EVALUATION OF DIFFERENT SYNTHETIC AND NATURAL POLYMERS AS PROTECTIVE LAYER ON HIGHLY SOLUBLE AND HIGH DOSE DRUG METOPROLOL SUCCINATEFOR MANUFACTURING OF CONTROL RELEASE MULTI UNIT PELLETS TABLETS
Keywords:MUPS, CR, Compression of pellets, Drug release, Natural and synthetic Polymers
Objective: Evaluation of different natural and synthetic polymers as protective layer (PL) in the manufacturing of control release (CR) multi-unit pellets (MUPS) tablets, highly soluble and high dose drug metoprolol succinate (MS) was selected as model drug. The function of PL is to protect CR functional coating layer of pellets from damage during compression of MUPS tablets.
Methods: MS is highly soluble biopharmaceutics classification system(BCS) Classâ€“I molecule, hence selected aqueous solution layering method for drug loading in fluid bed processor (FBP), optimized formulation was manufactured by using seal coating on microcrystalline cellulose (MCC) pellets followed by drug loading (DL) and CR coating, applied by using the solution layering method in FBP. Given coating on these functional coated pellets with different natural and synthetic polymers like hydroxypropyl cellulose (Klucel LF), polyethylene glycol 6000 (PEG 6000), hypromellose 5 cps (HPMC 5cps), guar gum (GG) and xanthan gum (XM). Evaluated these pellet's for physical characterization and chemical characterization.
Results: Drug release profiles of CR MUPS tablets containing PL coating were compared to those CR pellets and f2 values observed was 81.83, 49.92, 89.35, 66.44, and 85.25 with Klucel LF, PEG 6000, HPMC 5 cps, GG and XM coated MUPS tablets respectively. The dissolution data indicated that, there was no significant change were observed with MUPS containing Klucel LF, HPMC 5 cps, GG and XG PLs whereas faster release profiles were observed with PEG 6000PL MUPS tablets.
Conclusion: Based on these dissolution profiles it was concluded that by applying low viscous natural or synthetic binders like Klucel LF, HPMC 5 cps, GG and XG on functional coating pellets given good protection to functional coating pellets from damage during compression. It is a very effective and potent strategy for manufacturing of MUPS tablets. Whereas PEG 6000 polymer not able to give protection to functional coating pellets from damage during compression, it may be due to its very low viscosity of PEG 6000.
Ong LW, Ong KT, Heng PWS. Novel film modifiers to alter the physical properties of ethyl cellulose films. Pharm Res 2005;22:476â€“89.
Yao T, Yamadam M, Yamahara H, Masanori Yoshida. Tabletting of coated particles. II. Influence of particle size of pharmaceutical additives on the protection of coating membrane from mechanical damage during the compression process. Chem Pharm Bull 1998;46:826â€“30.
Mizumoto T, Tamura T, Kawai H, Atsushi K, Shigeru ITAI. Formulation design of an oral, fast-disintegrating dosage form containing taste-masked particles of famotidine. Chem Pharm Bull 2008;56:946â€“50.
Shajahan A, Chandewar Anil V, Jaiswal Sunil B. A flexible technology for modified-release drugs: multiple-unit pellet system (MUPS). J Controlled Release 2010;147:2-16.
Xu M, Heng PWS, Liew CV. Formulation and process strategies to minimize coat damage for compaction of coated pellets in a rotary tablet press: a mechanistic view. Int J Pharm 2016;499:29-37.
JJ Torrado, LL Augsburger. Effect of different excipients on the tableting of coated Particles. Int J Pharm 1994;106:149â€“55.
Tingting Peng, Chune Zhu, Ying Huang, Guilan Quan, Linchong Huang, Linna Wu, et al. Improvement of the stability of doxycycline hydrochloride pellet-containing tablets through a novel granulation technique and proper excipients. Powder Technol 2015;270:221-9.
P Bansal, S Vasireddy, F Plakogiannis, D Parikh. Effect of compression on the release properties of polymer coated niacin granules. J Controlled Release 1993;27:157â€“63.
S Bechard, J Leroux. Coated pelletized dosage form: effect of compaction on drug release. Drug Dev Ind Pharm 1992; 12:1927â€“44.
