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Received January 8, 2014
Accepted July 9, 2014
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This is an Open-Access article distributed under the terms of the Creative Commons Attribution Non-Commercial License (http://creativecommons.org/licenses/bync/3.0) which permits
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Process optimization and characterization of carvedilol solid dispersion with hydroxypropyl-β-cyclodextrin and tartaric acid
Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India
Korean Journal of Chemical Engineering, January 2015, 32(1), 132-140(9), 10.1007/s11814-014-0192-2
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Abstract
The present investigation concerns the experimental design in preparing a solid dispersion of ionized carvedilol with hydroxypropyl-β-cyclodextrin (HPβCD), tartaric acid (TA) by adopting ‘kneading technique’. Simplex lattice design has been chosen to develop model equations that correlate the process variables such as HPβCD (mg), TA (mg), and kneading time (min) with the response variables, such as solubility (mg/mL) and drug release (%) from the solid dispersion. Software-generated ANOVA results confirmed the sufficiency of model equations. Results predicted by model equations are in good agreement with that of experimental results. Optimized formulation with variables ‘CV: HPβCD: TA-kneading time’ (200mg: 689.6mg: 227.6mg-45 min) showed complete drug release (~99%) within 15 min and enhanced solubility of 1.89mg/mL. The instrumental analysis (DSC, XRD& FTIR) of the optimized solid dispersion suggests a transformation of crystallinity of drug to amorphous form, due to its complexation with HPβCD. Hence, this combination of drug and carriers suggests an improvement of carvedilol bioavailability.
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References
Nagarwal RC, Srinatha A, Pandit JK, AAPS PharmSciTech., 10, 977 (2009)
Friesen DT, Crew M, Curatolo WJ, Nightingale JAS, Shanker R, Smithey DT, Mol. Pharm., 5, 1003 (2008)
Stella VJ, Addae KWN, Adv. Drug Deliv. Rev., 59, 677 (2007)
Serajuddin ATM, Adv. Drug Deliv. Rev., 59, 603 (2007)
Brittain HG, J. Pharm. Sci., 91, 1573 (2002)
Li M, Davies A, Malek N, Qiao N, Schlindwein W, Trappitt G, Int. J. Pharm., 419, 1 (2011)
Loftsson T, Amiel C, Jansook P, Larsen KL, Messner M, Moya-Ortega MD, Nielsen TT, Sigurdsson HH, Wintgens V, J. Inclus. Phenom. Macro. Chem., 69, 377 (2011)
Rahman MA, Harwansh R, Hussain A, Hussain S, Mirza MA, Curr. Drug Deliv., 8, 330 (2011)
Keck CM, Gohla S, Muller RH, Eur. J. Pharm. Biopharm., 78, 1 (2011)
Lee JK, Kim KB, Lee MH, Intermetallics, 18, 2019 (2010)
Serajuddin ATM, J. Pharm. Sci., 10, 1058 (1999)
Loftsson T, Masson M, Schipper N, Sigurdsson HH, Pharmazie, 59, 25 (2004)
Cevallos PAP, Buera MP, Elizalde BE, J. Food Eng., 99(1), 70 (2010)
Duchene D, Wouessidjewe D, Drug Dev. Ind. Pharm., 16, 2487 (1990)
Misiuk W, Zalewska M, Carbohydr. Polym., 77, 482 (2009)
Lewis GA, Mathieu D, Luu RPT, Pharmaceutical experimental design, CRC Press, New York.
