Excipient selection can significantly affect solid-state phase transformation in formula wet granulation

AAPS PharmSciTech

Volumn 6, Issue 2, 2005, Pages

  Airaksinen, Sari ^a   Karjalainen, Milja ^a   Kivikero, Niina ^a   Westermarck, Sari ^b   Shevchenko, Anna ^b   Rantanen, Jukka ^a  

^a UNIVERSITY OF HELSINKI   (Finland)

^b ORION CORPORATION   (Finland)

Author keywords

Near infrared spectroscopy; Nitrofurantoin; Sorption; X ray powder diffraction

Indexed keywords

ALPHA LACTOSE; HYDROXYPROPYLCELLULOSE; LACTOSE; MICROCRYSTALLINE CELLULOSE; NITROFURANTOIN; PROSOLV 50; STA RX 1500;

ARTICLE; CONTROLLED STUDY; DRUG DOSAGE FORM; DRUG FORMULATION; DRUG GRANULATION; DRUG STABILITY; DRUG STORAGE; NEAR INFRARED SPECTROSCOPY; PHASE TRANSITION; SOLID STATE; WATER CONTENT; WETTABILITY; X RAY POWDER DIFFRACTION;

EID: 27744515510     PISSN: 15309932     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/pt060241     Document Type: Article

References (37)

