DOI QR코드

DOI QR Code

Percutaneous Absorption Characteristics of Antidepressant Paroxetine

항우울제인 Paroxetine의 피부 투과 특성 연구

  • Jung, Duck-Chae (Department of Chemistry, University of Incheon) ;
  • Hwang, Sung-Kwy (Department of Fine Chemistry, Seoul National University of Science and Technology) ;
  • Oh, Se-Young (Department of Chemistry, University of Incheon)
  • 정덕채 (인천대학교 자연과학대학 화학과) ;
  • 황성규 (서울과학기술대학교 정밀화학과) ;
  • 오세영 (인천대학교 자연과학대학 화학과)
  • Received : 2011.04.13
  • Accepted : 2011.06.29
  • Published : 2011.06.30

Abstract

Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

Keywords

References

  1. Ravi Kumar M. N. V, Handbook of Particulate Drug Delivery Volume II, American Scientific Publishers 332(2008).
  2. Nachum Z and Shupak A, "Transdermal scopolamine for prevention of motion sickness : clinical pharmacokinetics and therapeutic applications", Clinical Pharmacokinetics, 45(6), 543(2006). https://doi.org/10.2165/00003088-200645060-00001
  3. Berner B and John V.A, "Pharmacokinetic characterisation of transdermal delivery systems", Clinical pharmacokinetics, 26(2), 121(2004).
  4. P. Jinks and K. Hunt, "Improving Suspension MDI Dose Consistency in Patient Use by Incorporation of a Novel Semi-Permeable System Component," in Proceedings of Drug Delivery to the Lungs XVII., 172(2006).
  5. 3M published patent applications, WO200662651 and WO2006/071512. C. Jewell, J. Heylings, H. M. Clowes, and F. M. Williams, Percutaneous absorption and metabolism of dinitrochlorobenzene in vitro. Arch Toxicol, 74, 356 (2000). https://doi.org/10.1007/s002040000123
  6. M. Wang, Y. Yang, and P. W. Heng, Skin permeation of physostigmine from acid-based formulations: evaluating the choice of solvent. Int. J. Pharm., 290, 25 (2005). https://doi.org/10.1016/j.ijpharm.2004.10.027
  7. Wilby M., "Increasing Dose Consistency of pMDIs," Drug Delivery Technol., 5(9), 59(2005).
  8. B. M. Magnusson, S. E. Cross, G. Winckle, and M. S. Roberts, Percutaneous absorption of steroids: determination of in vitro permeability and tissue reservoir characteristics in human skin layers. Skin Pharmacol. Physiol, 19, 336 (2006). https://doi.org/10.1159/000095254
  9. Papakostas G.I., "Tolerability of modern antidepressants". J Clin Psychiatry Suppl. 69(2) 8(2008). https://doi.org/10.4088/JCP.0308e08
  10. Haddad P., "Antidepressant discontinuation syndromes". Drug Saf., 24(3), 183(2001). https://doi.org/10.2165/00002018-200124030-00003
  11. R. Ramasubbu, "Antidepressant treatment-associated behavioural expression of hypomania: a case series". Prog. Neuropsychopharmacol. Biol. Psychiatry, 28(7), 1201(2004). https://doi.org/10.1016/j.pnpbp.2004.06.015
  12. C. Amnuaikit, I. Ikeuchi, K. Ogawara, Higaki, K., and T. Kimura, Skin permeation of propranolol from polymeric film containing terpene enhancers for transdermal use, Int. J. Pharm., 289, 167 (2005). https://doi.org/10.1016/j.ijpharm.2004.11.007
  13. S. W. Stein and J. S. Stefely, "Reinventing Metered Dose Inhalers: From Poorly Efficient CFC MDIs to Highly Efficient HFA MDIs," Drug Delivery Technol., 3(1), 46(2003).
  14. S. Mutalik, and N. Udupa, Transdermal delivery of glibenclamide and glipizide : in vitro permeation studies through mouse skin, Pharmazie., 12, 838(2002).
  15. T. E. K Murthy, and V. S. Kishore., Effect of casting solvent on permeability of antihypertensive drugs through RS 100 films, Asian J Pharm. 1, 108(2002).
  16. Sher et al., "Adhesives Having a Microreplicated Topography and Methods of Making and Using Same," US Patent 6,197,397, (2001).
  17. J. Sandt, J. A. Van Burgsteden, S. Cage, P. L., Carmichael, Dick I, Kenyon S, Korinth G, and Larese F., In vitro predictions of skin absorption of caffeine, testosterone, and benzoic acid: a multi-centre comparison study. Regul. Toxicol. Pharmacol, 39(3), 271 (2004). https://doi.org/10.1016/j.yrtph.2004.02.004
  18. A. Fini, V. Bergamante, G. C. Ceschel, C. Ronchi, and De Moraes CA, Control of transdermal permeation of hydrocortisone acetate from hydrophilic and lipophilic formulations. AAPS. Pharm. Sci. Tech., 9(3), 762 (2008). https://doi.org/10.1208/s12249-008-9107-z
  19. M. Shevachman, N. Garti, and A. Shani, Enhanced percutaneous permeability of diclofenac using a new U-type dilutable microemulsion, Drug Dev. Ind. Pharm., 34, 403 (2008). https://doi.org/10.1080/03639040701662479
  20. J. Novotny, P. Kovarikova, M. Novotny, B. Janusova, A. Hrabalek, and K. Vavrova, Dimethylamino acid esters as biodegradable and reversible transdermal permeation enhancers: effects of linking chain length, chirality and polyfluorination, Pharm. Res., 26, 811 (2009). https://doi.org/10.1007/s11095-008-9780-3