Crystallisation of estradiol containing TDDS determined by isothermal microcalorimetry, X-ray diffraction, and optical microscopy

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 56, Issue 1, 2003, Pages 43-52

  Latsch, Silvia ^a   Selzer, Torsten ^b   Fink, Lothar ^a   Kreuter, Jörg ^a  

^a GOETHE UNIVERSITY   (Germany)

^b Baxter Oncology GmbH   (Germany)

Author keywords

Crystallisation; Estradiol; Microcalorimetry; Transdermal drug delivery system; X ray powder diffraction

Indexed keywords

ESTRADIOL; MACROGOL 400;

ARTICLE; CONCENTRATION RESPONSE; CONTROLLED DRUG RELEASE; CRYSTALLIZATION; DRUG DELIVERY SYSTEM; MICROCALORIMETRY; MICROSCOPY; THERMODYNAMICS; X RAY DIFFRACTION;

EID: 0037677679     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0939-6411(03)00042-0     Document Type: Article

References (37)

1. Finnin B.C., Morgan T.M. Transdermal penetration enhancers: applications, limitations, and potential. J. Pharm. Sci. 88:1999;955-958.
2. Hadgraft J. Passive enhancement strategies in topical and transdermal drug delivery. Int. J. Pharm. 184:1999;1-6.
3. Davis A.F., Hadgraft J. Effect of supersaturation on membrane transport: 1. hydrocortisone acetate. Int. J. Pharm. 76:1991;1-8.
4. Pellett M.A., Davis A.F., Hadgraft J. Effect of supersaturation on membrane transport: 2. Piroxicam. Int. J. Pharm. 111:1994;1-6.
5. Megrab N.A., Williams A.C., Barry B.W. Oestradiol permeation through human skin and silastic membrane: effects of propylene glycol and supersaturation. J. Control. Rel. 36:1995;277-294.
6. Iervolino M., Raghavan S.L., Hadgraft J. Membrane penetration enhancement of ibuprofen using supersaturation. Int. J. Pharm. 198:2000;229-238.
7. Iervolino M., Cappello B., Raghavan S.L., Hadgraft J. Penetration enhancement of ibuprofen from supersaturated solutions through human skin. Int. J. Pharm. 212:2001;131-141.
8. Stefano F.J.E., Biali F.I., Scasso A.F. Crystallization in NETA-17β-E2 transdermal patches. Proc. Int. Symp. Control. Release Bioact. Mater. 24:1997;703-704.
9. Variankaval N.E., Jacob K.I., Dinh S.M. Crystallization of β-estradiol in an acrylic transdermal drug delivery system. J. Biomed. Mater. Res. 44:1999;397-406.
10. Lipp R., Müller-Fahrnow A. Use of X-ray crystallography for the characterization of single crystals grown in steroid containing transdermal drug delivery systems. Eur. J. Pharm. Biopharm. 47:1999;133-138.
11. Kotiyan P.N., Vavia P.R. Eudragits: role as crystallization inhibitors in drug-in-adhesive transdermal systems of estradiol. Eur. J. Pharm. Biopharm. 52:2001;173-180.
12. Kim J.-H., Choi H.-K. Effect of additives on the crystallization and the permeation of ketoprofen from adhesive matrix. Int. J. Pharm. 236:2002;81-85.
13. Raghavan S.L., Trividic A., Davis A.F., Hadgraft J. Effect of cellulose polymers on supersaturation and in vitro membrane transport of hydrocortisone acetate. Int. J. Pharm. 193:2000;231-237.
14. Ma X., Taw J., Chiang C.-M. Control of drug crystallization in transdermal matrix system. Int. J. Pharm. 142:1996;115-119.
15. Raghavan S.L., Trividic A., Davis A.F., Hadgraft J. Crystallization of hydrocortisone acetate: influence of polymers. Int. J. Pharm. 212:2001;213-221.
16. Buckton G., Darcy P. Assessment of disorder in crystalline powders - a review of analytical techniques and their application. Int. J. Pharm. 179:1999;141-158.
17. Briggner L.E., Buckton G., Bystrom K., Darcy P. The use of isothermal microcalorimetry in the study of changes in crystallinity induced during the processing of powders. Int. J. Pharm. 105:1994;125-135.
