GLIMEPIRIDE FAST DISINTEGRATING TABLETS: FORMULATION, EVALUATION AND IN-VIVO DISINTEGRATION AND DYNAMIC STUDIES
Keywords:
superdisintegrants, fast disintegrating tablets, disintegration time, water absorption ratio, wetting time, dissolution, dynamic studiesAbstract
Objective: The main objective of the research was to formulate directly compressible fast disintegrating tablets of glimepiride by using different super disintegrants such as crospovidone, croscarmellose sodium, sodium starch glycolate and L-HPC in various concentrations.
Methods: The prepared tablets were evaluated for various tablet properties like weight variation, thickness, hardness, friability, taste, drug content, in vitro and in vivo disintegration time, and in vitro drug release, in vivo dynamic studies. Other parameters such as wetting time, water absorption ratio, and drug-excipient compatibility were also evaluated.
Results: The disintegration time of the optimized fast disintegrating tablet formulation was observed to be 12 s in vitro and 19.80 s in vivo. The correlation was observed between disintegration time and ‘R' for each of the four super disintegrants at the concentrations studied. Considering the ‘R' values and disintegration time, croscarmellose sodium was significantly superior compared to the other super disintegrants tested. Drug release was faster from formulations containing 25% croscarmellose sodium compared to the pure drug and without super disintegrant glimepiride tablet. FTIR studies did not indicate any excipient incompatibility, either during mixing or after compression. Optimized formulation exhibited good results in the decrease in blood glucose in rats when compared to the pure drug and marketed product.
Conclusion: Form the results if this study it can be concluded that prepared optimized fast disintegrating tablets of glimepiride are the better option to treat diabetes.
Keywords: Superdisintegrants, Fast disintegrating tablets, Disintegration time, Water absorption ratio, Wetting time, Dissolution, Dynamic studies
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References
Battu SK, Michael AR, Soumyajit M, Madhusudan Y. Formulation and evaluation of rapidly disintegrating fenoverine tablets: effect of super disintegrants. Drug Dev Ind Pharm 2007;33:1225-32.
Jianwen Q, Xiaoyan L, Robert, Schwartz, Brigid LM, Hogan. Multiple roles for Sox2 in the developing and adult mouse trachea. Development 2009;11:1899–907.
Goel H, Vora N, Rana V. A novel approach to optimize and formulate fast disintegrating tablets for nausea and vomiting. AAPS PharmSciTech 2008;9:774–8.
Tansel C, Aysegul D, Seluck C, Nursabah B. Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients. Drug Dev Ind Pharm 2011;37:260-7.
Wipada S, Praneet O, Prasert A, Tanasait N, Kaewnapa W, Suwannee P. Preparation and evaluation of taste-masked dextromethorphan oral disintegrating tablet. Pharm Dev Technol 2012;17:315-20.
Shery J, Arun S, Anroop N. Preparation and evaluation of fast disintegrating effervescent tablets of glibenclamide. Drug Dev Ind Pharm 2009;35:321-8.
Abdul B, Musarrat R, Asher F. Glimepiride: evidence-based facts, trends, and observations. Vasc Health Risk Manage 2012;8:463–72.
Rikka L, Eero S, Mikko B, Joakim R, Vesa PL, Kristiina, J, et al. Perphenazine solid dispersions for orally fast-disintegrating tablets: physical stability and formulation. Drug Dev Ind Pharm 2010;36:601-13.
Yourong F, Shicheng Y, Seong JH, Susumu K, Kinam P. Orally fast disintegrating tablets: developments, technologies, taste-masking and clinical studies. Crit Rev Ther Drug Carrier Syst 2004;21:433–75.
Rosie ML, Susan B, Kieran C. Orally disintegrating tablets: the effect of recent FDA Guidance on ODT technologies and applications. Pharm Technol 2009;4:1-6.
Goel H, Arora A, Tiwary AK, Rana V. Development and evaluation of a mathematical model to predict disintegration time of fast disintegrating tablets using powder characteristics. Pharm Dev Technol 2011;16:57-64.
Abdelbary A, Elshafeey AH, Zidan G. Comparative effects of different cellulosic-based directly compressed orodispersible tablets on oral bioavailability of famotidine. Carbohydrate Polymers 2009;77:799-806.
Jinichi F, Etsuo Y, Yasuo Y, Katsuhide T. Evaluation of rapidly disintegrating tablets containing glycine and carboxymethylcellulose. Int J Pharm 2006;31:101-09.
Ganesan K, Gani SB, Arunachalam GM. Anti-diabetic Activity of Helicteres isora L. Bark Extracts on Streptozotocin-induced diabetic rats. Int J Pharm Sci Nanotechnol 2009;1:379-82.
Chattopadhyay RR, Bandyopadhyay M. Effect of azadirachta indica leaf extract on serum lipid profile changes in normal and streptozotocin-induced diabetic rats. Afr J Biomed Res 2005;8:101-4.
Puttewar TY, Kshirsagar MD, Chandewar AV, Chikhale RV. Formulation and evaluation of orodispersible tablet of taste masked doxylamine succinate using ion exchange resin. J King Saud University (Sci) 2010;22:229–40.
Riikka L, Eero S, Toukola K, Mikko B, Joakim R, Pekka L, et al. Intraorally fast-dissolving particles of a poorly soluble drug: preparation and in vitro characterization. Eur J Pharm Biopharm 2009;71:271–81.
Shoukri R, Ahmed S, Shamma N. In vitro and in vivo evaluation of nimesulide lyophilized orally disintegrating tablets. Eur J Pharm Biopharm 2009;73:162–71.
Okuda Y, Irisawa Y, Okimoto K, Osawa T, Yamashita S. A new formulation for orally disintegrating tablets using a suspension spray-coating method. Int J Pharm 2009;382:80–7.
Xiao N, Jin S, Xiaopeng H, Wu Y, Zhongtian Y, Jihong H, et al. Strategies to improve dissolution and oral absorption of glimepiride tablets: solid dispersion versus micronization techniques. Drug Dev Ind Pharm 2011;37:727-36.
Li Q, Wei W, Xiaofeng C, Tao H. Evaluation of disintegrating time of rapidly disintegrating tablets by a paddle method. Pharm Dev Technol 2006;11:295–301.
Piera DM, Sante M, Pascal W. Evaluation of different fast melting disintegrants by means of a central composite design. Drug Dev Ind Pharm 2005;31:109–21.
Adamo F, Valentina B, Gian CC, Celestino R, Carlos AFM. Fast dispersible/slow releasing ibuprofen tablets. Eur J Pharm Biopharm 2008:69:335–41.
Abdelbary G, Eouani C, Prinderre P, Joachim J, Reynier J, Piccerelle P. Determination of the in vitro disintegration profile of rapidly disintegrating tablets and correlation with oral disintegration. Int J Pharm 2005;292:29–41.