Information de reference pour ce titreAccession Number: | 00009275-201108000-00026.
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Author: | Uchimoto, Takeaki a,1; Iwao, Yasunori a,1; Takahashi, Kana a; Tanaka, Shoko a; Agata, Yasuyoshi a; Iwamura, Takeru b; Miyagishima, Atsuo a; Itai, Shigeru a,*
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Institution: | (a)Department of Pharmaceutical Engineering, School of Pharmaceutical Sciences, University of Shizuoka, Shizuoka, Japan (b)Graduate School of Nutritional and Environmental Sciences, University of Shizuoka, Shizuoka, Japan
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Title: | A comparative study of glycerin fatty acid ester and magnesium stearate on the dissolution of acetaminophen tablets using the analysis of available surface area.[Article]
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Source: | European Journal of Pharmaceutics & Biopharmaceutics. 78(3):492-498, August 2011.
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Abstract: | To study the effect of glycerin fatty acid ester (Poem TR-FB) concentrations on the dissolution rate of acetaminophen (APAP), the dissolution and disintegration behaviors of APAP tablets formulated using various lubricants were examined. The change over time in the available surface area of APAP (S(t)), which is in direct contact with solvent, was also analyzed using these dissolution data. In the dissolution tests, a retarded dissolution of APAP was not observed with TR-FB, whereas magnesium stearate (Mg-St), which is widely used as a lubricant, retarded the dissolution. However, no significant difference in the disintegration time between the two lubricants was observed. With regard to the time course of the S(t), Mg-St at 0.1% gave a maximum surface area value at 9.19 min (peak time); however, the profiles for APAP with Mg-St at greater than 0.5% showed downward curvature indicating a gradual decrease in surface area over time. Conversely, with TR-FB, even when its concentration was increased, the S(t) profile for APAP had a maximum value that was more than twice that of APAP with that of 0.5-3.0% of Mg-St. Scanning electron microscopy (SEM) observations showed that the differences in the dissolution rate and S(t) patterns between Mg-St and TR-FB could be explained by differences in extensibility deriving from their morphology. Therefore, it was concluded that TR-FB does not cause retardation of drug dissolution and may prove to be a superior alternative lubricant to Mg-St.
(C) 2011Elsevier, Inc.
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Author Keywords: | Glycerin fatty acid esters; Magnesium stearate; Dissolution rate; Available surface area; Extensibility.
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References: | [1] W.A. Strickland Jr, E. Nelson, L.W. Busse, T. Higuchi, The physics of tablet compression. IX. Fundamental aspects of tablet lubrication. J. Am. Pharm. Assoc. Am. Pharm. (Baltim). 45 (1956) 51-55.
[2] O.K. Udeala, J.O. Onyechi, S.I. Agu, Preliminary evaluation of dika fat, a new tablet lubricant. J. Pharm. Pharmacol. 32 (1980) 6-9.
[3] L.E. Flores, R.L. Arellano, J.J.D. Esquivel, Lubricant susceptibility of cellactose and Avicel PH-200: a quantitative relationship. Drug Dev. Ind. Pharm. 26 (2000) 297-305.
[4] G. Levy, R.H. Gumtow, Effect of certain tablet formulation factors on dissolution rate of the active ingredient III. Tablet lubricants. J. Pharm. Sci. 52 (1963) 1139-1144.
[5] K.S. Murthy, J.C. Samyn, Effect of shear mixing on in vitro drug release of capsule formulations containing lubricants. J. Pharm. Sci. 66 (1977) 1215-1219.
[6] S.J. Homg, S.K. Kim, Effect of formulation factors on dissolution rate of nitrofurantoin tablet. Soul Taehakkyo Yakhak Nonmunjip. 10 (1985) 25-38.
[7] A.W. Holzer, J. Sjogren, Evaluation of sodium stearyl fumarate as a tablet lubricant. Int. J. Pharm. 2 (1979) 145-153.
