Cefdinir: A comparative study of anhydrous vs. monohydrate form. Microstructure and tabletting behaviour

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 64, Issue 2, 2006, Pages 212-221

  Cabri, Walter ^a   Ghetti, Paolo ^a   Alpegiani, Marco ^a   Pozzi, Giovanni ^a   Justo Erbez, Angel ^b   Pérez Martínez, José Ignacio ^c   Villalón Rubio, Rosario ^c   Monedero Perales, M Carmen ^c   Muñoz Ruiz, Angel ^c  

^a R and D Department   (Italy)

^b INSTITUTO DE CIENCIA DE MATERIALES DE SEVILLA   (Spain)

^c UNIVERSITY OF SEVILLE   (Spain)

Author keywords

Cefdinir; Dissolution profiles; Microstructural analysis; Tablets; X ray diffraction

Indexed keywords

CEFDINIR; MALTODEXTRIN; MERCURY;

ARTICLE; COMPARATIVE STUDY; COMPRESSION; CRYSTAL STRUCTURE; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; DRUG STRUCTURE; PHYSICAL CHEMISTRY; TABLET; X RAY DIFFRACTION;

ANTI-INFECTIVE AGENTS; CALORIMETRY, DIFFERENTIAL SCANNING; CEPHALOSPORINS; CHEMISTRY, PHARMACEUTICAL; MICROSCOPY, ELECTRON, SCANNING; MOLECULAR STRUCTURE; PARTICLE SIZE; PHOTOMICROGRAPHY; POLYSACCHARIDES; SOLUBILITY; SPECTROPHOTOMETRY, INFRARED; SPECTROPHOTOMETRY, ULTRAVIOLET; TABLETS; TECHNOLOGY, PHARMACEUTICAL; THERMOGRAVIMETRY; TRANSITION TEMPERATURE; WATER; X-RAY DIFFRACTION;

EID: 33748181565     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2006.05.007     Document Type: Article

References (37)

