Compatibility between Magnesium Stearate and Pharmaceutical Acidic Active Compounds/Excipients with DSC

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Abstract:

Compatibility investigation was performed between magnesium stearate and acidic drug compounds (ibuprofen, indomethacin and valproic acid) and acidic pharmaceutical excipients (lactic acid and citric acid) using differential scanning calorimetry (DSC). DSC study indicated the possible incompatibility for the mixture between magnesium stearate and any compounds. Alteration in DSC thermogram was found in all mixtures. The eutectic phenomenon was found in the powder mixture of magnesium stearate and ibuprofen. In addition, the presence of melting endothermic peak of stearic acid in other powder mixtures except the mixture of magnesium stearate and indomethacin indicating breakage of salt form of magnesium stearate. This alteration could relate to the influence on physicochemical properties of drug compounds and pharmaceutical excipients which powder x-ray diffraction (PXRD) and Fourier Transform Infrared Spectroscopy (FT-IR) should be further analyzed to confirm the interactions between compounds.

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190-197

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August 2020

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[1] R.C. Rowe, P.J. Sheskey, M.E. Quinn, Handbooks of pharmaceutical excipients, sixth ed., Pharmaceutical Press, London, (2009).

Google Scholar

[2] S.S. Bharate, S.B. Bharate, A.N. Bajaj, Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review, J. Excip. Food Chem. 1(3) (2010) 1-26.

DOI: 10.1002/chin.201147271

Google Scholar

[3] P. Bracconi, C. Andres, A. Ndiaye, Structural properties of magnesium stearate pseudopolymorphs: effect of temperature, Int. J. Pharm. 262 (2003) 109-124.

DOI: 10.1016/s0378-5173(03)00339-9

Google Scholar

[4] United States Pharmacopeia and National Formulary (USP 32-NF 27), United States Pharmacopeial Convention, Rockville, MD, (2008).

DOI: 10.4135/9781412963855.n1200

Google Scholar

[5] T.T. Kararli, T.E. Needham, C.J. Seul, P.M. Finnegan, Solid state interaction of magnesium oxide and ibuprofen to form a salt, Pharm. Res. 6 (1989) 804-808.

Google Scholar

[6] F. Marcotegui, J.M. Sanchez Monge, Application of differential thermal analysis to study the stability of acetylsalicylic acid in the solid state. I. Hydrolysis of acetylsalicylic acid, Revista Soc. Esp. Farm. Hosp. 5 (1981) 5-10.

Google Scholar

[7] C. Ahlneck, J.O. Waltersson, P. Lundgren, Difference in effect of powdered and granular magnesium stearate on the solid state stability of acetylsalicylic acid, Acta Pharm. Technol. 33 (1987) 21–26.

Google Scholar

[8] T.A. Miller, P. York, Pharmaceutical tablet lubrication, Int. J. Pharm. 41 (1988) 1-19.

Google Scholar

[9] S. Wissing, D.Q.M. Craig, S.A. Barker, W.D. Moore, An investigation into the use of stepwise isothermal high sensitivity DSC as a means of detecting drug-excipient incompatibility, Int. J. Pharm. 199(2) (2000) 141-150.

DOI: 10.1016/s0378-5173(00)00380-x

Google Scholar

[10] R.E. Gordon, C.L. Van Koevering, D.J. Reits, Utilization of differential scanning calorimetry in the compatibility screening of ibuprofen with the stearate lubricants and construction of phase diagrams, Int. J. Pharm. 21 (1984) 99-105.

DOI: 10.1016/0378-5173(84)90206-0

Google Scholar

[11] P.G. Johnston, M. Gillam-Krakauer, M.P. Fuller, J. Reese, Evidence-based use of indomethacin and ibuprofen in the neonatal intensive care unit, Clin. Perinatol. 39(1) (2012) 111-136.

DOI: 10.1016/j.clp.2011.12.002

Google Scholar

[12] Y. Ghodke-Puranika, C.F. Thorn, J.K. Lamba, J.F. Leederf, W. Song, A.K. Birnbaum, R.B. Altman, T.E. Klein, Valproic acid pathway: pharmacokinetics and pharmacodynamics, Pharmacogenet. Genomics. 23(4) (2013) 236-241.

DOI: 10.1097/fpc.0b013e32835ea0b2

Google Scholar

[13] G.P. Bettinetti, P. Mura, A. Liguori, G. Bramanti, F. Giordano, Solubilization and interaction of naproxen with polyvinylpyrrolidone in aqueous solution and in the solid state, Farmaco. 43(11) (1988) 331-343.

Google Scholar

[14] U.I. Leinonen, H.U. Jalonen, P.A. Vihervaara, E.S.U. Laine. Physical and lubrication properties of magnesium stearate, J. Pharm. Sci. 81(12) (1992) 1194-1198.

DOI: 10.1002/jps.2600811214

Google Scholar

[15] M. Roberts, J.L. Ford, G.S. MacLeod, J.T. Fell, G.W. Smith, P.H. Rowe, A.M. Dyas, Effect of lubricant type and concentration on the punch tip adherence of model ibuprofen formulations, J. Pharm. Pharmacol. 56 (2004) 299-305.

DOI: 10.1211/0022357022827

Google Scholar

[16] B. Tita, I. Ledeti, G. Bandur, D. Tita, Compatibility study between indomethacin and excipients in their physical mixtures, J. Therm. Anal. Calorim. 118 (2014) 1293-1304.

DOI: 10.1007/s10973-014-3986-x

Google Scholar

[17] A. Komesu, P.F.M. Martinez, B.H. Lunelli, J. Olivera, M.R.W. Maciel, R.M. Filho, Study of lactic acid thermal behavior using thermoanalytical techniques, J. chem. (Hindawi. Online). 2017 (2017) 1-7.

DOI: 10.1155/2017/4149592

Google Scholar

[18] B.P. Kumar, R.K. Sahu, K.V. Ramamurthy, S. Rao, B. Ramu, A review on mechanism, importance and methods of compatibility testing in formulation of dosage form, J. Chem. Pharm. Sci. 4(4) (2011) 141-151.

Google Scholar