Zileuton compression coated tablets : formulation development and in vitro evaluation
Abstract
In the present research work Zileuton tablets were formulated by employing compression coating technology. Initially the core tablets were prepared by using various concentrations of super disintegrates, the formulated core tablets were coated with the polymers by using compression coating technology. All the core and compress coated tablet formulations were subjected to various physical and chemical evaluation tests for core and compress coated tablets. The thickness, hardness and weight variation shown by all the tablet formulations were found within the official pharmacopoeial limits. In vitro release of Zileuton of core tablet formulations ZF5 showed faster drug release after 15 min. Faster drug release can be correlated with the high disintegration and friability observed in this study.
Keywords:
compression coating technology, zileuton, core
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References
1. Qiu Y., Cheskin H., Briskin J., Engh K. Sustained-release hydrophilic matrix tablets of zileuton: formulation and in vitro/in vivo studies. J. Control. Release 1997; 45: 249–256
2. Ford J. L., Rubinstein M. H., McCaul F., Hogan J. E., Edgar P. J. Importance of drug type, tablet shape and added diluents on drug release kinetics from hydroxypropylmethylcellulose matrix tablets. Int. J. Pharm. 1987; 40: 223–234
3. Mitchell K., Ford J. L., Armstrong D. J., et al. The influence of drugs on the properties of gels and swelling characteristics of matrices containing methylcellulose or hydroxypropylmethylcellulose. Int. J. Pharm. 1993; 100: 165–173
4. Hogan J. E. Hydroxypropylmethylcellulose sustained release technology. Drug Dev. Ind. Pharm. 1989; 15(6&7)975–999
5. Sarisuta N., Mahahpunt P. Effects of compression force and types of fillers on release of diclofenac sodium from matrix tablets. Drug Dev. Ind. Pharm. 1994; 20(6)1049–1061
6. Technical Information, Manual # 198–1029-1295X GW. Dow Chemical Company, Midland, Michigan 1995; 25
7. Nilsson S. Interactions between water-soluble cellulose derivatives and surfactants. 1. The HPMC/SDS/water system. Macromolecules 1995; 28: 7837–7844
8. Lofroth J. E., Johansson L., Norman A. C., Wettstrom K. Interactions between surfactants and polymers. I: HPMC. Progr. Colloid. Polym. Sci. 1991; 84: 73–77
9. Johnson J. L., Holinej J., Williams M. D. Influence of ionic strength on matrix integrity and drug release from hydroxypropyl cellulose compacts. Int. J. Pharm. 1993; 90: 151–159
10. Kararli T. T. Composition of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm. Drug Dispos. 1995; 16: 351–380
11. Pirkle W. H., Pochapsky T. C. Considerations of chiral recognition relevant to the liquid chromatographic separation of enantiomers. Chem. Rev. 1989; 89: 347–362
12. Dressman J. B., Yamada K. Animal models for oral drug absorption. Pharmaceutical Bioequivalence, P. G. Welling, F. L.S. Tse, S. V. Dighe. Marcel Dekker, Inc., New York 1991; 235–266
13. Marabathuni VJ, Dinesh P, Ravikumar R, Yamini P, Kiran PS, Hussain SP, Rao CM. Chitosan based sustained release mucoadhesive buccal patches containing amlodipine besylate (AMB). Asian Journal of Research in Pharmaceutical Science. 2017;7(2):97-104.
14. Marabathuni VJ, Bhavani M, Lavanya M, Padmaja K, Madhavi N, Babu P, Rao CM. Formulation and evaluation of mouth dissolving Tablets of carbamazepine. Asian Journal of Pharmacy and Technology. 2017;7(3):137-43.
