Carbamazepine parenteral nanoemulsions prepared by spontaneous emulsification process

International Journal of Pharmaceutics

Volumn 342, Issue 1-2, 2007, Pages 231-239

  Kelmann, Regina G ^a   Kuminek, Gislaine ^a   Teixeira, Helder F ^b   Koester, Letícia S ^a  

^a FEDERAL UNIVERSITY OF SANTA CATARINA   (Brazil)

^b FEDERAL UNIVERSITY OF RIO GRANDE DO SUL   (Brazil)

Author keywords

Carbamazepine; Factorial design; Intravenous; Nanoemulsions; Spontaneous emulsification

Indexed keywords

CARBAMAZEPINE;

ARTICLE; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; DRUG STRUCTURE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; PRIORITY JOURNAL; TRANSMISSION ELECTRON MICROSCOPY;

ANTICONVULSANTS; CARBAMAZEPINE; CASTOR OIL; CHEMISTRY, PHARMACEUTICAL; CHEMISTRY, PHYSICAL; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; DRUG COMPOUNDING; EMULSIONS; EXCIPIENTS; INJECTIONS, INTRAVENOUS; MICRODIALYSIS; MICROSCOPY, ELECTRON, TRANSMISSION; OILS; PARTICLE SIZE; SOLUBILITY; VISCOSITY;

EID: 34547971125     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2007.05.004     Document Type: Article

References (50)

