EFFECT OF COMPONENTS AND DEPOSITION ON TECHNOLOGICAL PERFORMANCE OF IBUPROFEN TABLETS


Yessica Guadalupe -sosa Velasco, Leopoldo Villafuerte Robles

Abstract


Objective: This work evaluated the influence of the technological properties of polyvinylpyrrolidone (PVP), calcium phosphate (CP) and cross-linked sodium carboxymethylcellulose (CC) as well as the deposition of a solid dispersion, through the solvent evaporation method, on the technological parameters that define the properties of ibuprofen tablets.

Methods: The powder flow rate through an orifice, bulk volume and tapped volume of powders, tablet hardness, disintegration time and dissolution profile of the tablets were determined on individual components, their physical mixtures, granules obtained by deposition and solvent evaporation, and tablets obtained at different compaction pressures.

Results: The very poor flowability of CP and the high compactibility of PVP were transferred to the powder mixtures, which showed poor flowability, and ibuprofen tablets with twice the compactibility. The tablets disintegration was high with a low proportion of CC (0.5%), but decreased linearly by increasing the proportion of the disintegrant up to 10%. At the same time, the dissolution of the drug after 30 minutes increased from 3% to 80%. The agglomeration of CP through the deposition of an alcoholic solution of the drug and PVP improved the flow properties and tripled the hardness of the tablets. However, the dissolution after 30 min decreased from 80% to 18%.

Conclusion: The physical mixture was the best option to improve the dissolution, while the deposition on an adsorbent, of a solid dispersion of drug-PVP, was the best option to improve the compactibility and flow properties.


Keywords


Calcium phosphate; Croscarmellose sodium; Drug deposition; Ibuprofen tablets; polyvinylpyrrolidone; Solid dispersion; Technological performance.

References


Parkash V, Maan SD, Yadav SKH, Jogpal V. Fast disintegrating tablets: Opportunity in drug delivery system. J Adv Pharm Tech Res 2011;2:223-35.

Beri Ch, Sacher I. Development of fast disintegration tablets as oral drug delivery system-A review. Indian J Pharm Biol Res 2013;1:80-99.

Moreton Ch. Functionality and Performance of Excipients in Quality-by-Design World, Part VIII: Excipient Specifications. 2010, available at http://www.americanpharmaceuticalreview.com/Featured-Articles/117308-Functionality-and-Performance-of-Excipients-in-Quality-by-Design-World-Part-VIII-Excipient-Specifications/

Basu P. A quality by design approach to the understanding and predicting excipient properties and functionalities. 2009, Available at http://ipec-europe.org/uploads/qbd_approach.pdf.

Rodríguez Valadez JA, Villafuerte Robles L. Functionality of Prosolv Easytab as direct compression excipient. Lat Am J Pharm 2013;32:1476-84.

Kishore VS, Kumar DG, Sudheer B, Sandeep M. Design and development of fast dissolving tablets of ibuprofen. Res Rev: J Pharm Pharmac Scis 2013;2:65-71.

Roni MA, Jalil R. Comparative study of ibuprofen solubility in synthetic and natural Lipid vehicles. Dhaka Univ J Pharm Sci 2011;10:65-6.

Ivanov IT, Tsokeva Z. Effect of chirality on PVP/drug interaction within binary physical mixtures of ibuprofen, ketoprofen, and naproxen: a DSC study. CHIRALITY 2009;21:719–27.

Elkhodairy KA, Hassan MA, Afifi SA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm J 2014;22:53–61.

Sharma A, Jain CP. Preparation and characterization of solid dispersions of carvedilol with PVP K30. Res Pharm Sci 2010;5:49–56.

Kim MJ, Lee JH, Yoon H, Kim SJ, Yeon DY, Jang JE, Lee D, Khang G. Preparation, characterization and in vitro dissolution of aceclofenac-loaded PVP solid dispersions prepared by spray drying or rotary evaporation method. J Pharm Invest 2013;43:107–13.