15. Rao CP, Rahaman SA, Prasad YR, Reddy PG. RP-HPLC method of simultaneous estimation of amlodipine besylate and metoprolol in combined dosage form. International Journal of Pharmaceutical Research and Development. 2010 Nov;2(9):69-76. IF=2.01
16. Rao CM, Konda R, Rao RN, Ramanjeneeyulu S, Reddy PG. Estimation of Nevirapine Anhydrous Bulk Formulation by Using IR, RP-HPLC, GC Methods. Research Journal of Pharmacy and Technology. 2010;3(4):1088-92.IF=0.38 Scopus Indexed
17. Rao CM, Rahaman SA, Prasad YR, Rao GE. Design and Synthesis of 1-(3’, 5’-bis trifluoromethyl phenyl)-3-(substituted phenyl)-2-propene-1-one as potent antifungal and antibacterial agents. Der Pharma Chemica. 1997;4(5):2012. SJR IF=0.19
18. Rao CM, Rehaman SA, Yejella RP. Synthesis of novel 1-(2, 4′-difluorophenyl)-3-(4 ″-aryl)-2-propen-1-ones and their pharmacological activities. World Journal of Pharmacy and Pharmaceutical Sciences (WJPPS). 2014;3(11):576-86. IF=7.62.
19. RAO CM, Dhachinamoorthi D, Mounika M, Pavani M, Shireennaaz S, Reddy CS, annapurna m. Synthesis, characterization and anti microbial activity of novel chalcones and its di hydro pyrimidinenones. International journal of life science and pharma research. 2015 Jul 1;5(3):P13-6. (Web of Science, Thomson Reuters)
20. Rao CM, Yejella RP, Rehman RS, Basha SH. Molecular docking based screening of novel designed chalcone series of compounds for their anti-cancer activity targeting EGFR kinase domain. Bioinformation. 2015;11(7):322. Avg.IF= 5.75 (PubMed)
21. Chennu MM, Abdul RS, Yejella RP. Molecular docking based screening of G6PS with 1, 5 Benzothiazepine derivates for a potential inhibitor. Bioinformation. 2015;11(12):525. Avg.IF= 5.75 (PubMed)
22. Rao CM, Rehaman SA, Yejella RP. Molecular Modelling And Docking Based Studies Of Novel Chalcone Skeleton Based Compounds On Glucosamine-6-Phosphate Synthase Enzyme. International Journal of Pharmaceutical Sciences and Research. 2016 May 1;7(5):1956.IF=0.27 (Scopus)
23. Rao CH, Prasada MM. Novel series of 1, 5 Benzothiazepine skeleton based compounds as anti-cancer agents–In silico and MTT assay-based study. Journal of PeerScientist. 2018;1(2):e1000008.
24. Rao CM, Rajewsari T. Review on biological nitrogen fixation (bnf) in soil management. International Journal of Pharmaceutics and Drug Analysis. 2019;7(8):46-50.
25. Rao CM, Narapusetty Naidu JP, Rao KP, Ranjith K, Shobha S, Chowdary BS, Siddiraju S. Molecular docking and dynamic simulations of benzimidazoles with beta-tubulins. Bioinformation. 2021;17(3):404. Avg.IF= 5.75 (PubMed)
26. Estimation of Rabeprazole Sodium and Itopride Hydrochloride in Tablet Dosage Form Using Reverse Phase High Performance Liquid Chromatography” E-Journal of Chemistry 2011, 8(1), 37-42.
27. “Synthesis and Antimicrobial Activity of Some Novel Chalcones of Acetophenone and Benzaldehyde Derivatives” IJPI’S journal of medicinal chemistry, September 2011, vol-i, issue6.
28. “Design and Synthesis of 1-(3’, 5’-Bis Trifluoromethyl Phenyl)-3-(Substituted Phenyl) - 2-Propene-1-One as Potent Antifungal and Antibacterial Agents” Der Pharma Chemica, 2012, 4(5):1997-2002.
29. “Evaluation Of Antiarthritic Activity Of Ethanolic Extract Of tephrosia purpurea (LINN)” Inventi Rapid: Ethanopharmacolgy, Vol-2013,Issue 4
30. “Analgesic Activity of Aueous and Alcholic Extract Root Extract of Shoots Of dendrophtoe falcate” IJRPP, VOL 3(1), 2013, 54-56.