[8] Z.T. Chowhan, L.H. Chi, Drug-excipient interactions resulting from powder mixing. IV: role of lubricants and their effect on in vitro dissolution. J. Pharm. Sci. 75 (1986) 542-545.
[9] A.M. Salpekar, L.L. Augsburger, Magnesium lauryl sulfate in tableting: effect on ejection force and compressibility. J. Pharm. Sci. 63 (1974) 289-293.
[10] T. Ugurlu, M. Turkoglu, Hexagonal boron nitride as a tablet lubricant and a comparison with conventional lubricants. Int. J. Pharm. 353 (2008) 45-51.
[11] H. Aoshima, A. Miyagishima, Y. Nozawa, Y. Sadzuka, T. Sonobe, Glycerin fatty acid esters as a new lubricant of tablets. Int. J. Pharm. 293 (2005) 25-34.
[12] T. Uchimoto, Y. Iwao, Y. Ikegami, T. Murata, A. Miyagishima, T. Sonobe, S. Itai, Lubrication properties of potential alternative lubricants, glycerin fatty acid esters, to magnesium stearate. Int. J. Pharm. 386 (2010) 91-98.
[13] Z.T. Chowhan, L.H. Chi, Drug-excipient interactions resulting from powder mixing. III: solid state properties and their effect on drug dissolution. J. Pharm. Sci. 75 (1986) 534-541.
[14] D. Shibata, Y. Shimada, Y. Yonezawa, H. Sunada, N. Otomo, K. Kasahara, Application and evaluation of sucrose fatty acid esters as lubricants in the production of pharmaceuticals. J. Pharm. Sci. Technol. Jpn. 62 (2002) 133-145.
[15] M.R. Billany, J.H. Richards, Batch variation of magnesium stearate and its effect on the dissolution rate of salicylic acid from solid dosage forms. Drug Dev. Ind. Pharm. 8 (1982) 497-511.
[16] V.M. Lethola, J.T. Heinamaki, P. Nikupaavo, J.K. Yliruusi, Effect of some excipients and compression pressure on the adhesion of aqueous-based hydroxypropyl methylcellulose film coatings to tablet surfaces. Drug Dev. Ind. Pharm. 21 (1995) 1365-1375.
[17] S. Kouchiwa, M. Nemoto, S. Itai, H. Murayama, T. Nagai, Prediction of available surface area of powdered particles of flufenamic acid in tablets. Chem. Pharm. Bull. 33 (1985) 1641-1651.
[18] S. Itai, S. Kouchiwa, M. Nemoto, H. Murayama, T. Nagai, Effect of compression pressure and formulation on the available surface area of flufenamic acid in tablets. Chem. Pharm. Bull. 34 (1986) 1264-1274.
[19] J. Wang, H. Wen, D. Desai, Lubrication in tablet formulations. Eur. J. Pharm. Biopharm. 75 (2010) 1-15.
[20] Y. Agata, Y. Iwao, A. Miyagishima, S. Itai, Novel mathematical model for predicting the dissolution profile of spherical particles under non-sink conditions. Chem. Pharm. Bull. 58 (2010) 511-515.
[21] A.C. Shah, A.R. Mlodozeniec, Mechanism of surface lubrication: influence of duration of lubricant-excipient mixing on processing characteristics of powders and properties of compressed tablets. J. Pharm. Sci. 66 (1977) 1377-1382.
[22] F. Ebba, P. Piccerelle, P. Prinderre, D. Opota, J. Joachim, Stress relaxation studies of granules as a function of different lubricants. Eur. J. Pharm. Biopharm. 52 (2001) 211-220.
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Language: | English.
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Document Type: | Research paper.
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Journal Subset: | Pharmacology.
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ISSN: | 0939-6411
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NLM Journal Code: | c4y, 9109778
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DOI Number: | https://dx.doi.org/10.1016/j.ejp...- ouverture dans une nouvelle fenêtre
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