DOI QR코드

DOI QR Code

알긴산 나트륨이 장용코팅된 란소프라졸 제제의 저장안정성 및 용출률에 미치는 영향에 관한 연구

The Effect of Sodium Alginate Coating on the Storage Stability and Dissolution Rate of Enteric Coated Lansoprazole

  • 김정훈 (전북대학교 유기신물질공학과) ;
  • 오정민 (전북대학교 유기신물질공학과) ;
  • 강길선 (전북대학교 유기신물질공학과) ;
  • 정제교 (삼천당제약 중앙연구소) ;
  • 이정식 (삼천당제약 중앙연구소) ;
  • 정상영 (한국화학연구원 생체의료고분자팀) ;
  • 이해방 (한국화학연구원 생체의료고분자팀)
  • Kim, Jung-Hoon (Department of Advanced Organic Materials Engineering, Chonbuk National University) ;
  • Oh, Jung-Min (Department of Advanced Organic Materials Engineering, Chonbuk National University) ;
  • Khang, Gil-Son (Department of Advanced Organic Materials Engineering, Chonbuk National University) ;
  • Jeong, Je-Kyo (Research Center, Samchundang Pharm. Co. Ltd.) ;
  • Lee, Jung-Sik (Research Center, Samchundang Pharm. Co. Ltd.) ;
  • Jeung, Sang-Young (Biomaterials Laboratory, Korea Research Institute of Chemical Technology) ;
  • Lee, Hai-Bang (Biomaterials Laboratory, Korea Research Institute of Chemical Technology)
  • 발행 : 2002.12.20

초록

Lansoprazole, pharmaceutics for acid-related diseases, is unstable in low pH environments and generally coated with enteric polymer to obtain gastroresistance in stomach. Because its storage stability is influenced by acidic substitutes of enteric polymer, alkaline chemicals wεre generally addεd to dosage form as a stabilizer. In this experience, we coated lansoprazole bead with sodium alginate and evaluated the effect of bead size and sodium alginate coating on the storage stability and dissolution profile of lansoprazole. Sodium alginate solution containing lansoprazole was sprayed as a droplet into 3% (w/v) $CaCl_2$ solution and the resultant bead was coated with starch, sodium alginate, and hydroxypropyl methylcellulose phthalate. The content of lansoprazole granule not coated with sodium alginate decreased to 57.96% of initial content when stored at a severe condition for 4 weeks, but that of lansoprazole granule coated with sodium alginate before enteric coating decreased little and as the thickness of sodium alginate film increased, the content of bead didn't decreased for 4 weeks. Sodium alginate film also improved the gastroresistance without much influencing the maximum dissolution rate.

