Enhancement Drug Dissolution of Celecoxib by Solid Dispersion in HPMC Polymer Combined with PVP and PEG 6000

  • Danang Novianto Wibowo Fakultas Farmasi Universitas Wahid Hasyim
  • Anita Sukmawati Fakultas Farmasi Universitas Wahid Hasyim

Abstract

Celecoxib has poor solubility and categorized as Biopharmaceutical Classification System (BCS) class II drug therefore, it prepared into the solid dispersion system in order to enhance drug solubility. This study aims to determine physical characteristic and the dissolution rate of celecoxib in solid dispersion systems using Hydroxypropyl methylcellulose (HPMC) polymers combined with polyvinyl pyrrolidone (PVP) and polyethylene glycol (PEG) 6000. Celecoxib solid dispersions (CSDs) were prepared with HPMC-PVP in ratio of 1:2 and 2:1 and HPMC-PEG 6000 in ratio 1:2 and 2:1. The dissolution rate of CSDs were evaluated using dissolution method and physical characteristics were evaluated using the X-ray Powder Diffraction (XRPD). The result showed that the CSD containing HPMC-PVP 1:2 as a matrix had the highest dissolution rate (0.808 mg/cm2/minute). The dissolution rate was higher than pure celecoxib (0.400 mg / cm2 / minute). The characterisation of the crystalline degree of celecoxib solid dispersions (CSDs) using the X-ray Diffraction showed a decrease in the peak intensity of the interferance of the crystalline phase. The solid dispersion system using HPMC-PVP 1:2 could enhance the rate of dissolution of celecoxib twice highest than pure celecoxib. The highest dissolution rate value was found in celecoxib solid dispersion with 1:2 HPMC-PVP as a matrix.

References

1. Goldenberg MM. Celecoxib: A COX-2 inhibitor for the treatment of osteoarthritis and rheumatoid arthritis. Clin Ther. 1999;21(5):405–17.

2. Yazdanian M, Briggs K, Jankovsky C, Hawi A. The “High Solubility” Definition of the Current FDA Guidance on Biopharmaceutical Classification System May Be Too Strict for Acidic Drugs. Pharm Res. 2004;21(2):293–9.

3. Wu CY, Benet LZ. Predicting drug disposition via application of BCS: Transport/absorption/ elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res. 2005;22(1):11–23.

4. Chaudhari SP, Dugar RP. Application of surfactants in solid dispersion technology for improving solubility of poorly water soluble drugs. J Drug Deliv Sci Technol [Internet]. 2017;41:68–77. Available from: http://dx.doi.org/10.1016/j.jddst.2017.06.010

5. Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion systems. J Pharm Sci. 1971;60(9):1281–302.

6. Jansook P, Kulsirachote P, Loftsson T. Cyclodextrin solubilization of celecoxib: solid and solution state characterization. J Incl Phenom Macrocycl Chem [Internet]. 2018;90(1–2):75–88. Available from: http://dx.doi.org/10.1007/s10847-017-0769-6

7. Lee JH, Kim MJ, Yoon H, Shim CR, Ko HA, Cho SA, et al. Enhanced dissolution rate of celecoxib using PVP and/or HPMCbased solid dispersions prepared by spray drying method. J Pharm Investig. 2013;43:205–13.

8. Wahyuni R, Halim A, Siska F. Studi Sistem Dispersi Padat Karbamazepin Menggunakan Campuran Polimer PEG 6000 dan HPMC dengan Metoda Pelarutan. Pros Semin Nas dan Work “Perkembangan Terkini Sains Farm dan Klin IV” tahun 2014. 2014;220–7.

9. Janssens S, De Armas HN, Robert SJ, Mooter G Van Den. Characterization of Ternary Solid Dispersions of Itraconazole, PEG 6000, and HPMC 2910 E5. J Pharm Sci [Internet]. 2007;99(5):2386–2398. Available from: http://onlinelibrary.wiley.com/doi/10.1002/jps.22007/full%5Cnhttp://www.ncbi.nlm.nih.gov/pubmed/19967780

10. Paradkar A, Ambike AA, Jadhav BK, Mahadik KR. Characterization of kurkumin-PVP solid dispersion obtained by spray drying. Int J Pharm. 2004;271(1–2):281–6.

11. Zerrouk N, Chemtob C, Arnaud P, Toscani S. In Vitro and In Vivo Evaluation of Carbamazepine-PEG 6000 Solid Dispersion. Int J Pharm. 2001;225:49–62.

12. FDA. Dissolution Method [Internet]. 2010. Available from: https://www.accessdata.fda.gov/scripts/CDER/dissolution/dsp_SearchResults.cfm

13. Yu LX, Carlin AS, Amidon GL, Hussain AS. Feasibility studies of utilizing disk intrinsic dissolution rate to classify drugs. Int J Pharm. 2004;270(1–2):221–7.

14. Nugrahani I. Analisis dan Rekayasa Bahan Padat Farmasi. Bandung: ITP Press; 2020. 93–100 p.

15. Shargel, L. Wu-Pong, S. dan Yu ABC. Biofarmasetika dan Farmakokinetika Terapan. 5th ed. Surabaya: Pusat Penerbitan dan Percetakan Universitas Airlangga; 2010. 5, 724, 730, 736 p.
Published
2022-04-29
How to Cite
WIBOWO, Danang Novianto; SUKMAWATI, Anita. Enhancement Drug Dissolution of Celecoxib by Solid Dispersion in HPMC Polymer Combined with PVP and PEG 6000. JURNAL ILMU KEFARMASIAN INDONESIA, [S.l.], v. 20, n. 1, p. 81-86, apr. 2022. ISSN 2614-6495. Available at: <http://jifi.farmasi.univpancasila.ac.id/index.php/jifi/article/view/887>. Date accessed: 05 nov. 2024. doi: https://doi.org/10.35814/jifi.v20i1.887.
Section
Articles