Abstract
The microencapsulation of sodium naproxen with Eudragit RS was studied by coacervation/phase separation process using Span 80 in mineral oil/acetone system. Various factors which affect the microencapsulation, e.g., stiming speed, and surfactant concentration, Eudragit RS concentration and loading drug amounts were examined. For the evaluation of the prepared microcapsules, release rate, particle size distribution and surface appearance as well asin vivo test were carried out. The addition of n-hexane and freezing of microcapsules accelerated the hardening of microcapsules. The optimum concentration of Span 80 to prepare the smallest microcapsules was the same value with the CMC of Span 80 in solvent system. When 1.5% (w/w) Span 80 was used, the smallest microcapsules were formed (30.02±5.05 μm in diameter) belonging to the powder category showing smooth, round and uniform surface. The release of sodium naproxen was retarded by microencapsulation with Eudragit RS. The Eudragit RS microcapsules showed significantly increased AUC and MRT and decreased Cl/F in rabbits.
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Literature Cited
Abakke, J., Gadeholt, G. and Hoeylandskjaer, A., Pharmacokinetics of naproxen after oral administration of two tablet formations in healthy volunteers.Int. J. Clin. Pharmacol. Ther. Toxicol., 21, 281–2883 (1983).
Bogataj, M., Mrhar, A., Kristl A. and Kozjek, F., Preparation and evaluation of Eudragit E microspheres containing bacampicillin.Drug. Devel. Ind. Pharm., 15, 2295–2313 (1989).
Carli, F., Cappone, G., Colombo, I., Margarotto, L. and Motta, A., Surface and transport properties of acrylic polymers influencing drug release from porous matrices.J. Pharm. Sci., 73, 317–320 (1984).
Chafi, N., Montheard, J. P. and Vergnaud, J. M., Dosage form with drug attached to polymer(polyanhydride) dispersed in Eudragit matrix: Preparation and release of drug in gastric liquid.Int. J. Pharm., 45, 229–236 (1988).
Dakkuri, A., Schroeder, H. G. and DeLuca, D. P., Sustained release from inert wax matrices II: Effect of surfactant on tripelennamine hydrochloride release.J. Pharm. Sci., 67, 354–357 (1978).
Dahl, T., Ling, J., Yee, J. and Bormeth, A., Effect of various granulating systems on the bioavailability of naproxen sodium from the polymeric matrix tablets.J. Pharm. Sci., 79, 3889–392 (1990).
Goto, S., Kawata, M., Nakamura, M., Maekawa, K. and Aoyama, T., Eudragit E, L and S (acrylic resins) microcapsules as pH sensitive release preparations of ketoprofen.J. Microencapsulation, 34, 305–316 (1986a).
Goto, S., Kawata, M., Nakamura, M., Maekawa, K. and Aoyama, T., Eudragit RS and RL (acrylic resins) microcapsules as pH sensitive and sustained release preparations of ketoprofen.J. Microencapsulation, 34, 293–304 (1986b).
Ismail, F. A., Lhalafallah, N. and Khalil, S. A., Disease and drug-induced changes in naproxen binding plasma.Drug Devel. Ind. Pharm., 15, 147–164 (1985).
Lamson, M. L.,RSTRIP-polyexponential curve stripping/least squares parameter estimation, user handbook, Micromath. Inc., Salt Lake City, 1987.
Maharai, I., Naim, J. G. and Campbell, J. B., Simple rapid method for the preparation of enteric-coated microspheres.J. Pharm. Sci., 73, 9–42 (1984).
Merkle, H. P. and Speicer, P. J., Preparation andin vivo evaluation of cellulose acetate phthalate coacervation microcapsules.J. Pharm. Sci., 62, 1444–1448 (1973).
Nixon, J. R. and Agyilirah, G. A., Effect of microcapsule core-wall ratio aggregate size on the properties of tableted microcapsules.J. Pharm. Sci., 73, 52–54 (1984).
Okor, R. S. and Obi, C. E., Drug release through aqueous-based film coatings of acrylate-methacrylate, a water-insoluble copolymer.Int. J. Pharm., 58, 89–91 (1990).
Riegelman, S. and Collier, P., The application of statistical moment theory to the evaluation ofin vivo dissolution time and absorption time.J. Pharmacokinet. Biopharm. 8, 509 (1980).
Runkel, R., Chaplin, M., Boost, G., Segre, E. and Forchielli, E., Absorption, distribution, metabolism and excretion of naproxen in various laboratory animals and human subjects.J. Pharm. Sci., 61, 703–708 (1972).
Takenaka, H., Kawashima, Y. and Lin, S. Y., Preparation of enteric-coated microcapsules for tableting by spray-drying technique andin vitro andin vivo simulation on the drug release from the tablets in GI tract.J. Pharm. Sci., 69, 1388–1392 (1980).
Vandegaer, J. E.,Microencapsulation, Processes and Aplications. Plenum Publishing Co., New York (1973).
Yoshioma, T., Hashida, M., Muranish, S. and Sezaki, H., Specific delivery of mitomycin to the liver, spleen and lung: Nano and microspherical carriers of gelatin.Int. J. Pharm., 81, 131 (1981).
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Shin, SC., Lee, KR. Studies on the development for sustained release preparation (II): Preparation and evaluation of eudragit microcapsules of sodium naproxen. Arch. Pharm. Res. 16, 50–56 (1993). https://doi.org/10.1007/BF02974128
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DOI: https://doi.org/10.1007/BF02974128