Vutthipong A, Monton C, Saingam W, Bunluepuech K, Charoonratana T. Evaluation of physicochemical properties of a traditional Thai antihypertensive herbal recipe in various preparations. Int J Pharm Pharm Sci 2014;6:479-82.

Punitha A, Visweswaran S, Muthukumar NJ, Murugesan M. Physico-chemical evaluation and HPTLC finger print of Siddha poly herbal formulation “Swasa kudori mathirai”. Int J Pharm Pharm Sci 2015;7:560-7.

Castillo S, Villafuerte L. Compactibility of binary mixtures of pharmaceutical powders. (1995) Eur J Pharm Biopharm 1995;41:309-14.

Castillo S, Villafuerte L. Compactibility of ternary mixtures of pharmaceutical powders. Pharm Acta Helv 1995;70:329-37.

Díaz Ramírez, CC, Villafuerte Robles L. Surrogate functionality of celluloses as tablet excipients. Drug Dev Ind Pharm 2010;36:1422-35.

Jain H, Pasha TY, Bais CS, Anil B. Formulation and characterization of liquisolid tablets of valsartan for improvement of dissolution rate. Asian J Pharm Clin Res 2014;7:21-6.

USP 35. General information/1174 Powder Flow. The United States Pharmacopoeial Convention. 2011. Pp. 802-3. Also available at http://pharmacopeia.cn/v29240/usp29nf24s0_c1174.html.

Chalmers AA, Elworthy PH. Oxytetracyline tablet formulations: effect of variations in binder concentration and volume on granule and tablet properties. J Pharm Pharmacol 1976;28:228-33.

Szumilo M, Swiander K, Belniak P, Wojciechowsaka J, Poleszak E. The influence of excipients on physical properties of tablets and dissolution of caffeine. Acta Pol Pharm - Drug Research 2015;72:791-7.

Tonglairoum P, Ngawhirunpat T, Akkaramongkolporn P, Opanasopit P, Nattapulwat N. Effect of particle size and diluent type on critical parameters for disintegration of tablets containing croscarmellose sodium as a disintegrant. Trop J Pharm Res 2017;16:1215-21.

Lopez-Solis J, Villafuerte-Robles L. Effect of disintegrants with different hygroscopicity on dissolution of Norfloxacin/Pharmatose DCL 11 tablets. Int J Pharm 2001;216:127–35.

Patel RC, Keraliya RA, Patel MM, Patel NM. Formulation of furosemide solid dispersion with microcrystalline cellulose for achieve rapid dissolution. J Adv Pharm Technol Res 2010;1:180–9.

Agrawal AM, Dudhedia MS, Patel AD, Raikes MS. Characterization and performance assessment of solid dispersions prepared by hot melt extrusion and spray drying process. Int J Pharm 2013;457:71-81.

Garr JSM, Rubinstein MH. The effect of rate of force application on the properties of microcrystalline cellulose and dibasic calcium phosphate mixtures. Int J Pharm 1991;73:75-80.

Hasnain MS, Nayak AK. Solubility and dissolution enhancement of ibuprofen by solid dispersion technique using PEG 6000-PVP K 30 combination carrier. Chemistry: Bulg J Sci Edu 2012;21:118-32.

Chen L, Dang Q, Liu Ch, Chen J, Song L, Chen X. Improved dissolution and anti-inflammatory effect of ibuprofen by solid dispersion. Frontiers of Medicine 2012;6:195–203.

Kshirsagar S J, Bhalekar M R, Madgulkar A R, Sable P N, Gupta B K. Dissolution improvement of poorly water soluble drug valsartan and improving flow properties of solid dispersion. Lat Am J Pharm 2010;29:393-400.

Goddeeris C, Willems T, Van den Mooter G. Formulation of fast disintegrating tablets of ternary solid dispersions consisting of TPGS 1000 and HPMC 2910 or PVPVA 64 to improve the dissolution of the anti-HIV drug UC 781. Eur J Pharm Biopharm 2008;34:293-302.




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