1. Abrol S., Trehan A., and Katare O.P. Comparative study of different silymarin formulations: formulation, characterization and in vitro/in vivo evaluation. Curr. Drug Deliv. 2 (2005) 45-51
2. ® technology. Eur. J. Pharm. Biopharm. 55 (2003) 305-312
3. Becirevic-Lacan M., Jug M., Bacic-Vrca V., and Cetina-Cizmek B. Development of o/w emulsion formulation for carbamazepine by using modified cyclodextrins. Acta Pharm. 52 (2002) 149-159
4. Benita S., and Levy M.Y. Submicron emulsions as colloidal drug carriers for intravenous administration: comprehensive physicochemical characterization. J. Pharm. Sci. 82 (1993) 1069-1079
5. Bouchemal K., Briançon S., Perrier E., and Fessi H. Nano-emulsion formulation using spontaneous emulsification: solvent, oil and surfactant optimization. Int. J. Pharm. 280 (2004) 241-251
6. Brewster M.E., Anderson W.R., Meinsma D., Moreno D., Webb A.I., Pablo L., Estes K.S., Derendorf H., Bodor N., Sawchuk R., Cheung B., and Pop E. Intravenous and oral pharmacokinetic evaluation of a 2-hydroxypropyl-beta-cyclodextrin-based formulation of carbamazepine in the dog: comparison with commercially available tablets and suspensions. J. Pharm. Sci. 86 (1997) 335-339
7. Chaubal, M.V., Roseman, T.J., 2006. Drug delivery trends for parenteral therapeutics. Pharm. Technol. Oct 2. Available online at the site: http://www.pharmtech.com/pharmtech/article/articleDetail.jsp?id=378748 &sk=&date=&pageID=2.
8. Constantinides P.P., Lambert K.J., Tustian A.K., Schneider B., Lalji S., Ma W., Wentzel B., Kessler D., Worah D., and Quay S.C. Formulation development and antitumor activity of a filter-sterilizable emulsion of paclitaxel. Pharm. Res. 17 (2000) 175-182
9. Constantinides P.P., Tustian A., and Kessler D.R. Tocol emulsions for drug solubilization and parenteral delivery. Adv. Drug Deliv. Rev. 56 (2004) 1243-1255
10. Costa P., and Lobo J.M.S. Modeling and comparison of dissolution profiles. Eur. J. Pharm. Sci. 13 (2001) 123-133
11. D'Souza S.S., and DeLuca P.P. Methods to assess in vitro drug release from injectable polymeric particulate systems. Pharm. Res. 23 (2006) 460-474
12. Food and Drug Administration (FDA), 2006a. Approved Drug Products with Therapeutic Equivalence Evaluations, 26th ed. pp. 92-93. Available at: (November 12, 2006).
13. Food and Drug Administration (FDA), 2006b. Inactive Ingredient Database. Available at: (November 12, 2006).
14. Floyd A.G. Top ten considerations in the development of parenteral emulsions. Pharm. Sci. Technol. 2 (1999) 134-143
15. In: Genaro A.R. (Ed). Remington: The Pharmaceutical Sciences and Practice of Pharmacy (2000), Lippincott, Williams & Wilkins, Philadelphia
16. Goodman L.S., Gilman A.G., Hardman J.G., and Limbird L.E. Goodman & Gilman's the pharmacological basis of therapeutics (2001), McGraw-Hill Book Co., New York
17. Grassi M., Coceani N., and Magarotto L. Mathematical modeling of drug release from microemulsions: theory in comparison with experiments. J. Colloid Interface Sci. 228 (2000) 141-150
18. Han J., Davis S.S., and Washington C. Physical properties and stability of two emulsion formulations of propofol. Int. J. Pharm. 215 (2001) 207-220
19. Henriksen I., Sande S.A., Smistad G., Agren T., and Karlsen J. In vitro evaluation of drug release kinetics from liposomes by fractional dialysis. Int. J. Pharm. 119 (1995) 231-238
20. ICH. Validation of analytical procedures: text and methodology. International Conference on Harmonization. IFPMA, Geneva (2005)
21. Jumaa M., and Müller B.W. The effect of oil components and homogenization conditions on the physicochemical properties and stability of parenteral fat emulsions. Int. J. Pharm. 163 (1998) 81-89
22. Jumaa M., and Müller B.W. In vitro investigation of the effect of various isotonic substances in parenteral emulsions on human erythrocytes. Eur. J. Pharm. Sci. 9 (1999) 207-212
23. Jumaa M., and Müller B.W. Development of a novel parenteral formulation for tetrazepam using a lipid emulsion. Drug Dev. Ind. Pharm. 27 (2001) 1115-1121
24. Kelmann, R.G., Kuminek, G., Teixeira, H.F., Koester, L.S., 2007a. Preliminary study on the development of nanoemulsions for carbamazepine intravenous delivery: investigation of drug polymorphic transition. Drug Dev. Ind. Pharm., in press
25. Kelmann, R.G., Kuminek, G., Teixeira, H.F., Koester, L.S, 2007b. Determination of carbamazepine in parenteral nanoemulsions: Development and validation of an HPLC method Chromatographia. Chromatographia,.in press
