Drug controlled release from dosage forms coated with aqueous cellulose and acrylic polymer dispersions
Authors:
D. Vetchý 1; H. Leštinová 2
Authors‘ workplace:
Veterinární a farmaceutická univerzita Brno, Farmaceutická fakulta, Ústav technologie léků
1; Lékárna Na Předměstí, Třeboň
2
Published in:
Čes. slov. Farm., 2010; 59, 163-171
Overview
Current scientific papers concerning aqueous cellulose and acrylic polymer dispersions for controlled drug delivery are focused on stability studies and the search for suitable coated formulations for drug release at a specific time and site of the gastrointestinal tract. It can be achieved especially by preparing polymer blends or using other additives. The permeability of the ethylcellulose membranes can be increased by the addition of water-soluble polymers (drug release modifiers). If there is no independence of solubility of the drug on pH, a poly(vinyl alcohol)–poly(ethylene glycol) graft copolymer is frequently used, because it simultaneously hinders further polymer particle coalescence during long term storage. With respect to a low glass transition temperature and consequently high tackiness of polymer films, Eudragit NE should be blended with high glass transition temperature polymers which are miscible with the functional coating, for example Eudragit L or Eudragit RS. Eudragit L 30 D-55 coatings take over 2 hours to dissolve in vivo in the human small intestine. This fact can cause delayed drug release and bioavailability reduction of those drugs which are to be absorbed in proximal small intestine. Accelerated coating disintegration can be achieved by preparation of double-coating enteric systems or leaky enteric coatings.
Key words:
controlled release – ethylcellulose – Eudragit RS – Eudragit NE – Eudragit L-55
Sources
1. Gryczová, E., Rabišková, M., Tomášek, V., Prokopová, A., Cepáková, L.: Vliv tepelného ošetření ethylcelulosového filmu na rychlost uvolňování sodné soli diklofenaku z pelet. Čes. slov. Farm., 2007; 56, 235–242.
2. Krejčová, K., Rabišková, M., Vetchý, D., Tomášek, V., Prokopová, A.: Vliv typu polymerové disperze na uvolňování diklofenaku sodné soli z obalených pelet. Čes. slov. Farm., 2007; 56, 190–199.
3. Meincken, M., Sanderson, R. D.: Determination of the inuence of the polymer structure and particle size on the lm formation process of polymers by atomic force microscopy. Polymer., 2002; 43, 4947–4955.
4. Sastry, S. V., Wilber, W., Reddy, I. K., Khan, M. A.: Aqueous-based polymeric dispersion: preparation and characterization of cellulose acetate pseudolatex. Int. J. Pharm., 1998; 165, 175–189.
5. Bauer, K., Lehman, K., Osterwald, H. P., Rothgang, G.: Coated Pharmaceutical Dosage Forms: Fundamentals, Manufacturing Techniques, Biopharmaceutical Aspects, Test Methods and Raw Materials. 1st ed. Boca Raton: CRC Press 1998; 280 p.
6. Wheatley, T. A., Steuernagel, C. R., Lehmann, K. O. R.: Aqueous Polymeric Coatings for Pharmaceutical Dosage Forms. In: McGinity, J. W. ed. Aqueous polymeric coatings for pharmaceutical dosage forms, 2nd ed. New York: Marcel Dekker, Inc. 1997.
7. Pongjanyakul, T., Puttipipatkhachorn, S.: Alginate-magnesium aluminum silicate lms: Effect of plasticizers on lm properties, drug permeation and drug release from coated tablets. Int. J. Pharm., 2007; 333, 34–44.
8. Mendoza-Romero, L., Pinon-Segundo, E., Nava-Arzaluz, M. G., Ganem-Quintanar, A., Cordero-Sánchez, S., Quintanar-Guerrero, D.: Comparison of pharmaceutical lms prepared from aqueous polymeric dispersions using the cast method and the spraying technique. Colloids and Surfaces A: Physicochem. Eng. Aspects., 2009; 337, 109–116.
9. Okarter, T. U., Sngla, K.: The effects of plasticizers on the release of metoprolol tartrate from granules coated with a polymethacrylate film. Drug Dev. Ind. Pharm., 2000; 26, 323–329.
10. Blackley, D. C.: Polymer latices: Science and technology. 2nd ed. London: Chapman & Hall 1997; 583p.
11. Jones, D.: Pharmaceutical applications of polymers for drug delivery. 1st ed. Shawbury: iSmithers Rapra Publishing 2004; 124p.
