PREPERATION AND CHARACTERIZATION OF β-CYCLODEXTRIN INCLUSION COMPLEXES ORAL TABLETS CONTAINING POORLY WATER SOLUBLE GLIMIPIRIDE USING FREEZE DRYING METHOD
Glimepiride is an oral antidiabetic drugs which is practically insoluble in water. The formation of β-cyclodextrin inclusion complex was able to increase the solubility of glimepiride. This study aim to prepare, characterize and formulation of inclusion complex tablets in order to meet the requirement in Pharmacopeia. The inclusion complex were prepared in a molar ratio of 1:1 and 1:2 by freeze drying method, afterthat characterized include FTIR spectroscopy and scanning electro microscope (SEM). Further, it was formulated into tablets by direct compression technique using primogel and crospovidone as superdisintegrants. The tablets were evaluated include weight uniformity, hardness, friability, disintegration, and dissolution. The dissolution studies of inclusion complex were performed by using USP II apparatus. The result of FTIR and SEM provided evidence of the formation of complexes after utilizing freeze-drying methods. The tablet evaluation containing inclusion complex glimepiride-β cyclodextrin with primogel and cropovidone as disintegrant showed that increased concentration of disintegrant will increase disintegration time of the tablets. All of formulas meet the requirements in the Pharmacopoeia. The inclusion complex of glimepiride–β cyclodextrin successfully used for enhancing the solubility of glimepiride and the tablets meet the requirement in Pharmacopeia.Keywords: Glimepirid, β-cyclodextrin, primogel, crospovidone
Ammar HO., Salama HA., Ghorab M., Mahmoud AA., 2006. Implication of inclusion complexation of glimepiride in cyclodextrin–polymer systems on its dissolution, stability and therapeutic efficacy. Int. J. Pharm. 320 : 53–57.
Challa R., Ahuja A., Ali J., Khar RK., 2005. Cyclodextrins in drug delivery: An updated review. AAPS PharmSciTech 6 : E329–E357.
Figueiras A., Carvalho RA., Ribeiro L., Torres-Labandeira JJ., Veiga FJB., 2007. Solid-state characterization and dissolution profiles of the inclusion complexes of omeprazole with native and chemically modified β-cyclodextrin. Eur. J. Pharm. Biopharm. 67 : 531–539.
Frick A., Möller H., Wirbitzki E., 1998. Biopharmaceutical characterization of oral immediate release drug products. In vitro/in vivo comparison of phenoxymethylpenicillin potassium, glimepiride and levofloxacin. Eur. J. Pharm. Biopharm. 46 : 305–311.
Ilić I., Dreu R., Burjak M., Homar M., Kerč J., Srčič S., 2009. Microparticle size control and glimepiride microencapsulation using spray congealing technology. Int. J. Pharm., Challenges in Nano- Micro- and Macro-Systems 381 : 176–183.
Kawabata Y., Wada K., Nakatani M., Yamada S., Onoue S., 2011. Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int. J. Pharm. 420 : 1–10.
Lee CW., Kim SJ., Youn YS., Widjojokusumo E., Lee YH., Kim J., Lee YW., Tjandrawinata RR., 2010. Preparation of bitter taste masked cetirizine dihydrochloride/β-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process. J. Supercrit. Fluids 55 348–357.
Liu M., Cao W., Sun Y., He Z., 2014. Preparation, characterization and in vivo evaluation of formulation of repaglinide with hydroxypropyl-β-cyclodextrin. Int. J. Pharm. 477 : 159–166.
Michel D., Chitanda JM., Balogh R., Yang P., Singh J., Das U., El-Aneed A., Dimmock J., Verrall R., Badea I., 2012. Design and evaluation of cyclodextrin-based delivery systems to incorporate poorly soluble curcumin analogs for the treatment of melanoma. Eur. J. Pharm. Biopharm. 81 : 548–556.
Ramadhani N., Shabir M., McConville C., 2014. Preparation and characterisation of Kolliphor® P 188 and P 237 solid dispersion oral tablets containing the poorly water soluble drug disulfiram. Int. J. Pharm. 475 : 514–522.
Reven S., Grdadolnik J., Kristl J., Žagar E., 2010. Hyperbranched poly(esteramides) as solubility enhancers for poorly water-soluble drug glimepiride. Int. J. Pharm. 396 : 119–126.
Sajeev KB., Saraswathi R., Dhanaraj SA., 2013. Solid-state characterization studies and effect of PEG 20000 and P90G on particle size reduction and stability of complexed glimepiride nanocrystals. J. Young Pharm. 5 : 83–89.
Santos EH., Kamimura JA., Hill LE., Gomes CL., 2015. Characterization of carvacrol beta-cyclodextrin inclusion complexes as delivery systems for antibacterial and antioxidant applications. LWT - Food Sci. Technol. 60 : 583–592.
Saravana KK., Sushma M., Prasanna RY., 2013. Dissolution Enhancement of Poorly Soluble Drugs by Using Complexation Technique—A Review. J. Pharm. Sci. Res. 5.
Savjani KT., Gajjar AK., Savjani JK., 2012. Drug Solubility: Importance and Enhancement Techniques. Int. Sch. Res. Not. 2012 : e195727.
Shanmuga PA., Sivakamavalli J., Vaseeharan, B., Stalin T., 2013. Improvement on dissolution rate of inclusion complex of Rifabutin drug with β-cyclodextrin. Int. J. Biol. Macromol. 62 : 472–480.
Krishnaiah SRY., 2010. Pharmaceutical Technologies for Enhancing Oral Bioavailability of Poorly Soluble Drugs. J. Bioequivalence Bioavailab. 02 : 28–36.
Sunil SA., Srikanth MV., Rao NS., Raju V., Murthy KVR., 2012. Investigation on in vitro dissolution rate enhancement of indomethacin by using a novel carrier sucrose fatty acid ester. DARU J. Pharm. Sci. 20 : 4.
Taupitz T., Dressman JB., Buchanan CM., Klein S., 2013. Cyclodextrin-water soluble polymer ternary complexes enhance the solubility and dissolution behaviour of poorly soluble drugs. Case example: Itraconazole. Eur. J. Pharm. Biopharm. 83 : 378–387.
Yao Y., Xie Y., Hong C., Li G., Shen H., Ji G., 2014. Development of a myricetin/hydroxypropyl-β-cyclodextrin inclusion complex: Preparation, characterization, and evaluation. Carbohydr. Polym. 110 : 329–337.
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