Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics

doi:10.5246/jcps.2022.07.047

Abstract

Abstract:

In the present study, we aimed to formulate matrix tablets of celecoxib with immediate-release (IR) and sustained-release (SR) and evaluate the influence of different types and concentrations of polymers on drug release characteristics in vitro. All formulations were prepared by using the wet granulation technique. One formulation (F5) with the traditional release was composed without release-control polymers. In contrast, four formulations (F1–F4) with prolonged action were designed by using different cellulosic polymers, such as hydroxypropyl methylcellulose polymers (HPMC-K100M and HPMC-Е6), hydroxypropyl cellulose with high viscosity grade (HPC_h), carboxymethyl cellulose (CMC), and ethylcellulose (EC-10 cps). All tablet formulations contained sodium lauryl sulfate (SLS), polyvinylpyrrolidone (PVP-k30), microcrystalline cellulose (MCC), and lactose monohydrate. The MCC and PVP-k30 were used in a fixed quantity in all formulations except for formulation F5, which contained 10% and 2.7% of them, respectively. The effects of polymer viscosity grade and its quantity on celecoxib release from two formulations containing the same polymer were studied. Drug release in vitro was evaluated in phosphate buffer (pH = 7.4). The amount of celecoxib released in phosphate medium was calculated by preparing a standard series. In vitro profile indicated that formulations F1 (HPMC-K100M) and F2 (HPMC-E6) extended the drug release for 18 h (82%) and 10 h (96.001%), respectively. Formulations F3 and F4 released 72.09% and 59.8% of their contents during 18 h, respectively, and thus their effects could last for more than a day. However, IR formulation (F5) released more than 90% of its content within 1–2 h. 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. The release mechanism of all formulations was Case II relaxation release. This study showed that cellulosic derivative polymers could successfully prolong IR of matrix tablet formulation.

Key words: Immediate release, Sustained release, Celecoxib, HPMC, Wet granulation, Dissolution profile

Supporting:

Ahmed Alkhodri, Svetlana Suslina. Preparation of solid pharmaceutical forms of celecoxib with immediate-release and sustained-release by using wet granulation techniques and evaluation of their in vitro characteristics[J]. Journal of Chinese Pharmaceutical Sciences, 2022, 31(7): 536-544.

Figures/Tables 7

Table 1. Compositions of celecoxib IR and SR tablet formulations.

Table 2. Technological characteristics of granule formulations after adding lubricant.

Table 3. Physicochemical of IR and SR tablet formulations.

Table 4. Standard series in alkaline medium (pH = 7.4).

Table 5. Profile drug release kinetic formulations.

