paxil) Inhibition of the Serotonin Transporter. Sci Report. 2016;6:23789. https://doi.org/10.1038/srep23789
  • 5. Rajesh HJ, Shashikiran YH, Anu PA, Priyanka RG. Review on Sustain Release Matrix Tablets. World J Pharm Pharm Sci. 2021;10(11):545-553
  • 6. Khan R, Ashraf MS, Afzal M, Kazmi I, Jahangir MA, Singh R. Formulation and evaluation of sustained release matrix tablet of rabeprazole using wet granulation technique. J Pharm Bioal Sci. 2014;6(3):180-184. https://doi.org/10.4103%2F0975-7406.130961
  • 7. Madgulkar AR, Bhalekar MR, Kolhe VJ, Kenjale YD. Formulation and optimization of sustained release tablets of venlafaxine resinates using response surface methodology. Indian J Pharm Sci. 2009;71(4):387-394. https://doi.org/10.4103%2F0250-474X.57287
  • 8. Mortazavi SA, Jafariazar Z, Ghadjahani Y, Mahmoodi H, Mehtarpour F. Formulation and In vitro Characterization of Sustained Release Matrix Type Ocular Timolol Maleate Mini-Tablet. Iranian J Pharm Res. 2014;13(1), 19–27
  • 9. Sheskey PJ, Robb RT, Moore RD, Boyce BM. Effects of lubricant level, method of mixing, and duration of mixing on a controlled-release matrix tablet containing hydroxypropyl methylcellulose. Drug Develop Ind Pharm. 1995;21(19):2151–2165. https://doi.org/10.3109/03639049509065898
  • 10. Bravo SA, Lamas MC, Salomón CJ. In vitro studies of diclofenac sodium controlled-release from biopolymeric hydrophilic matrices. J Pharm Pharm Sci. (2002); 5(3):213–219.
  • 11. Shah VP, Gurbarg M, Noory A, Dighe S, Skelly JP. Influence of higher rates of agitation on release patterns of immediate-release drug products. J Pharm Sci. 1992;81(6) 500–503. https://doi.org/10.1002/jps.2600810604
  • 12. Nair A, Gupta R, Vasanti S. In vitro controlled release of alfuzosin hydrochloride using HPMC-based matrix tablets and its comparison with marketed product. Pharm Develop Technol. 2007;12(6):621–625. https://doi.org/10.1080/10837450701563277
  • 13. Ravi PR, Kotreka UK, Saha RN. Controlled release matrix tablets of zidovudine: effect of formulation variables on the in vitro drug release kinetics. AAPS Pharm SciTech. 2008;9(1):302–313. https://doi.org/10.1208/s12249-007-9030-8
  • 14. Patel H, Panchal DR, Patel U, Brahmbhatt T, Suthar M. Matrix type drug delivery system: A review. J Pharm Sci Biosci Res. 2011; 1(3):143–151
  • 15. Bang LM, Keating GM. Paroxetine Controlled Release. CNS Drugs. 2004; 18, 355–364. https://doi.org/10.2165/00023210-200418060-00003
  • 16. Aulton ME. Aulton’s Pharmaceutics: The design and manufacture of medicine. 3rd Edition. Churchil livingstone, Elsevier, UK, 2008
  • 17. Lachman L, Liberman HA, Kanig JL. The theory and practice of industrial pharmacy. 3rd Edition. Varghese Publishing House, Bombay, India. 1991
  • 18. Higuchi T. Mechanism of sustained-action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci. 1963;52(12):1145–1149. https://doi.org/10.1002/jps.2600521210
  • 19. Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15(1):25-35. https://doi.org/10.1016/0378-5173(83)90064-9
  • 20. Lieberman HA, Lachman L. Pharmaceutical Dosage Forms. In: Dekker M (ed) Tablet 1980.75-128
  • 21. Bushra R, Shoaib MH, Ali H, Zafar F, Naeem MI, Aslam N. Formulation design and optimization of aceclofenac tablets (100 mg) using central composite design with response surface methodology. Lat Am J Pharm. 2014;33(6):1009–1018
  • 22. Barsagade P, Khetade R, Nirwan K, Agrawal T, Gotafode S, Lade U. Review Article of Dissolution Test Method Development and Validation of Dosage Form by Using RP-HPLC. Int J Pharm Sci Rev Res. 2021; 70(1):28-38 https://dx.doi.org/10.47583/ijpsrr.2021.v70i01.005
  • 23. Kunamaneni P, Kovvasu SP, Janjanam KC. Formulation and optimization of controlled release paroxetine hydrochloride tablets using response surface methodology. J Global Trend Pharm Sci. 2016; 7(4):3520–3534
  • 24. Thirumaran M, Balakumar K, Vijaya Raghavan C, Thuvaragan S. Formulation and in vitro release kinetic study of an enteric coated paroxetine-controlled release tablets. Asian J Res Chem Pharm Sci. 2014; 2(2):63-73
  • 25. Avachat A, Kotwal V. Design and evaluation of matrix-based controlled release tablets of diclofenac sodium and chondroitin sulphate. AAPS Pharm SciTech. 2007; 8(4):51–56. https://doi.org/10.1208/pt0804088
There are 25 citations in total.

Details

Primary Language English
Subjects Pharmaceutical Sciences, Pharmaceutical Delivery Technologies
Journal Section Research Articles
Authors

Komal Parmar 0009-0009-9678-5044

Mehul Patel 0000-0002-5823-9706

Punitkumar Bhatt 0000-0001-6324-051X

Tejal Soni 0000-0002-9159-4400

Bhanubhai Suhagia 0000-0002-2527-9963

Publication Date December 1, 2024
Submission Date March 28, 2024
Acceptance Date November 14, 2024
Published in Issue Year 2024

Cite

Vancouver Parmar K, Patel M, Bhatt P, Soni T, Suhagia B. Optimization of HPMC Loaded Paroxetine HCl Controlled Release Matrix Tablet by Central Composite Design. HUJPHARM. 2024;44(4):289-305.