FORMULATION AND DESIGN OF EXTENDED RELEASE MATRIX TABLETS OF ZIDOVUDINE HYDROCHLORIDE: A STUDY ON EFFECT OF VARIOUS GRADES OF ETHOCEL AND HPMC
DOI:
https://doi.org/10.22159/ijpps.2018v10i3.24258Keywords:
Zidovudine hydrochloride, Ethocel, Innovator, Compression, HardnessAbstract
Objective: The current research was an attempt to formulate and design an extend release dosage form of zidovudine hydrochloride using various grades of ethyl cellulose (ethocel) such as ethocel 4CPS, ethocel 7 CPS and aqualon T10 Pharm EC with two grades of hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M).
Methods: Pilot scale batches of nine formulations were prepared using kollidon and adopting wet granulation technique. Physiochemical properties of tablet and granules were examined prior compression to get tablet. Tablets were characterized as drug content, percentage weight variation, thickness, Hardness, percentage friability and in vitro drug release pattern and studied for 12 hour in USP Type-II apparatus using 900 ml Phosphate buffer at 37±0.5 °C. The dissolution release profile of drug in tablet was performed by various drug release kinetic modelling.
Results: The result revealed formulation F8 containing ethocel 7CPS and aqualon T10 was able to delay the pure drug release for 12 h and followed Higuchi pattern. Whereas; formulations containing only ethocel 4CPS provided earlier drug release. Dissolution data of promising formulation were analysed with innovator formulation for similarity factor (f2), exhibited an acceptable value more than 50. FT-IR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) study revealed no such incompatibility found between the pure drug and polymers but slight change in crystalinity were observed in XRD study (X-ray diffraction). SEM (scanning electron microscope) study revealed very rare intragranular pore and cavity.
Conclusion: From that, it can be marked as viscosity and selection of ethocel have great importance in delay drug release.Â
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References
Chien YW. Novel drug delivery systems. 2nd ed. New York: Marcel Dekker; 1992.
Singh BN, Kim KH. Floating drug delivery system: an approach to oral controlled drug delivery via gastric retention. J Controlled Release 2000;63:235-59.
Brazel CS, Peppas NA. Temperature-and pH-sensitive hydrogels for controlled release of antithrombotic agents. Mater Res Soc Symp Proc 1994;331:211-6.
https://www.webmd.com/drugs/2/drug-4386/zidovudine-oral/details. [Last accessed on 08 Sep 2017]
https://aidsinfo.nih.gov/drugs/4/zidovudine/0/patient. [Last accessed on 10 Sep 2017]
Santos JV, Pina ME, Marques MP, de Carvalho LA. New sustained release of Zidovudine Matrix tablets− cytotoxicity toward Caco-2 cells. Drug Dev Ind Pharm 2013;39:1154-66.
Ganesh S, Radhakrishnan M, Ravi M, Prasannakumar B, Kalyani J. In vitro evaluation of the effect of combination of hydrophilic and hydrophobic polymers on controlled release zidovudine matrix tablets. Indian J Pharm Sci 2008;70:461-5.
Kuksal A, Tiwary AK, Jain NK, Jain S. Formulation and in vitro, in vivo evaluation of extended-release matrix tablet of zidovudine: influence of combination of hydrophilic and hydrophobic matrix formers. AAPS PharmSciTech 2006;7:E1-9.
Tiwari SB, Murthy TK, Pai MR, Mehta PR, Chowdhary PB. Controlled release formulation of tramadol hydrochloride using hydrophilic and hydrophobic matrix system. AAPS PharmaSciTech 2003;4:110-6.
Harland R, Dubernet C, Benoit JP, Peppas NA. A model of dissolution-controlled, release from non-swellable polymeric microspheres. J Controlled Release 2003;6:282-91.
Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder: Effect of formulation and process parameter on drug release. Eur J Pharm Sci 2003;18:37-45.
Aslani A, Fattahi F. Formulation, characterization and physicochemical evaluation of potassium citrate effervescent tablets. Adv Pharm Bull 2013;3:217-25.
Costa P, Manuel J, Labao S. Modeling and comparision dissolution profiles. Eur J Pharm Sci 2002;13:123-33.
Ritger PL, Peppas NA. A simple equation for description of solute release, II: Fickian and anomalous release from swellable devices. J Controlled Release 1987;5:37-42.
Goswami KO, Khurana GA, Marwaha RK, Gupta MI. Development and evaluation of extended release ethylcellulose based matrix tablet of diclofenac sodium. Int J Pharm Pharm Sci 2014;6:296-301.
Ramenskaya GV, Shlykov VS, Dekhanova OA. Comparative in vitro dissolution testing of trimetazidine prolonged-release tablets. Pharm Chem J 2009;43:677-9.
Elkhodairy KA, Hassan MA, Afifi SA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm J 2014;22:53-61.
Harekrishna Roy. Formulation of sustained release matrix tablets of metformin hydrochloride by polyacrylate polymer. Int J Pharma Res Health Sci 2015;3:900-6.
Md Mofizur R, Sumon R, Sreedam Chandra D, Mithilesh Kumar J, Taslima B, Md Qamrul A, et al. Evaluation of various grades of hydroxypropylmethylcellulose matrix systems as oral sustained release drug delivery systems. J Pharm Sci Res 2011;3:930-8.
Pawar HA, Dhavale R. Development and evaluation of gastroretentive floating tablets of an antidepressant drug by thermoplastic granulation technique. Beni-Suef University J Basic Appl Sci 2014;3:122-32.
Song SH, Chae BR, Sohn SI, Yeom DW, Son HY, Kim JH, et al. Formulation of controlled-release pelubiprofen tablet using Kollidon® SR. Int J Pharm 2016;511:864-75.
Ravala JA, Patela JK, Naihong L, Patela MM. Ranitidine hydrochloride floating matrix tablets. Asian J Pharm Sci 2007;2:130-42.
Khan GM, Meidan VM. Drug release kinetics from tablet matrices based upon ethylcellulose ether-derivatives: a comparison between different formulations. Drug Dev Ind Pharm 2007;33:627-39.
Guideline IH. Stability testing of new drug substances and products. Q1A(R2), current step; 2003. p. 4.
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