Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Stability Improvement of Amlodipine Maleate Tablets using Aqueous Polymer Coating Technique

친수성 폴리머 제피를 이용한 말레인산암로디핀 정제의 안정성 개선

  • Published : 2004.10.20
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Abstract

New formulations of amlodipine maleate tablet have been investigated to enhance the stability of the drug against light and humidity. Three kinds of amlodipine maleate tablets were prepared. One is prepared by previously known formulation (formulation C), the others were by new formulations using hydrophilic polymer $(Opadry^{\circledR})$ coated granules (formulations A and B). Amlodipine maleate powder was coated with $Opadry^{\circledR}$ to produce the coated granules and it was mixed with other excipients to produce the tabletting mass of new formulations A and B. Dissolution rate of newly formulated tablets was over 80% within 10 minutes in 0.01 M HCl medium, and its dissolution pattern was similar to that of $Norvasc^{\circledR}$ tablet. After 6 months storage under accelerated conditions, residual drug contents of tested formulations (A and B) were not significantly different from formulation C, ranging from 96.2 to 100.4%. Meanwhile, dissolution amount of formulation C was significantly reduced compared to that of formulation A (p<0.05), showing formulation A was more stable than unprotected formulation C at the accelerated conditions. Results of appearance, hardness and disintegration remained unchanged during stability study. In conclusion, it showed that the new formulations had enhanced the stability characteristics and hydrophilic coating technique was an alternative and promising method to improve the stability of amlodipine maleate tablet.

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References

  1. K.K. Pandya, M. Satia, T.P. Gandhi, I.A. Modi, R.I. Modi and B.K. Chakravarthy, Detection and detennination of total amlodipine by high performance thin layer chromatography, a useful technique for pharmacokinetic studies, J. Chromatogr. B., 667, 315-320 (1995) https://doi.org/10.1016/0378-4347(95)00016-C
  2. H. Kudat, N. Eren and F. Erzengin, Efficacy and tolerability of amlodipine in patients with stable angina pectoris, an open-label, multicenter trial, Curr. Ther. Res., 59, 215-222 (1998) https://doi.org/10.1016/S0011-393X(98)85074-1
  3. 화이자 리미티드, 암로디핀 말레에이트를 포함하는 약학 조성물, 대한민국특허청, 특 2003-0070594 (2003)
  4. S.S. Suh, M.S. Mohan and M.W. Davis, Amlodipine pharmacokinetics of the maleate vs besylate salts, Am. J. Hypertens., 17, S123-S124 (2004)
  5. J.Y. Park, K.H. Kim, G.S. Lee, P.W. Park, S. Kim, Y.S. Lee, Y.W. Lee and E.K. Shin, Randomized, Open label Two period crossover comparison of the Pharmacokinetic and pharmacodynamic properties of two amlodipine formulation in healthy adult male Korean subjects, Clin. Ther., 26, 715-723 (2004) https://doi.org/10.1016/S0149-2918(04)90071-9
  6. G. Ragno, E. Cione, A. Garofalo, G. Genchi, G. Ioele, A, Risoli and A. Spagnoletta, Design and monitoring of photostability system for amlodipine dosage forms, Int. J. Pharm., 265, 125-132 (2003) https://doi.org/10.1016/j.ijpharm.2003.07.001
  7. G. Ragno, A. Garofalo and C. Vetuschi, Photodegradation monitoring of amlodipine by derivative spectrophotometry, J. Pharm. Biomed. Anal., 27, 19-24 (2002) https://doi.org/10.1016/S0731-7085(01)00556-8
  8. U.S.P. 27 General Information, Packaging practice-repackaging a single solid oral drug product into a unit dose container, U.S. Pharmacopoeia, 1146, 2573-2577 (2004)
  9. B. Guignon, E. Regalado, A. Duquenoy and E. Dumoulin, Helping to choose operating parameter for a coating fluid bed process, Powder Technol., 130, 193-198 (2003) https://doi.org/10.1016/S0032-5910(02)00265-6
  10. K. Thoma and K. Bechtold, Influence of aqueous coating on the stability of enteric coated pellets and tablets, Eur. J. Pharm. Biopharm., 47, 39-50 (1999) https://doi.org/10.1016/S0939-6411(98)00086-1
  11. C.C. DeMerlis and D.R. Schoneker, Review of the oral toxicity of polyvinyl alcohol (PVA), Food Chem. Toxicol., 41, 319-326 (2003)
  12. ICH Harmonized Tripartite Guidline, Impurity: Guideline for residual solvents, Q3C (1997)
  13. M.P Jordan, Moisture barrier film coating composition, method and coated form, U.S. Patent, Patent No 5885617 (1995)
  14. A.H. Kibbe, Handbook of Pharmaceutical Excipients, 3rd Eds, 424-425 (2000)
  15. C.C. Larsen, J.M. Sonnergaard, P. Bertelsen and P. Holm, A new process control strategy for aqueous film coating of pellets in fluidised bed, Eur. J. Pharm., 20, 273-283 (2003) https://doi.org/10.1016/S0928-0987(03)00206-9