31. “Development and Validation of New Derivative Uv-Spectrophotometric Methods for Quantitative Estimation of Abacavir Sulphate in Bulk and Pharmaceutical Dosage Form” International Journal of Biological & Pharmaceutical Research. 2013; 4(8): 608-613
2. Ford J. L., Rubinstein M. H., McCaul F., Hogan J. E., Edgar P. J. Importance of drug type, tablet shape and added diluents on drug release kinetics from hydroxypropylmethylcellulose matrix tablets. Int. J. Pharm. 1987; 40: 223–234
3. Mitchell K., Ford J. L., Armstrong D. J., et al. The influence of drugs on the properties of gels and swelling characteristics of matrices containing methylcellulose or hydroxypropylmethylcellulose. Int. J. Pharm. 1993; 100: 165–173
4. Hogan J. E. Hydroxypropylmethylcellulose sustained release technology. Drug Dev. Ind. Pharm. 1989; 15(6&7)975–999
5. Sarisuta N., Mahahpunt P. Effects of compression force and types of fillers on release of diclofenac sodium from matrix tablets. Drug Dev. Ind. Pharm. 1994; 20(6)1049–1061
6. Technical Information, Manual # 198–1029-1295X GW. Dow Chemical Company, Midland, Michigan 1995; 25
7. Nilsson S. Interactions between water-soluble cellulose derivatives and surfactants. 1. The HPMC/SDS/water system. Macromolecules 1995; 28: 7837–7844
8. Lofroth J. E., Johansson L., Norman A. C., Wettstrom K. Interactions between surfactants and polymers. I: HPMC. Progr. Colloid. Polym. Sci. 1991; 84: 73–77
9. Johnson J. L., Holinej J., Williams M. D. Influence of ionic strength on matrix integrity and drug release from hydroxypropyl cellulose compacts. Int. J. Pharm. 1993; 90: 151–159
10. Kararli T. T. Composition of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm. Drug Dispos. 1995; 16: 351–380
11. Pirkle W. H., Pochapsky T. C. Considerations of chiral recognition relevant to the liquid chromatographic separation of enantiomers. Chem. Rev. 1989; 89: 347–362
12. Dressman J. B., Yamada K. Animal models for oral drug absorption. Pharmaceutical Bioequivalence, P. G. Welling, F. L.S. Tse, S. V. Dighe. Marcel Dekker, Inc., New York 1991; 235–266
13. Marabathuni VJ, Dinesh P, Ravikumar R, Yamini P, Kiran PS, Hussain SP, Rao CM. Chitosan based sustained release mucoadhesive buccal patches containing amlodipine besylate (AMB). Asian Journal of Research in Pharmaceutical Science. 2017;7(2):97-104.
14. Marabathuni VJ, Bhavani M, Lavanya M, Padmaja K, Madhavi N, Babu P, Rao CM. Formulation and evaluation of mouth dissolving Tablets of carbamazepine. Asian Journal of Pharmacy and Technology. 2017;7(3):137-43.
15. Rao CP, Rahaman SA, Prasad YR, Reddy PG. RP-HPLC method of simultaneous estimation of amlodipine besylate and metoprolol in combined dosage form. International Journal of Pharmaceutical Research and Development. 2010 Nov;2(9):69-76. IF=2.01
16. Rao CM, Konda R, Rao RN, Ramanjeneeyulu S, Reddy PG. Estimation of Nevirapine Anhydrous Bulk Formulation by Using IR, RP-HPLC, GC Methods. Research Journal of Pharmacy and Technology. 2010;3(4):1088-92.IF=0.38 Scopus Indexed
17. Rao CM, Rahaman SA, Prasad YR, Rao GE. Design and Synthesis of 1-(3’, 5’-bis trifluoromethyl phenyl)-3-(substituted phenyl)-2-propene-1-one as potent antifungal and antibacterial agents. Der Pharma Chemica. 1997;4(5):2012. SJR IF=0.19
18. Rao CM, Rehaman SA, Yejella RP. Synthesis of novel 1-(2, 4′-difluorophenyl)-3-(4 ″-aryl)-2-propen-1-ones and their pharmacological activities. World Journal of Pharmacy and Pharmaceutical Sciences (WJPPS). 2014;3(11):576-86. IF=7.62.