키워드

참고문헌

  1. L.B. Baradell, D. Faulds and D. McTavish, Lansoprasole: A review of its pharmacodynamic and pharmacokinetic properties and its therapeutic efficacy in acid-related disorders, Drugs, 44, 225-250 (1992) https://doi.org/10.2165/00003495-199244020-00007
  2. A.E. Zimmermann and B.G. Katona, Lansoprazole: A comprehensive review, Pharmacotherapy, 17, 308-326 (1997)
  3. A. Kristl and F. Vrecer, Preformulation investigation of the novel proton pump inhibitor lansoprazole, Drug Dev. Ind. Pharm., 26, 781-783 (2000) https://doi.org/10.1081/DDC-100101299
  4. T. Tabata, T. Makino, T. Kashihara, S. Hirai, N. Kitamori and H. Toguchi, Stabilization of a new antiulcer drug (lansoprazole) in the solid dosage forms, Drug Dev. Ind. Pharm., 18, 1437-1447 (1992) https://doi.org/10.3109/03639049209040850
  5. A.B. Robert, Lansoprazole and omeprazole in the treatment of acid peptic disorders, Am. J. Health-Syst. Pharm., 53, 1401-1415 (1996)
  6. T. Tabata, T. Makino, J. Kikuta, S. Hirai and N. Kitamori, Manufacturing method of stable enteric granules of a new antiulcer drug (lansoprazole), Drug Dev. Ind. Pharm., 20, 1661-1672 (1994) https://doi.org/10.3109/03639049409050206
  7. M.A. Bayomi, S.A. Al-Suwayeh and A.R. El-Helw, Excipient-excipient interaction in the design of sustained-release theophylline tablets: In vitro and in vivo evaluation, Drug Dev. Ind. Pharm., 27, 499-506 (2001) https://doi.org/10.1081/DDC-100105174
  8. N.N. Salib and S.A. El-Gamal, Application of some polymers in the physiocochemical design of tablet formulation, Die Pharmazie, 31, 718-721 (1976)
  9. A.M. Sakr, H.M. Elsabbagh and A.H. Shalaby, Effect of the technique of incorporating sodium alginate on its binding and/or disintegrating effectiveness in sulfathiazole tablets, Pharm. Ind., 40, 1080-1086 (1978)
  10. K.A. Khan and C.T. Rhodes, Disintegration properties of calcium phosphate dibasic dihydrate tablets, J. Pharm. Sci., 64, 166-168 (1975) https://doi.org/10.1002/jps.2600640141
  11. P. Veski and M. Marvola, Sodium alginates as diluents in hard gelatin capsules containing ibuprofen as a model drug, Pharmazie, 48, 757-760 (1993)
  12. S. Klaudianos, Alginate sustained-action tablets, Dtsch Apoth Ztg, 118, 683-684 (1978)
  13. Bodmeier and J. Wang, Microencapsulation of drugs with aqueous colloidal polymer dispersions, J. Pharm. Sci., 82, 191-194 (1993) https://doi.org/10.1002/jps.2600820215
  14. F. Lim and R.D. Moss, Microencapsulation of living cells and tissues, J. Pharm. Sci., 70, 351-354 (1981) https://doi.org/10.1002/jps.2600700402
  15. M. Rajaonarivony, C. Vauthier, G. Couarraze, F. Puisieux and P. Couvreur, Development of a new drug carrier made from alginate, J. Pharm. Sci., 82, 912-917 (1993) https://doi.org/10.1002/jps.2600820909
  16. R. Bodmeier, H.G. Chen and O. Paeratakul, A novel approach to the oral delivery of micro- or nanoparticles, Pharm. Res., 6, 413-417 (1989) https://doi.org/10.1023/A:1015987516796
  17. W.R. Gombotz and S.F. Wee, Protein release from alginate matrices, Adv. Drug Delivery Rev., 31, 267-285 (1998) https://doi.org/10.1016/S0169-409X(97)00124-5
  18. T. Yotsuyanagi, T. Ohkubo, T. Ohhashi and K. Ikeda, Calcium-induced gelation of alginic acid and pH-sensitive reswelling of dried gels, Chem. Pharm. Bull., 35, 1555-1563 (1987) https://doi.org/10.1248/cpb.35.1555
  19. A.H. Kibbe, Handbook of Pharmaceutical Excipients, 3rd Ed., 465-467 (2000)
  20. R.J. Mumper, A.S. Hoffman, P. Puolakkainen, L.S. Bouchard and W.R. Gombotz, Calcium-alginate beads for the oral delivery of transforming growth factor-1: Stabilization of TGF-1 by the addition of polyacrylic acid within acid-treated beads, J. Control. Rel., 30, 241-251 (1994) https://doi.org/10.1016/0168-3659(94)90030-2
  21. C.K. Kim and E.J. Lee, The controlled release of blue dextran from alginate bead, Int. J. Pharm., 79, 11-19 (1992) https://doi.org/10.1016/0378-5173(92)90088-J
  22. S. Sugawara, R. Imai and M. Otagiri, The controlled release of prednisolone using alginate gel, Pharm. Res., 11, 272-277 (1994) https://doi.org/10.1023/A:1018963626248
  23. V. Pillay, R. Fassihi, In vitro release modulation from crosslinked pellets for site-specific drug delivery to the gastrointestinal tract I. Comparison of pH-responsive drug release and associated kinetics, J. Control. Rel., 59, 229-242 (1999) https://doi.org/10.1016/S0168-3659(98)00196-5