Compatibility of the antitumoral β-lapachone with different solid dosage forms excipients
作者： Marcílio S.S. Cunha-Filho , Ramón Martínez-Pacheco , Mariana Landín
DOI: 10.1016/J.JPBA.2007.08.016
关键词: Fourier transform infrared spectroscopy 、 Differential scanning calorimetry 、 Infrared spectroscopy 、 Nuclear chemistry 、 Mannitol 、 Chemistry 、 Excipient 、 Stereochemistry 、 Magnesium stearate 、 Diluent 、 Dosage form
摘要: Abstract The objective of the present study was to evaluate compatibility β-lapachone (βLAP), an antitumoral drug in clinical phase, with pharmaceutical excipients common use including diluents, binders, disintegrants, lubricants and solubilising agents. Differential scanning calorimetry (DSC) used for a first screening find small variations peak temperatures and/or their associated enthalpy six drug/excipient combinations (magnesium stearate, sodium estearyl fumarate, dicalcium phosphate dihydrate, mannitol, randomized methyl-β-cyclodextrin hydroxypropyl-β-cyclodextrin), which indicate some degree interaction. Additional studies using Fourier transformed infrared spectroscopy (FTIR), optical microscopy (OM) heating–cooling DSC (HC-DSC) confirmed incompatibility βLAP magnesium stearate dihydrate. Those should be avoided development solid dosage forms.
elsevier.com
sci-hub.se 参考文章(24)
Paul J Sheskey, Marian E Quinn, Raymond C Rowe, Handbook of Pharmaceutical Excipients ,(1994)
Arthur B. Pardee, Chuanlin Wang, Chiang J. Li, Induction of Apoptosis by β-Lapachone in Human Prostate Cancer Cells Cancer Research. ,vol. 55, pp. 3712- 3715 ,(1995)
A. Marini, V. Berbenni, S. Moioli, G. Bruni, P. Cofrancesco, C. Margheritis, M. Villa, Drug-excipient compatibility studies by physico-chemical techniques; The case of Indomethacin Journal of Thermal Analysis and Calorimetry. ,vol. 73, pp. 529- 545 ,(2003) , 10.1023/A:1025426012578
Shelly Wuerzberger, David A. Boothman, George Wilding, Paul Hutson, Dawn R. Church, Benjamin Frydman, Sarah M. Planchon, Donald T. Witiak, β-Lapachone-mediated Apoptosis in Human Promyelocytic Leukemia (HL-60) and Human Prostate Cancer Cells: A p53-independent Response Cancer Research. ,vol. 55, pp. 3706- 3711 ,(1995)
M. Landín, R.C. Rowe, P. York, Particle size effects on the dehydration of dicalcium phosphate dihydrate powders International Journal of Pharmaceutics. ,vol. 104, pp. 271- 275 ,(1994) , 10.1016/0378-5173(94)90167-8
George Pyramides, John W. Robinson, S. William Zito, The combined use of DSC and TGA for the thermal analysis of atenolol tablets Journal of Pharmaceutical and Biomedical Analysis. ,vol. 13, pp. 103- 110 ,(1995) , 10.1016/0731-7085(94)00112-F
M. Landín, M. J. Fontao, R. Martínez-Pacheco, A Comparison of Trehalose Dihydrate and Mannitol as Stabilizing Agents for Dicalcium Phosphate Dihydrate Based Tablets Drug Development and Industrial Pharmacy. ,vol. 31, pp. 249- 256 ,(2005) , 10.1081/DDC-52040
Marcílio S. S. Cunha-Filho, Bruno Dacunha-Marinho, Juan J. Torres-Labandeira, Ramón Martínez-Pacheco, Mariana Landin, Characterization of β-lapachone and methylated β-cyclodextrin solid-state systems Aaps Pharmscitech. ,vol. 8, ,(2007) , 10.1208/PT0803060
G. G. G. Oliveira, H. G. Ferraz, J. S. R. Matos, Thermoanalytical study of glibenclamide and excipients Journal of Thermal Analysis and Calorimetry. ,vol. 79, pp. 267- 270 ,(2005) , 10.1007/S10973-005-0047-5
P. Corvi Mora, M. Cirri, P. Mura, Differential scanning calorimetry as a screening technique in compatibility studies of DHEA extended release formulations. Journal of Pharmaceutical and Biomedical Analysis. ,vol. 42, pp. 3- 10 ,(2006) , 10.1016/J.JPBA.2006.02.038