1. Inamoto Y., Chiba T., Kamimura T., and Takaya T. FK 482, a new orally active cephalosporin synthesis and biological properties. J. Antibiot. 41 (1988) 828-830
2. Neu H.C., Saha G., and Chin N.X. Comparative in vitro activity and beta-lactamase stability of FK482, a new oral cephalosporin. Antimicrob. Agents Chemother. 33 (1989) 1795-1800
3. Mine Y., Yokota Y., Wakai Y., Kamimura T., Tawara S., Shibayama F., Kikuchi H., and Kuwahara S. In vivo antibacterial activity of FK482, a new orally active cephalosporin. J. Antibiot. 41 (1988) 1888-1895
4. Sakamoto H., Hirose T., Nakamoto S., Hatano K., Shibayama F., Kikuchi H., Mine Y., and Kuwahara S. Pharmacokinetics of FK482, a new orally active cephalosporin, in animals. J. Antibiot. 41 (1988) 1896-1905
5. Mikamo H., Izumi K., Ito K., Katoh N., Watanabe K., Ueno K., and Tamaya T. Study on treatment of bacterial vaginosis with oral administration of metronidazole or cefdinir. Chemotherapy 40 (1994) 362-368
6. T. Takaya, H. Takasugui, T. Masugui, H. Yamamaka, K. Kawabata, 7-Substitutes-3-vynil-3-cephem compound and processes for production of the same, US Patent 4,559,334, 1985.
7. T. Takaya, F. Shirai, H. Nakamura, Y. Inaba, Crystalline 7-(2-(2-aminothiazol-4-YL)-2-Hydroxyiminoacetamido)-3Vinyl-3-cephem-4- carboxylic acid (syn isomer), US Patent 4,935,507, 1990.
8. H. Sturm, S. Wolf, J. Ludescher, Crystalline amine salt of Cefdinir, US Patent 6,350,869, 2002.
9. Okamoto Y., Kiriyama K., Namiki Y., Fujioka M., and Yasuda T. Degradation kinetics and isomerization of cefdinir, a new oral cephalosporin, in aqueous solution 1. J. Pharm. Sci. 85 (1996) 976-983
10. Okamoto Y., Kiriyama K., Namiki Y., Matsushita J., Fujioka M., and Yasuda T. Degradation kinetics and isomerization of cefdinir, a new oral cephalosporin in aqueous solution. 2. Hydrolytic degradation pathway and mechanism for β-lactam ring opened lactones1. J. Pharm. Sci. 85 (1996) 984-989
11. Muñoz-Ruiz A., Monedero M.C., Velasco M.V., and Jiménez-Castellanos M.R. A Physical and rheological properties of raw materials. S.T.P. Pharma Sci. 3 (1993) 307-312
12. Muñoz Ruiz A., Payán T., Justo A., Velasco M.V., and Jiménez-Castellanos M.R. A X-ray tablet and raw diffraction as method to study compression parameters in a direct compression excipients. Int. J. Pharm. 144 (1996) 147-152
13. Muñoz Ruiz A., Gallego R., Pozo R.M., Jiménez-Castellanos M.R., and Domínguez-Abascal J. A comparison of three methods to correct the accuracy of displacement measurements by instrumented single punch tablet machines. Drug Dev. Ind. Pharm. 21 (1995) 215-227
14. Lowell S., and Shield J.E. Powder Surface Area and Porosity. 2nd ed. (1984), Chapman and Hall, New York pp. 130-141
15. Avnir D. The Fractal Approach to Heterogeneous Chemistry (1989), Wiley, New York pp. 78-84
16. Cao W., Bates S., Peck G.E., Wildfong P.L.D., Qiu Z., and Morris K. Quantitative determination of polymorphic composition in intact compacts by parallel-beam X-ray powder diffractometry. J. Pharm. Biomed. Anal. 30 (2002) 1111-1119
17. Brittain H.G. Spectral methods for the characterization of polymorphs and solvates. J. Pharm. Sci. 86 (1997) 405-412
18. Ito S., Nishimura M., Kobayashi Y., Itai S., and Yamamoto K. Characterization of polymorphs and hydrates of GK-128 a serotonin receptor agonist. Int. J. Pharm. 151 (1997) 133-143
19. Di Martino P., Barthélémy C., Palmieri G.F., and Martelli S. Physical characterization of naproxen sodium hydrate and anhydrate forms. Eur. J. Pharm. Sci. 14 (2001) 293-300
20. Rollinger J.M., Gstrein E.M., and Burger A. Crystal forms of torasemide: new insight. Eur. J. Pharm. Biopharm. 53 (2001) 75-86
21. Ford J.L., and Timmins P. Pharmaceutical Thermal Analysis. Techniques and Applications (1989), Ellis Horwood, Chichester pp. 205-220
22. Umprayn K., and Mendes R.W. Hygroscopicity and moisture adsorption kinetics of pharmaceutical solid: a review. Drug Dev. Ind. Pharm. 13 (1987) 653-693
23. Coelho M.C., and Harnby N. Moisture bonding in powders. Powder Technol. 20 (1978) 197-200
24. Khankari R.J., and Grant D.J.W. Pharmaceutical hydrates. Thermochim. Acta 248 (1995) 61-79
25. Di Martino P., Piva F., Conflant P., and Guyot-Hermann A.M. Thermal analysis and powder X-ray diffraction study of terpin. Evidence of a eutectic 'hydrate /anhydrous form'. J. Therm. Anal. Calorim. 57 (1999) 95-109
26. Han J., and Suryanarayanan R. Applications of pressure differential scanning calorimetry in the study of pharmaceutical Tucker, hydrates I. Carbamazepine dehydrate. Int. J. Pharm. 157 (1997) 209-218
27. Fini A., Fazio G., Rabasco A.M., Fernández M.J., and Holgado M.A. Effect of temperature on a hydrate diclofenac salt. Int. J. Pharm. 181 (1999) 95-106
28. Hintz R.J., and Johnson K.C. The effect of particle size distribution on dissolution rate and oral absorption. Int. J. Pharm. 51 (1989) 9-17
29. Balbach S., and Korn C. Pharmaceutical evaluation of early development candidates "the 100 mg-approach". Int. J. Pharm. 275 (2004) 1-12
30. Brittain H.G., and Byrn S.R. Structural aspects of polymorphism. In: Brittain H.G. (Ed). Polymorphism in Pharmaceutical Solids vol. 95 (1999), Marcel Dekker, New York 73-124
31. Fernández M.J., Holgado M.A., Rabasco A.M., Fazio G., and Fini A. Use of fractal geometry on the characterization of particles morphology. Application to diclofenac hydroxyethylpyrrolidone. Int. J. Pharm. 108 (1994) 187-194
32. Vippagunta R.S., Brittain H.G., and Grant D.J.W. Crystalline solids. Adv. Drug Delivery Rev. 48 (2001) 3-26
33. Suryanarayanan R. Determination of the relative amounts of anhydrous carbamazepine (C15H12N2o) and carbamazepine dehydrate in a mixture by powder X-ray diffractometry. Pharm. Res. 6 (1989) 1017-1024
34. Kamat M.S., Osawa T., DeAngelis R.J., Koyama Y., and DeLuca P.P. Estimation of the degree of crystallinity of cefazolin sodium by X-ray and infrared methods. Pharm. Res. 5 (1988) 426-429
35. Debnath S., Predecki P., and Suryanarayanan R. Use of glancing angle X-ray powder diffractometry to depth profile phase transformations during dissolution of indomethacin and theophylline tablets. Pharm. Res. 21 (2004) 149-159
36. García E., Vessler S., Boistelle R., and Hoff C. Crystallization and dissolution of pharmaceutical compounds. An experimental approach. J. Crystal Growth 199 (2000) 1360-1364
37. Swannepoel E., Liebengerg W., and M de Villiers M. Quality evaluation of generic drugs by dissolution test: changing the USP dissolution medium to distinguish between active and non-active mebendazole polymorphs. Eur. J. Pharm. Biopharm. 55 (2003) 345-349