12. Ducháček, V.: Polymery – výroba, vlastnosti, zpracování, použití. Dostupné na: http://vydavatelstvi. vscht.cz/knihy/uid_isbn-80-7080-617-6/pages-img/obsah. html (10. 10. 2009).
13. Augsburger, L. L., Hoag, S. W.: Pharmaceutical dosage forms: Tablets: Volume 1: Unit operations and mechancial properties, 3rd ed. New York: Informa Healthcare 2008.
14. Wang, J., Ghebre-Sellassie, I.: Aqueous polymeric dispersions as film formers. In: Lieberman, H. A., Rieger, M. M., Banker,G. S. eds. Pharmaceutical Dosage Forms: Disperse Systems, 2nd ed. New York: Marcel Dekker, Inc. 1998.
15. Siepmann, F., Siepmann, J., Walther, M., MacRae, R. J., Bodmeier, R.: Polymer blends for controlled release coatings. J. Control. Release, 2008; 125, 1–15.
16. Siepmann, F., Hoffmann, A., Leclercq, B., Carlin, B., Siepmann, J.: How to adjust desired drug release patterns from ethylcellulose-coated dosage forms. J. Control. Release, 2007; 119, 182–189.
17. Siepmann, F., Wahle, C., Leclercq, B., Carlin, B., Siepmann, J.: pH-sensitive lm coatings: Towards a better understanding and facilitated optimization. Eur. J. Pharm. Biopharm., 2008; 68, 2–10.
18. Kranz, H., Gutsche, S.: Evaluation of the drug release patterns and long term stability of aqueous and organic coated pellets by using blends of enteric and gastrointestinal insoluble polymers. Int. J. Pharm., 2009; 380, 112–119.
19. Siepmann, F., Muschert, S., Leclercq, B., Carlin, B., Siepmann, J.: How to improve the storage stability of aqueous polymeric film coatings. J. Control. Release, 2008; 126, 26–33.
20. Frohoff-Hülsmann, M. A., Schmitz, A., Lippold, B. C.: Aqueous ethyl cellulose dispersions containing plasticizers of different water solubility and hydroxypropyl methylcellulose as coating material for diffusion pellets I. Drug release rates from coated pellets. Int. J. Pharm. 1999; 177, 69–82.
21. Frohoff-Hülsmann, M. A., Lippold, B. C., McGinity, J. W.: Aqueous ethyl cellulose dispersion containing plasticizers of different water solubility and hydroxypropyl methyl-cellulose as coating material for diffusion pellets II: properties of sprayed films. Eur. J. Pharm. Biopharm., 1999; 48, 67–75.
22. Yang, Q. W., Flament, M. P., Siepmann, F., Busignies, V., Leclercq, B. Herry, C., Tchoreloff, P., Siepmann, J.: Curing of aqueous polymeric film coatings: importance of the coating level and type of plasticizer. Eur. J. Pharm. Biopharm., 2010; 74, 362–370.
23. Muschert, S., Siepmann, F., Cuppok, Y., Leclercq, B., Carlin, B., Siepmann, J.: Improved long term stability of aqueous ethylcellulose lm coatings: Importance of the type of drug and starter core. Int. J. Pharm., 2008; 368, 138–145.
24. Technical information: Kollicoat IR. http://www.makeni. com.br/Portals/Makeni/prod/boletim/Kollicoat%20IR.pdf (12. 5. 2010).
25. Muschert, S., Siepmann, F., Leclercq, B., Carlin, B., Siepmann, J.: Drug release mechanisms from ethylcellulose: PVA-PEG graft copolymer-coated pellets. Eur. J. Pharm., Biopharm. 2009; 72, 130–137.
26. Muschert, S., Siepmann, F., Leclercq, B., Carlin, B., Siepmann, J.: Prediction of drug release from ethylcellulose coated pellets. J. Control. Release, 2009; 135, 71–79.
27. Lecomte, F., Siepmann, J., Walther, M., MacRae, R. J., Bodmeier, R.: pH-Sensitive Polymer Blends Used as Coating Materials to Control Drug Release from Spherical Beads: Elucidation of the Underlying Mass Transport Mechanisms. Pharm. Res., 2005; 22, 1129–1141.
28. Lecomte, F., Siepmann, J., Walther, M., MacRae, R. J., Bodmeier, R.: Polymer blends used for the aqueous coating of solid dosage forms: importance of the type of plasticizer. J. Control. Release, 2004; 99, 1–13.