26. Kobayashi Y., Itai S., and Yamamoto K. Pysicochemical propreties and bioavailability of carbamazepine polymorphs and dehydrate. Int. J. Pharm. 193 (2000) 137-146
27. Levy R.H., Lockard J.S., Green J.R., Friel P., and Martis L. Pharmacokinetics of carbamazepine in monkeys following intravenous and oral administration. J. Pharm. Sci. 64 (1975) 302-307
28. Löscher W., and Hoenack D. Intravenous carbamazepine: comparison of different parenteral formulations in a mouse model of convulsive status epilepticus. Epilepsia 38 (1997) 106-113
29. Löscher W., Honack D., Richter A., Schulz H.U., Schurer M., Dusing R., and Brewster M.E. New injectable aqueous carbamazepine solution through complexing with 2-hydroxypropyl-beta-cyclodextrin: tolerability and pharmacokinetics after intravenous injection in comparison to a glycofurol-based formulation. Epilepsia 36 (1995) 255-261
30. Lund W. The Pharmaceutical Codex: Principles and Practices of Pharmaceutics. 12th ed. (1994), The Pharmaceutical Press, London
31. Michalowski C.B., Guterres S.S., and Dalla Costa T. Microdialysis for evaluating the entrapment and release of a lipophilic drug from nanoparticles. J. Pharm. Biomed. Anal. 35 (2004) 1093-1100
32. Montgomery D.C. Design and Analysis of Experiments. 3rd ed. (1991), Wiley, New York pp. 228-301
33. ®-novel technology for the formulation of i.v. emulsions with poorly soluble drugs. Int. J. Pharm. 269 (2004) 293-302
34. Nair R., Gonen S., and Hoag S.W. Influence of polyethylene glycol and povidone on the polymorphic transformation and solubility of carbamazepine. Int. J. Pharm. 240 (2002) 11-22
35. Nielloud F., Marti-Mestres G., Laget J.P., Fernendez C., and Maillols H. Emulsion formulation: study of the influence of parameters with experimental designs. Drug Dev. Ind. Pharm. 22 (1996) 159-166
36. Otsuka M., Ofusa T., and Matsuda Y. Effect of environmental humidity on the transformation pathway of carbamazepine polymorphic modifications during grinding. Colloids Surf. B 13 (1999) 263-273
37. Schultz K., Mollgaard B., Frokjaer S., and Larsen C. Rotating dialysis cell as in vitro release method for oily parenteral depot solutions. Int. J. Pharm. 157 (1997) 163-169
38. Sethia S., and Squillante E. Physicochemical characterization of solid dispersions of carbamazepine formulated by supercritical carbon dioxide and conventional solvent evaporation method. J. Pharm. Sci. 91 (2002) 1948-1957
39. Sucker H. Methoden zum Planen und Auswerten von Versuchen. I. Factorial design, eine Einführung. APV-Informationsdienst 17 (1971) 52-68
40. Sweetman, S.C. (Ed.), 2006. Martindale: The Complete Drug Reference. Pharmaceutical Press, London, UK. (electronic version).
41. Sznitowska M., Janicki S., Dabrowska E., and Zurowska-Pryczkowska K. Submicron emulsions as drug carriers: studies on destabilization potential of various drugs. Eur. J. Pharm. Sci. 12 (2001) 175-179
42. Tauboll E., Lindström S., Klem W., and Gjerstad L. A new injectable carbamazepine solution: antiepileptic effects and pharmaceutical properties. Epilepsy Res. 7 (1990) 59-64
43. Thompson D.O., and Chaubal M.V. Cyclodextrins (CDS)-excipients by definition, drug delivery systems by function. Part I. Injectable applications. Drug Deliv. Technol. 2 (2002) 34-38
44. Tian F., Zeitler J.A., Strachan C.J., Saville D.J., Gordon K.C., and Rades T. Characterizing the conversion kinetics of carbamazepine polymorphs to the dihydrate in aqueous suspension using Raman spectroscopy. J. Pharm. Biomed. Anal. 40 (2006) 271-280
45. US Pharmacopeia/The National Formulary (USP 28/NF23), 2005. United States Pharmacopeial Convention, Rockville, MD, p. 343
46. Vitale S.A., and Katz J.L. Liquid droplet dispersions formed by homogeneous liquid-liquid nucleation: the Ouzo effect. Langmuir 19 (2003) 4105-4110
47. Wang J., Sung K.C., Hu O.Y., Yeh C., and Fang J. Submicron lipid emulsion as a drug delivery system for nalbuphine and its prodrugs. J. Contr. Rel. 115 (2006) 140-149
48. Washington C. Stability of lipid emulsions for drug delivery. Adv. Drug Deliv. Rev. 20 (1996) 131-145
49. Yamagushi T., Nishizaki K., Itai S., Hayashi H., and Ohshima H. Physicochemical characterization of parenteral lipid emulsion: influence of cosurfactants on flocculation and coalescence. Pharm. Res. 12 (1995) 1273-1278
50. Yu W., Tabosa Do Egito E.S., Barrat G., Fessi J.P., Devissaguet J.P., and Puisieux F. A novel approach to the preparation of injectable emulsions by spontaneous emulsification process. Int. J. Pharm. 89 (1993) 139-146