References 23

[1]	Chen, A.; Shi, Y.; Yan, Z.Q.; Hao, H.X.; Zhang, Y.; Zhong, J.; Hou, H.M. Dosage form developments of nanosuspension drug delivery system for oral administration route. Curr. Pharm. Des. 2015, 21, 4355–4365.
[2]	Homayun, B.; Lin, X.T.; Choi, H.J. Challenges and recent progress in oral drug delivery systems for biopharmaceuticals. Pharmaceutics. 2019, 11, 129.
[3]	Ali, H.; Suliman, R.; Elhaj, B.M.; Abdulgader, R. The effect of modified release dosage forms on absorption of medications. Int. J. Pharm. Clin. Res. 2019, 11, 30–33.
[4]	Singhvi, G.; Singh, M. Review: in vitro drug release characterization models. Int. J. Pharm. Stud. Res. 2011, 2, 77–84.‏
[5]	Adilakshmi, D.; Mohammad, A.S.; Rasheed, N.; Umadevi, K.; Pasupuleti, C. Simultaneous Formulation, Estimation and Evaluation of Allopurinol Sustained Release Tablets using various suitable Excipients. Asian Jour. Pharmac. Anal. 2016, 6, 155.
[6]	Ratnaparkhi M.; Jyoti, P. Sustained release oral drug delivery system - an overview. Int. J. Pharm. Stud. Res. 2013, 2, 11–21
[7]	Gong, L.; Thorn, C.F.; Bertagnolli, M.M.; Grosser, T.; Altman, R.B.; Klein, T.E. Celecoxib pathways: pharmacokinetics and pharmacodynamics. Pharmacogenet. Genom. 2012, 22, 310–318.
[8]	Montrose, D.C.; Zhou, X.K.; McNally, E.M.; Sue, E.; Yantiss, R.K.; Gross, S.S.; Leve, N.D.; Karoly, E.D.; Suen, C.S.; Ling, L.L.; Benezra, R.; Pamer, E.G.; Dannenberg, A.J. Celecoxib alters the intestinal microbiota and metabolome in association with reducing polyp burden. Cancer Prev. Res. Phila. Pa. 2016, 9, 721–731.
[9]	USP39-NF34-vol2. The United States Pharmacopeial Convention, USA. 2016.
[10]	Siu, Y.A.; Hao, M.H.; Dixit, V.; Lai, W.G. Celecoxib is a substrate of CYP2D6: impact on celecoxib metabolism in individuals with CYP2C93 variants. Drug Metab. Pharmacokinet. 2018*, 33, 219–227.
[11]	Chan, F.K.; Lanas, A.; Scheiman, J.; Berger, M.F.; Nguyen, H.; Goldstein, J.L. Celecoxib versus omeprazole and diclofenac in patients with osteoarthritis and rheumatoid arthritis (CONDOR): a randomised trial. Lancet. 2010, 376, 173–179.
[12]	Nagendrakumar, D.; G, K.G.; AG, S. An overview: matrix tablets as sustained release. Recent Res. Sci. Technol. 2013, 5, 36–45.
[13]	Sawant, V.; Jayprabha, P.; Shende, V.; Borkar, S.; Wakale, V.; Deore, S.; Dame, G.; Barve, A.; Chatap, V. In-vitro release kinetic study of mosapride citrate dihydrate from sustained release matrix tablet containing two different viscosity grades of HPMC. Res. J. Pharm. Dosage Forms Technol. 2013, 1, 207–212.
[14]	Sirisolla, J.; Ramanamurthy, K.V. Formulation and evaluation of cefixime trihydrate matrix tablets using HPMC, sodium CMC, ethyl cellulose. Indian J. Pharm. Sci. 2015, 77, 321.
[15]	Qi, X.L.; Chen, H.Y.; Rui, Y.; Yang, F.J.; Ma, N.; Wu, Z.H. Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. Int. J. Pharm. 2015, 489, 210–217.
[16]	Chaudhari, S.P.; Dugar, R.P. Application of surfactants in solid dispersion technology for improving solubility of poorly water soluble drugs. J. Drug Deliv. Sci. Technol. 2017, 41, 68–77.
[17]	USP 41- NF36. The United States Pharmacopeial Convention, USA. 2018.
[18]	Hamed, R.; Omran, H. Development of dual-release pellets of the non-steroidal anti-inflammatory drug celecoxib. J. Drug Deliv. Sci. Technol. 2020, 55, 101419.
[19]	Singhvi, G.; Singh, M. Review: in vitro drug release characterization models. Int. J. Pharm. Stud. Res. 2011. 2, 77–84.
[20]	USP 39-NF 34- Vol 1- Powder flow «1174» - (2016) The United States Pharmacopeial Convention, USA.
[21]	Sawant, V.; Jayprabha, P.; Shende, V.; Borkar, S.; Wakale, V.; Deore, S.; Dame, G.; Barve, A.; Chatap, V. In-vitro release kinetic study of mosapride citrate dihydrate from sustained release matrix tablet containing two different viscosity grades of HPMC. Res. J. Pharm. Dosage Forms Technol. 2013, 1, 207–212.
[22]	CELECOXIB COMPOSITIONS - European Patent Office - EP 1049467 B1. Available at: URL: https://patentimages.storage.googleapis.com/1f/12/8b/0d155cbe051c78/EP1049467B1.pdf (дата обращения–09.10.2002).
[23]	Mostafavi, A.; Emami, J.; Varshosaz, J.; Davies, N.M.; Rezazadeh, M. Development of a prolonged-release gastroretentive tablet formulation of ciprofloxacin hydrochloride: Pharmacokinetic characterization in healthy human volunteers. Int. J. Pharm. 2011, 409, 128–136.