19. RAO CM, Dhachinamoorthi D, Mounika M, Pavani M, Shireennaaz S, Reddy CS, annapurna m. Synthesis, characterization and anti microbial activity of novel chalcones and its di hydro pyrimidinenones. International journal of life science and pharma research. 2015 Jul 1;5(3):P13-6. (Web of Science, Thomson Reuters)
20. Rao CM, Yejella RP, Rehman RS, Basha SH. Molecular docking based screening of novel designed chalcone series of compounds for their anti-cancer activity targeting EGFR kinase domain. Bioinformation. 2015;11(7):322. Avg.IF= 5.75 (PubMed)
21. Chennu MM, Abdul RS, Yejella RP. Molecular docking based screening of G6PS with 1, 5 Benzothiazepine derivates for a potential inhibitor. Bioinformation. 2015;11(12):525. Avg.IF= 5.75 (PubMed)
22. Rao CM, Rehaman SA, Yejella RP. Molecular Modelling And Docking Based Studies Of Novel Chalcone Skeleton Based Compounds On Glucosamine-6-Phosphate Synthase Enzyme. International Journal of Pharmaceutical Sciences and Research. 2016 May 1;7(5):1956.IF=0.27 (Scopus)
23. Rao CH, Prasada MM. Novel series of 1, 5 Benzothiazepine skeleton based compounds as anti-cancer agents–In silico and MTT assay-based study. Journal of PeerScientist. 2018;1(2):e1000008.
24. Rao CM, Rajewsari T. Review on biological nitrogen fixation (bnf) in soil management. International Journal of Pharmaceutics and Drug Analysis. 2019;7(8):46-50.
25. Rao CM, Narapusetty Naidu JP, Rao KP, Ranjith K, Shobha S, Chowdary BS, Siddiraju S. Molecular docking and dynamic simulations of benzimidazoles with beta-tubulins. Bioinformation. 2021;17(3):404. Avg.IF= 5.75 (PubMed)
26. Estimation of Rabeprazole Sodium and Itopride Hydrochloride in Tablet Dosage Form Using Reverse Phase High Performance Liquid Chromatography” E-Journal of Chemistry 2011, 8(1), 37-42.
27. “Synthesis and Antimicrobial Activity of Some Novel Chalcones of Acetophenone and Benzaldehyde Derivatives” IJPI’S journal of medicinal chemistry, September 2011, vol-i, issue6.
28. “Design and Synthesis of 1-(3’, 5’-Bis Trifluoromethyl Phenyl)-3-(Substituted Phenyl) - 2-Propene-1-One as Potent Antifungal and Antibacterial Agents” Der Pharma Chemica, 2012, 4(5):1997-2002.
29. “Evaluation Of Antiarthritic Activity Of Ethanolic Extract Of tephrosia purpurea (LINN)” Inventi Rapid: Ethanopharmacolgy, Vol-2013,Issue 4
30. “Analgesic Activity of Aueous and Alcholic Extract Root Extract of Shoots Of dendrophtoe falcate” IJRPP, VOL 3(1), 2013, 54-56.
31. “Development and Validation of New Derivative Uv-Spectrophotometric Methods for Quantitative Estimation of Abacavir Sulphate in Bulk and Pharmaceutical Dosage Form” International Journal of Biological & Pharmaceutical Research. 2013; 4(8): 608-613
Published
22/02/2022
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Ilapavuluri, S., Marabathuni, V. J. P., & Narapusetty , N. (2022). Zileuton compression coated tablets : formulation development and in vitro evaluation. Journal of Innovations in Applied Pharmaceutical Science (JIAPS), 7(1), 45-50. https://doi.org/10.37022/jiaps.v7i1.290
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