Abraham B Bashaiwoldu, Fridrun Podczeck, J Michael Newton. Compaction of and drug release from coated pellets of different mechanical properties. Adv Powder Technol 2011;22:340-53.
Sombor Csoban, Barnabas Kallai-Szabo, Nikolett Kallai-Szabo, Istvan Sebe, Peter Gordon, Istvan Antal. Improvement of mechanical properties of a pellet containing tablets by thermal treatment. Int J Pharma 2015;496:489-96.
Hosseini, M KÃ¶rber, R Bodmeier. Direct compression of cushion-layered ethylcellulose-coated CRpellets into rapidly disintegrating tablets without changes in the release profile. Int J Pharm 2013;457:503â€“9.
Olvishkumar M Kothiya, Bhavana A Patel, Kunal N Patel, Madhabhai M Patel. Formulation and characterization of sustained release matrix tablets of ivabradine using 32 full factorial design. Int J Appl Pharm 2018;10:59-66.
Laila H Emara, Aya R Abdou, Ahmed A El-ashmawy, Nadia M Mursi. Preparation and evaluation of metronidazole sustained release floating tablets. Int J Pharm Pharm Sci 2014;6:198-204.
K Pallavi, T Pallavi. Formulation and evaluation of fast dissolving films of eletriptan hydrobromide. Int J Curr Pharm Res 2017;9:59-63.
Y Deepthi Priya, YA Chowdary, TEGK Murthy, B Seshagiri. Design and evaluation of atomoxetine HCl pellets by mups technology. Int J Pharm Pharm Sci 2014;6:110-5.
Shajan Abraham, Muhammed Naufal, Vidya Peter, Susan Raju, Christina Das. Formulation and evaluation of gastro-retentive drug delivery system containing a combination of glipizide and metformin hydrochloride. Asian J Pharm Clin Res 2016;9:235-40.
Krishna Mohan Chinnala, Sirish Vodithala. Formulation development and evaluation of fast disintegrating tablets of cinitapride hydrogen tartarate by using direct compression technique. Int J Curr Pharm Res 2017;9:98-103.
Anurupa C, Suseem SR. Aloe vera powder based matrix tablet for oral controlled delivery of the highly soluble drug. Innovare J Sci 2014;2:1-3.
Gurav AS, Sayyad FJ, Gavhane YN, Khakal NN. Development of olmesartan medoxomil-loaded chitosan microparticles: a potential strategy to improve physicochemical and micromeritic properties. Int J Pharm Pharm Sci 2015;7:324-30.
Balagani Pavan Kumar, Pallepati Kavitha, Katamreddy Jyothshna Devi. Formulation design and evaluation of mucoadhesive buccal tablets of nitroglycerin. Int J Pharm Pharm Sci 2014;6:251-9.
Lannie Hadisoewignyo, Lisa Soegianto, Martha Ervina, Indahwati Wijaya, Sari Dewi Santoso, Novi tania1etal. Formulation development and optimization of a tablet containing a combination of salam (syzygium polyanthum) and sambiloto (andrographis paniculata) ethanolic extracts. Int J Pharm Pharm Sci 2016;8:267-73.
M Sunitha Reddy, Vasam Tweja. Formulation and evaluation of lamivudine sustained release matrix tablets using jackfruit seed extract as release retardant. World J Pharm Pharm Sci 2017;6:1050-62.
Swapna K, Aparna C, Prathima Srinivas. Formulation and evaluation of montelukast sodium and levocetirizine dihydrochloride sublingual tablets. Asian J Pharm Clin Res 2015; 8:171-5.
Ashish Masih, Ajay Kumar Tiwari. Formulation and evaluation of fast dissolving tablets of amoxycillin trihydrate and potassium clavulanate. Int J Curr Pharm Res 2017;9:48-58.
The United States Pharmacopoeia/National Formulary, USP 37/NF 32. Vol. I. The United States Pharmacopoeial Convention, Timbrook Parkway, Rockville; 2014. p. 344-6, 487, 491-4, 1145-7.
Delina Xhafaj, Ledjan Malaj, Migena Mileti. A comparative quality control study of cetirizine hydrochloride 10 mg tablets on the albanian pharmaceutical market. Int J Pharm Pharm Sci 2015;7:504-7.