THE INFLUENCE OF MAGNESIUM STEARATE, PURIFIED TALC AND COMBINATION OF BOTH ON TERNARY/QUATERNARY INTERACTIVE MIXTURE OF FREELY AND POORLY WATER-SOLUBLE DRUG
Keywords:
Magnesium stearate, Talc, Interactive mixture, Drug release, Disintegration timeAbstract
Objective: This research purposed to describe and evaluate the influence of magnesium stearate (MgSt), purified talc (talc) and combination of both (MgSt-PT) on ternary/quaternary mixture of freely and poorly water-soluble drug.
Methods: Chlorpheniramine maleate (CPM) and prednisone (PDN) were used as the drug model of freely and poorly water-soluble drug, respectively. Compatibility studies between drugs and lubricants were carried out using Fourier transform infrared spectroscopy (FTIR). Ternary/quaternary interactive mixture of drugs, lubricants and carriers were conducted using granules of lactose-starch (1:1) as carriers with particle size 250 – 425 µm. Characterizations were conducted by homogeneity of mixture, physical properties of granules and tablets and drug releases. The results were analyzed statistically using one-way analysis of variance (ANOVA) with 95% of confidence interval level and dependent method for drug release.
Results: Homogeneity of binary mixture within drug and carrier was achieved in 60 minutes with 20 revolutions per minute. MgSt, talc and combination of both provided stable ternary/quaternary interactive mixture. MgSt affected the reduction of compactibility, prolong the disintegration time, retardation the drug release and talc improved flowability.
Conclusion: Talc provided more preferable effects than MgSt, and combination of both lubricants showed desirable physical properties of tablet. MgSt, talc and combination of both provided no significant effect on physical properties and drug release of CPM as freely water-soluble drug and the significant effect was observed on PDN as poorly water-soluble drug.
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References
Fan LT, Chen YM, Lai FS. Recent development in solids mixing. Pow Technol 1990;61:255-87.
Mendez ASL, de Carli G, Garcia CV. Evaluation powder mixing operation during batch production: application to operational qualification procedure in the pharmaceutical industry. Pow Technol 2010;198:310-3.
Egermann H. Effect of adhesion on mixing homogeneity Part I: ordered adhesion-random adhesion. Pow Technol 1980;27:203-6.
Soebagyo SS, Stewart PJ. The effect of cohesive and non-cohesive ternary component on the homogeneity and stability of a prednisolone interactive mixture. Int J Pharm 1985;25:255-36.
Soebagyo SS, Stewart PJ. The characterization of drug redistribution in a ternary interactive mixture of diazepam. Int J Pharm 1993;91:227-33.
Swaminathan V, Kildsig DO. Effect of magnesium stearate on the content uniformity of active ingredient in pharmaceutical powder mixture. AAPS Pharm Sci Tech 2002;3:1-5.
Hussain MSH, York P, Timmins P. A study of the formation of magnesium stearate film on sodium chloride using energy-dispersive X-ray analysis. Int J Pharm 1988;42:89-95.
Wang J, Wen H, Desai D. Lubricant in tablet formulations. Eur J Pharm Biopharm 2010;75:1-15.
Pingali K, Mendez R, Lewis D, Mickniak-Kohn B, Cuitino A, Muzzio F. Mixing order of glidant and lubricant-influence on powder and tablet properties. Int J Pharm 2011;409:269-77.
Rashid I, Daraghmeh N, Al-Remawi M, Leharne SA, Cowdhry BZ, Badwan A. Characterization of the impact of magnesium stearate lubrication on the tableting properties of chitin-Mg silicate as a superdisintegrating binder when compared to Avicel PH 200. Pow Technol 2010;203:609-19.
Tay T, Morton DAV, Gengenbach TR, Stewart PJ. Dissolution of a poorly water-soluble drug dry coated with magnesium and sodium stearate. Eur J Pharm Biopharm 2012;80:443-52.
Tay T, Das S, Stewart P. Magnesium stearate increases salbutamol sulfate dispersion: what is the mechanism? Int J Pharm 2010;383:62-9.
Dawoodbhai SS, Chueh HR, Rhodes CT. Glidants and lubricant properties of several types of talc. Drug Dev Ind Pharm 1987;13:2441-67.
Gadalla MAF, El-Hameed MHA, Ismail AA. Lubricants as a formulation factor affecting In vitro properties of double compressed tablet. Drug Del Ind Pharm 1988;14:1107-23.
Uchimoto T, Iwao Y, Takahashi K, Tanaka S, Agata Y, Iwamura T, et al. A comparative study of glycerin fatty acid ester and magnesium stearate on the dissolution of acetaminophen tablets using the analysis of available surface area. Eur J Pharm Biopharm 2011;76:492-8.
Fudholi A. Methodology formulationin direct compression. Medika 1983;7(9):586-93.
Jallo LJ, Choroi C, Gurumurthy L, Patel U, Dave RN. Improvement of flow and bulk density of pharmaceutical powders using surface modification. Int J Pharm 2012;423:213-25.
Uchimoto T, Iwao Y, Ikegami Y, Murata T, Sonobe T, Miyagishima A, et al. Lubricant properties of potential alternative lubricants, glycerin fatty acid ester to magnesium stearate. Int J Pharm 2010;286:91-8.
Yuksel N, Kanik AE, Baykara T. Comparison of In vitro dissolution profiles by ANOVA-based, model-dependent and independent methods. Int J Pharm 2000;209:57-67.
Shah VP, Tsong Y, Sathe P, Liu JP. In vitro dissolution profile comparison-statistics and analysis of the similarity factor (f2). Pharm Res 1998;15:889-96.
Costa P, Lobo JMS. Review: modeling and comparison of dissolution profile. EurJ Pharm Sci 2001;13:123-33.
Ainurofiq A, Choiri S. Model and release pattern water-soluble drug from natural polymer-based sustained release tablet dosage form. Int J Pharm Pharm Sci 2014;6(9):179-82.
Allahham A, Stewart PJ, Das SC. Improving the de-agglomeration and dissolution of a poorly water soluble drug by decrease the agglomerate strength of cohesive powder. Int J Pharm 2013;457:101-9.