Preparation and physicochemical properties of niclosamide anhydrate and two monohydrates

International Journal of Pharmaceutics

Volumn 269, Issue 2, 2004, Pages 417-432

  Van Tonder, Elsa C ^a   Maleka, Tshoane S P ^b   Liebenberg, Wilna ^a   Song, Mingna ^d   Wurster, Dale Eric ^c   De Villiers, Melgardt M ^d  

^a NORTH WEST UNIVERSITY   (South Africa)

^b Medicines Control Council   (South Africa)

^c UNIVERSITY OF IOWA   (United States)

^d UNIVERSITY OF LOUISIANA AT MONROE   (United States)

Author keywords

Hydrates; Moisture adsorption; Niclosamide; Solubility; Stability; Transformation

Indexed keywords

NICLOSAMIDE; NICLOSAMIDE A; NICLOSAMIDE B; UNCLASSIFIED DRUG;

ADSORPTION; ARTICLE; CALORIMETRY; CRYSTAL; CRYSTALLIZATION; DESORPTION; DIFFERENTIAL SCANNING CALORIMETRY; DIFFUSION; DRUG SCREENING; DRUG SOLUBILITY; DRUG STABILITY; DRUG SYNTHESIS; HIGH TEMPERATURE; HUMIDITY; KINETICS; MOISTURE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RANDOMIZATION; TEMPERATURE MEASUREMENT; THERMAL ANALYSIS; THERMOGRAVIMETRY; TITRIMETRY; X RAY POWDER DIFFRACTION;

EID: 0347360187     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2003.09.035     Document Type: Article

References (23)

1. British Pharmacopeia, 1993. Her Majesty's Stationary Office, London, p. 445.
2. Brittain, H.G., 1995. Physical Characterization of Pharmaceutical Solids. Marcel Dekker, New York, pp. 322-327.
3. Burger A., Griesser U.J. The polymorphic drug substances of the European Pharmacopoeia. Part 7. Physical stability, hygroscopicity, and solubility of succinylsulfathiazole crystal forms. Eur. J. Pharm. Biopharm. 37:1991;118-124.
4. Caira M.R., Van Tonder E.C., De Villiers M.M., Lötter A.P. Diverse modes of solvent inclusion in crystalline pseudopolymorphs of the anthelmintic drug niclosamide. J. Incl. Phenom. Mol. Rec. Chem. 31:1998;1-16.
5. Flynn J.H., Wall L.A. Quick, direct method for determination of activation energy from thermogravimetric data. Pol. Lett. 4:1966;323-328.
6. Giron D. Thermal analysis and calorimetric methods in the characterization of polymorphs and solvates. Therm. Acta. 248:1995;1-59.
7. Guillory, J.K., Erb, D.M., 1985. Using solution calorimetry to quantitate binary mixtures of the three crystalline forms of sulfamethoxazole. Pharm. Manufact., 2, Sept, 29-33.
8. Heidemann D.R., Jarosz J. Preformulation studies involving moisture uptake in solid dosage forms. Pharm. Res. 8:1991;292-297.
9. Khankhari R.K., Grant D.W. Pharmaceutical hydrates. Therm. Acta. 248:1995;61-79.
10. Kosheleva L.I., Bekhli A.F. Polymorphic modifications of phenasal and their IR spectra. Khimiko-farmatsevticheskii Zhurnal. 8:1974;57-60.
11. Kosheleva L.I., Shumakovich I.E., Bekhli A.F. IR spectra and structure of substituted salicylanilides. Zhurnal Obshchei Khimii. 45:1975;407-411.
12. Lindenbaum, S., Mcgraw, S.E., 1985. The identification and characterization of polymorphism in drug solids by solution calorimetry. Pharm. Manufact., 2, Jan, 27-30.
13. Lötter A.P., Flanagan D.R., Palepu N.R., Guillory J.K. A simple reproducible method for determining dissolution rates of hydrophobic powders. Pharm. Technol. 7:1983;55-66.
14. Maleka, T.S.P., 2000. Aqueous adsorption and desorption behaviour of niclosamide anhydrate and monohydrates. M.Sc. Dissertation, Potchefstroom University for CHE, South Africa.
15. Merck Index, 13th ed., 2001. Merck, New Jersey, p. 1030.
16. Moffat, A.C., Jackson, J.V., Moss, M.S., Widdop, B., 1986. Clarke's Isolation and Identification of Drugs in Pharmaceuticals, Body Fluids, and Post-mortem Materials, 2nd ed. Pharmaceutical Press, London.
17. Nyqvist H. Saturated salt solutions for maintaining specified relative humidities. Int. J. Pharm. Technol. Prod. Manufact. 4:1983;47-48.
18. Reynolds, J.G.F., 1993. Martindale: The Extra Pharmacopeia, 30th ed. Pharmaceutical Press, London, p. 48.
19. Singh P., Desai S.J., Flanagan D.R., Simonelli A.P., Higuchi W.I. Mechanistic study of the influence of micelle solubilization and hydrodynamic factors on the dissolution rate of solid drugs. J. Pharm. Sci. 57:1968;959-965.
20. Van Tonder, E.C., 1996. Preparation and characterisation of niclosamide crystal modifications. Ph.D. Thesis, Potchefstroom University for CHE, South Africa.
21. Van Tonder E.C., Lötter A.P., De Villiers M.M., Caira M.R., Liebenberg W. Correlation between hydrate formation and the physical instability of suspensions prepared with different niclosamide crystal forms. Pharm. Ind. 60:1998;722-725.
22. Wells, J.I., Aulton, M.E., 1988. Preformulation. In: Aulton, M.E. (Ed.), Pharmaceutics: The Science of Dosage Form Design. Churchill, New York, pp. 223-253.
23. Yoshihashi Y., Makita M., Yamamura S., Fukuoka E., Terarda K. Determination of the heat of hydration and hydration kinetics of theophylline by thermal analysis. Chem. Pharm. Bull. 46:1998;1148-1152.