18. Sebhatu T., Angberg M., Ahlneck C. Assessment of the degree of disorder in crystalline solids by isothermal microcalorimetry. Int. J. Pharm. 104:1994;135-144.
19. Aso Y., Yoshioka S., Otsuka T., Kojima S. The physical stability of amorphous nifedipine determined by isothermal microcalorimetry. Chem. Pharm. Bull. 43:1995;300-303.
20. Angberg M. Lactose and thermal analysis with special emphasis on microcalorimetry. Thermochim. Acta. 248:1995;161-176.
21. Buckton G., Darcy P., Greenleaf D., Holbrook P. The use of isothermal microcalorimetry in the study of changes in crystallinity of spray-dried salbutamol sulphate. Int. J. Pharm. 116:1995;113-118.
22. Buckton G., Darcy P. The influence of additives on the recrystallisation of amorphous spray dried lactose. Int. J. Pharm. 121:1995;81-87.
23. Ahmed H., Buckton G., Rawlins D.A. The use of isothermal microcalorimetry in the study of small degrees of amorphous content of a hydrophobic powder. Int. J. Pharm. 130:1996;195-201.
24. Ahmed H., Buckton G., Rawlins D.A. Crystallisation of partially amorphous griseofulvin in water vapour: determination of kinetic parameters using isothermal heat conduction microcalorimetry. Int. J. Pharm. 167:1998;139-145.
25. Chidavaenzi O.C., Buckton G., Koosha F., Pathak R. The use of thermal techniques to assess the impact of feed concentration on the amorphous content and polymorphic forms present in spray dried lactose. Int. J. Pharm. 159:1997;67-74.
26. Lehto V.P., Laine E. A kinetic study on crystallization of an amorphous lubricant. Pharm. Res. 14:1997;899-904.
27. Darcy P., Buckton G. Quantitative assessments of powder crystallinity: estimates of heat and mass transfer to interpret isothermal microcalorimetry data. Thermochim. Acta. 316:1998;29-36.
28. Darcy P.A., Wiencek J.M. Estimating lysozyme crystallization growth rates and solubility from isothermal microcalorimetry. Acta Cryst. D54:1998;1387-1394.
29. Gustafsson C., Lennholm H., Iversen T., Nyström C. Comparison of solid-state NMR and isothermal microcalorimetry in the assessment of the amorphous component of lactose. Int. J. Pharm. 174:1998;243-252.
30. Chidavaenzi O.C., Buckton G., Koosha F. The effect of co-spray drying with polyethylene glycol 4000 on the crystallinity and physical form of lactose. Int. J. Pharm. 216:2001;43-49.
31. Kawakami K., Numa T., Ida Y. Assessment of amorphous content by microcalorimetry. J. Pharm. Sci. 91:2002;417-422.
32. Lehto V.-P., Laine E. A kinetic study of polymorphic transition of anhydrous caffeine with microcalorimeter. Thermochim. Acta. 317:1998;47-58.
33. Variankaval N.E., Jacob K.I., Dinh S.M. Characterization of crystal forms of β-estradiol - thermal analysis, Raman microscopy, X-ray analysis and solid-state NMR. J. Cryst. Growth. 217:2000;320-331.
34. Kuhnert-Brandstätter M., Grimm H. Zur Unterscheidung von lösungsmittelhaltigen pseudopolymorphen Kristallformen und polymorphen Modifikationen bei Steroidhormonen. II. Mikrochim. Acta. 1968;127-139.
35. Kuhnert-Brandstätter M., Winkler H. Thermoanalytische und IR-spektroskopische Untersuchungen an verschiedenen Kristallformen von Arzneistoffen aus der Östradiol-und Androstangruppe. Sci. Pharm. 44:1976;177-190.
36. Leuner C., Dressman J. Improving drug solubility for oral delivery using solid dispersions. Eur. J. Pharm. Biopharm. 50:2000;47-60.
37. Fukuoka E., Makita M., Yamamura S. Glassy state of pharmaceuticals. III. Thermal properties and stability of glassy pharmaceuticals and their binary glass systems. Chem. Pharm. Bull. 37:1989;1047-1050.