29. Komárek, P., Rabišková, M.: Technologie léků, 3. vyd. Praha: Galén 2006, 399 s.
30. EUDRAGIT® – Targeted Drug Release and Tailored Service, http://eudragit.evonik.com/product/eudragit/en/ Pages/default.aspx (1. 12. 2009).
31. Nimkulrat, S., Suchiva, K., Phinyocheep, P., Puttipipatkhachorn, S.: Inuence of selected surfactants on the tackiness of acrylic polymer lms. Int. J. Pharm., 2004; 287, 27–37.
32. Ishikawa, Y., Katoh, Y., Oshima, H.: Colloidal stability of aqueous polymeric dispersions: Effect of pH and salt concentration. Colloids Surface B., 2005; 42, 53–58.
33. Bajdik, J., Pintye-Hódi, K., Regdon, G. Jr., Fazekas, P., Szabó-Révész, P., Erös, I.: The effect of storage on the behaviour of Eudragit NE free film. J. Therm. Anal. Calorim., 2003; 73, 607–613.
34. Kucera, S., Shah, N. H., Malick, A. W., Infeld, M. H., McGinity J. W.: Inuence of an acrylic polymer blend on the physical stability of film-coated theophylline pellets. AAPS PharmSciTech., 2009; 10, 864–871.
35. Kibria, G., Roni, M. A., Absar M. S., Jalil, R.: Effect of plasticizer on release kinetics of diclofenac sodium pellets coated with Eudragit RS 30 D. AAPS PharmSciTech., 2008; 9, 1240–1246.
36. Kim, T., Ji C.-W., Shim, S.-Y., Lee, B.-J.: Modified release of coated sugar spheres using drug-containing polymeric dispersions. Arch. Pharm. Res., 2007; 30, 124–130.
37. Dashewsky, A., Wagner, K., Kolter, K., Bodmeier, R.: Physicochemical and release properties of pellets coated with Kollicoat® SR 30 D, a new aqueous polyvinyl acetate dispersion for extended release. Int. J. Pharm., 2005; 290, 15–23.
38. Siepmann, F., Le Brun, V., Siepmann, J.: Drugs acting as plasticizers in polymeric systems: A quantitative treatment. J. Control. Release, 2006; 115, 298–306.
39. Bhattacharjya, S., Wurster, D. E.: Investigation of the drug release and surface morphological properties of film-coated pellets, and physical, thermal and mechanical properties of free films as a function of various curing conditions. AAPS PharmSciTech., 2008; 9, 449–457.
40. Wurster, D. E., Bhattacharjya, S., Flanagan, D. R.: Effect of curing on water diffusivities in acrylate free films as measured via a sorption technique. AAPS PharmSciTech., 2007; 8, E1–E6.
41. Zheng, W., Sauer, D., McGinity, J. W.: Inuence of hydroxyethylcellulose on the drug release properties of theophylline pellets coated with Eudragit® RS 30 D. Eur. J. Pharm. Biopharm., 2005; 59, 147–154.
42. Bendas, E. R., Ayres, J. W.: Leaky enteric coating on ranitidine hydrochloride beads: Dissolution and prediction of plasma data. Eur. J. Pharm. Biopharm., 2008; 69, 977–985.
43. El-Malah, Y., Nazzal, S.: Novel use of Eudragit® NE 30D/Eudragit® L 30D-55 blends as functional coating materials in time-delayed drug release applications. Int. J. Pharm., 2008; 357, 219–227.
44. Liu, F., Lizio, R., Meier, C., Petereit, H.-U., Blakey, P., Basit, A. W.: A novel concept in enteric coating: A double-coating system providing rapid drug release in the proximal small intestine. J. Control. Release, 2009; 133, 119–124.
45. Liu, F., Lizio, R., Schneider, U. J., Petereit, H.-U., Blakey, P., Basit, A. W.: SEM/EDX and confocal microscopy analysis of novel and conventional enteric-coated systems. Int. J. Pharm., 2009; 369, 72–78.
46. Catteau, D., Barthelemy, C., Deveaux, M., Robert, H., Trublin, F., Marchandise, X., Van Drunen, H.: Contribution of scintigraphy to verify the reliability of different preparation processes for enteric coated capsules. Eur. J. Drug. Metab. Pharmacokinet., 1994; 19, 91–98.
47. McConnell, E. L., Fadda, H. M., Basit, A. W.: Gut instincts: explorations in intestinal physiology and drug delivery. Int. J. Pharm., 2008; 364, 213–226.
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Pharmacy Clinical pharmacologyArticle was published in
Czech and Slovak Pharmacy
2010 Issue 4
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