1. York P. Solid-state properties of powders in the formulation and processing of solid dosage forms. Int J Pharm. 1983;14:1-28.
2. Morris KR, Griesser UJ, Eckhardt CJ, Stowell JG. Theoretical approaches to physical transformations of active pharmaceutical ingredients during manufacturing processes. Adv Drug Deliv Rev. 2001;48:91-114.
3. FDA. PAT: a framework for innovative pharmaceutical development, manufacturing and quality assurance. In: Guidance for Industry. Rockville, MD: US. Food and Drug Administration: 2004.
4. Yu LX, Lionberger RA, Raw AS, D'Costa R, Wu H, Hussain AS. Applications of process analytical technology to crystallization processes. Adv Drug Deliv Rev. 2004:56:349-369.
5. Grant DJ, Byrn SR. A timely re-examination of drug polymorphism in pharmaceutical development and regulation. Adv Drug Deliv Rev. 2004;56:237-239.
6. Ahlneck C, Zografi G. The molecular basis of moisture effects on the physical and chemical stability of drugs in the solid state. Int J Pharm. 1990;62:87-95.
7. Hancock BC, Zografi G. Characteristics and significance of amorphous state in pharmaceutical systems. J Pharm Sci. 1997;86: 1-12.
8. Kontny MJ. Distribution of water in solid pharmaceutical systems. Drug Dev Ind Pharm. 1988; 14:1991-2027.
9. Stubberud L, Arwidsson HG, Graffner C. Water-solid interactions: I. A technique for studying moisture sorptio/desorption. Int J Pharm. 1995;114:55-64.
10. Phadnis NV, Suryanarayanan R. Polymorphism in anhydrous theophylline - implications on the dissolution rate of theophylline tablets. J Pharm Sci. 1997;86:1256-1263.
11. Newman AW, Byrn SR. Solid-state analysis of the active pharmaceutical ingredient in drug products. Drug Discovery Today. 2003;8:898-905.
12. Airaksinen S, Karjalainen M, Räsänen E, Rantanen J, Yliruusi J. Comparison of the effects of two drying methods on polymorphism of theophylline. Int J Pharm. 2004;276:129-141.
13. Buckton G, Darcy P. The influence of additives on the recrystallisation of amorphous spray dried lactose. Int J Pharm. 1995;121:81-87.
14. Herman J, Visavarungroj N, Remon JP. Instability of drug release from anhydrous theophylline-microcrystalline cellulose formulations. Int J Pharm. 1989;55:143-146.
15. Kontny MJ, Zografi G. Sorption of water by solids. In: Brittain HG, ed. Physical Characterization of Pharmaceutical Solids. New York: Marcel Dekker Inc; 1995:387-418.
16. Zografi G. States of water associated with solids. Drug Dev Ind Pharm. 1988;14:1905-1926.
17. Pienaar EW, Caira MR, Lötter AP. Polymorphs of nitrofurantoin.I. Preparation and X-ray crystal structures of two monohydrated forms of nitrofurantoin. J Cryst Spectrosc Res. 1993;23:739-744.
18. Pienaar EW, Caira MR, Lötter AP. Polymorphs of nitrofurantoin. 2. Preparation and X-ray crystal structures of two anhydrous forms of nitrofurantoin. J Cryst Spectrosc Res. 1993;23:785-790.
19. Caira MR, Pienaar EW, Lötter AP. Polymorphism and pseudopolymorphism of the antibacterial nitrofurantoin. Mol Cryst Li Qcryst. 1996;279:241-264.
20. Otsuka M, Matsuda Y. The effect of humidity on hydration kinetics of mixtures of nitrofurantoin anhydride and diluents. Chem Pharm Bull. 1994;42:156-159.
21. Kishi A, Otsuka M, Matsuda Y. The effect of humidity on dehydration behavior of nitrofurantoin monohydrate studied by humidity controlled simultaneous instrument for X-ray diffractometry and differential scanning calorimetry (XRD-DSC). Colloid Surf B: Biointerfaces. 2002;25:281-291.
22. Khankari RK, Grant DJW. Pharmaceutical hydrates. Thermochimica Acta, 1995;248:61-79.
23. Savitzky A, Golay M. Smoothing and differentiation of data by simplified least squares procedures. Anal Chem. 1964;36:1627-1639.
24. Otsuka M, Teraoka R, Matsuda Y. Physicochemical properties of nitrofurantoin anhydrate and monohydrate and their dissolution. Chem Pharm Bull. 1991;39:2667-2670.
25. Airaksinen S, Luukkonen P, Jørgensen A, Karjalainen M, Rantanen J, Yliruusi J. Effects of excipients on hydrate formation in wet masses containing theophylline. J Pharm Sci. 2003;92:516-528.
26. Zhou GX, Ge Z, Dorwart J, et al. Determination and differentation of surface and bound water in drug substances by near-infrared spectroscopy. J Pharm Sci. 2003:92:1058-1065.
27. Bronlund J, Paterson T. Moisture sorption isotherms for crystalline, amorphous and predominantly crystalline lactose powders. Int Dairy J. 2004;14:247-254.
28. Zografi G, Kontny MJ, Yang AYS, Brenner GS. Surface area and water vapor sorption of microcrystalline cellulose. Int J Pharm. 1984;18:99-116
29. Heidemann DR, Jarosz: PJ. Preformulation studies involving moisture uptake in solid dosage forms. Pharm Res. 1991;8:292-297.
30. Kibbe AH. Starch, pregelatinized. In: Kibbe AH, ed. Handbook of Pharmaceutical Excipients. 3rd ed. Washington DC: American Pharmaceutical Association; 2000:528-530.
31. Delwiche SR, Pitt RE, Norris KH. Examination of starch-water and cellulose-water interactions with near-infrared (NIR) diffuse reflectance spectroscopy. Starch. 1991;43:415-422.
32. Kawashima Y, Takeuchi H, Hino T, et al. The effects of particle size, degree of hydroxypropyl substittution and moisture content of low-substituted hydroxypropylcellulose on the compactibility of acetaminophen and the drug release rate of the resultant tablets. STP Pharma Sci. 1993;3:170-177.
33. Garnier S, Petit S, Coquerel G. Dehydration mechanism and crystallization behavior of lactose. J Therm Anal Calorim. 2002;68:489-502.
34. Fukuoka M, Ohta K, Watanabe H. Determination of terminal extent of starch gelatinization in a limited water system by DSC. J Food Eng. 2002;53:39-42.
35. Alvarez-Lorenzo C, Gómez-Amoza JL, Martinez-Pacheco R, Souto C, Concheiro A. Interactions between hydroxylpropylcelluloses and vapour/ liquid water. Eur J Pharm Biopharm. 2000;50:307-318.
36. Taylor LS, Langkilde FW, Zografi G. Fourier transform Raman spectroscopic study of the interaction of water vapor with amorphous polymers. J Pharm Sci. 2001;90:888-901.
37. Zhang GGZ, Law D, Schmitt EA, Qiu Y. Phase transformation considerations during process development and manufacture of solid oral dosage forms. Adv Drug Deliv Rev. 2004;56:371-390.