James Goodnight., JMP 10 Design of Experiments Guide, SAS Publishing, Cary, 177 (2012)
Pokharkar V, Dhar S, Khanna A, Mandpe L, Venkatpurwar V, Acta Pharm., 59, 121 (2009)
Karasov WH, Diamond JM, J. Comp. Physiol. [B], 152, 105 (1983)
Bouer R, Barthe L, Houin G, Philibert C, Tournaire C, Woodley J, Fundam Clin Pharmacol., 13, 494 (1999)
Mura P, Bramanti G, Faucci MT, Manderioli A, J. Incl. Phenom. Macroc. Chem., 39, 131 (2001)
Labanderia JJT, Diaz MTE, Kata M, Jato JLV, Eur. J. Pharm. Sci., 1, 291 (1994)
Ginski MJ, Polli JE, Taneja R, Int. J. Pharm., 177, 117 (1999)
Paradkar A, Ambike AA, Jadhav BK, Mahadik KR, Int. J. Pharm., 271, 281 (2004)
Wang J, Cao Y, Sun B, Wang C, Food Chem., 124, 1069 (2011)
Shamma RN, Basha M, Powder Technol., 237, 406 (2013)
Pincu E, Meltzer V, Cent. Eur. J. Chem., 10, 1584 (2012)
Pokharkar VB, Mandpe LP, Padamwar MN, Ambike AA, Mahadik KR, Paradkar A, Powder Technol., 167(1), 20 (2006)
Friesen DT, Crew M, Curatolo WJ, Nightingale JAS, Shanker R, Smithey DT, Mol. Pharm., 5, 1003 (2008)
Stella VJ, Addae KWN, Adv. Drug Deliv. Rev., 59, 677 (2007)
Serajuddin ATM, Adv. Drug Deliv. Rev., 59, 603 (2007)
Brittain HG, J. Pharm. Sci., 91, 1573 (2002)
Li M, Davies A, Malek N, Qiao N, Schlindwein W, Trappitt G, Int. J. Pharm., 419, 1 (2011)
Loftsson T, Amiel C, Jansook P, Larsen KL, Messner M, Moya-Ortega MD, Nielsen TT, Sigurdsson HH, Wintgens V, J. Inclus. Phenom. Macro. Chem., 69, 377 (2011)
Rahman MA, Harwansh R, Hussain A, Hussain S, Mirza MA, Curr. Drug Deliv., 8, 330 (2011)
Keck CM, Gohla S, Muller RH, Eur. J. Pharm. Biopharm., 78, 1 (2011)
Lee JK, Kim KB, Lee MH, Intermetallics, 18, 2019 (2010)
Serajuddin ATM, J. Pharm. Sci., 10, 1058 (1999)
Loftsson T, Masson M, Schipper N, Sigurdsson HH, Pharmazie, 59, 25 (2004)
Cevallos PAP, Buera MP, Elizalde BE, J. Food Eng., 99(1), 70 (2010)
Duchene D, Wouessidjewe D, Drug Dev. Ind. Pharm., 16, 2487 (1990)
Misiuk W, Zalewska M, Carbohydr. Polym., 77, 482 (2009)
Lewis GA, Mathieu D, Luu RPT, Pharmaceutical experimental design, CRC Press, New York.
James Goodnight., JMP 10 Design of Experiments Guide, SAS Publishing, Cary, 177 (2012)
Pokharkar V, Dhar S, Khanna A, Mandpe L, Venkatpurwar V, Acta Pharm., 59, 121 (2009)
Karasov WH, Diamond JM, J. Comp. Physiol. [B], 152, 105 (1983)
Bouer R, Barthe L, Houin G, Philibert C, Tournaire C, Woodley J, Fundam Clin Pharmacol., 13, 494 (1999)
Mura P, Bramanti G, Faucci MT, Manderioli A, J. Incl. Phenom. Macroc. Chem., 39, 131 (2001)
Labanderia JJT, Diaz MTE, Kata M, Jato JLV, Eur. J. Pharm. Sci., 1, 291 (1994)
Ginski MJ, Polli JE, Taneja R, Int. J. Pharm., 177, 117 (1999)
Paradkar A, Ambike AA, Jadhav BK, Mahadik KR, Int. J. Pharm., 271, 281 (2004)
Wang J, Cao Y, Sun B, Wang C, Food Chem., 124, 1069 (2011)
Shamma RN, Basha M, Powder Technol., 237, 406 (2013)
Pincu E, Meltzer V, Cent. Eur. J. Chem., 10, 1584 (2012)
Pokharkar VB, Mandpe LP, Padamwar MN, Ambike AA, Mahadik KR, Paradkar A, Powder Technol., 167(1), 20 (2006)
