Journal of Pharmaceutical Investigation

  • 제36권6호
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  • Pages.393-399
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  • 2006
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  • 2093-5552(pISSN)
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  • 2093-6214(eISSN)
한국약제학회 (The Korean Society of Pharmaceutical Sciences and Technology)
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수분 감응성 아시클로버 패취제의 설계 및 평가

Formulation and Evaluation of Moisture-activated Acyclovir Patches

  • 김아미 (동덕여자대학교 약학대학) ;
  • 곽혜선 (이화여자대학교 약학대학) ;
  • 전인구 (동덕여자대학교 약학대학)
  • Kim, Ah-Mee (College of Pharmacy, Dongduk Women's University) ;
  • Gwak, Hye-Sun (College of Pharmacy, Ewha Womans University) ;
  • Chun, In-Koo (College of Pharmacy, Dongduk Women's University)
  • 발행 : 2006.12.21
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초록

This study was aimed to design, formulate and characterize the moisture-activated patches containing acyclovir for antiviral action. Gel intermediates for film-type patches were prepared with mucoadhesive polymer, viscosity builders, enhancers and acyclovir. Patches containing acyclovir were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane, and of drug flux through the hairless mouse skin. Film-type patches obtained were uniform in the thickness and showed a mucoadhesive property when contacted with moisture. The formulation was optimized, which consisted of $Cantrez^{\circledR}$ AN-169(2%), $Kollidon^{\circledR}$ VA 64(1%), $Natrosol^{\circledR}$(1%), hydroxypropyl-$\beta$-cyclodextrin(1%) and dimethylsulfoxide(0.5%). Release rates of acyclovir patches increased dose-dependently. The addition of terpenes such as d-limonene or cineole increased release rates of acyclovir, but decreased permeation rates. The permeation rates were enhanced by 2 and 2.5 times by the addition of glycyrrhizic acid ammonium salt and sodium glycocholate, respectively, compared with that of no enhancer. These results suggest that it may be feasible to deliver acyclovir through the skin or gingival mucosa from the moisture-activated patches.

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참고문헌

  1. J. Neyts, G. Andrei and E. De Clercq, The novel immuno- suppressive agent mycophenolate mofetil markedly poten- tiates the antiherpesvirus activities of acyclovir, gancyclovir, and penciclovir in vitro and in vivo, Antimicrob. Agents Chemother., 181, 216-222 (1998)
  2. F.G. Hayden, Antimicrobial Agents: In The Pharmacological Basis of Therapeutics, J.G. Hardman, L.E. Limbird and A.G. Gilman (Ed.), McGraw-Hill, New York, USA, pp. 1317-1322 (2001)
  3. M. Ishida, N. Nambu, and T. Nagai, Mucosal dosage form of lidocaine for toothache using hydroxypropyl cellulose and Carbopol, Chem. Pharm. Bull., 30, 980-984 (1982) https://doi.org/10.1248/cpb.30.980
  4. A.D. Woolfson, D.F. McCafferty and V. Boston, Clinical experiences with a novel percutaneous amethocaine prepara- tion: prevention of pain due to venepuncture in children, Br. J. Clin. Pharmacol., 30, 273-279 (1990) https://doi.org/10.1111/j.1365-2125.1990.tb03775.x
  5. A.D. Woolfson, D.F. McCafferty and G.P. Moss, Develop- ment and characterization of a moisture-activated bioad- hesive drug delivery system for percutaneous local anaes- thesia, Int. J. Pharm., 169, 83-94 (1998) https://doi.org/10.1016/S0378-5173(98)00109-4
  6. D.F. McCafferty and A.D. Woolfson, New patch delivery system for percutaneous local anaesthesia, Br. J. Anaesth., 71, 370-374 (1993) https://doi.org/10.1093/bja/71.3.370
  7. D.F. McCafferty, A.D. Woolfson and G.P. Moss, Novel bioadhesive delivery system for percutaneous local anaesthesia, Br. J. Anaesth., 84, 456-458 (2000) https://doi.org/10.1093/oxfordjournals.bja.a013469
  8. E. Sozen, A.M. Avunduk and N. Akyol, Comparison of efficacy of oral valacyclovir and topical acyclovir in the treatment of herpes simplex keratitis: a randomized clinical trial, Chemotherapy, 52, 29-31 (2006) https://doi.org/10.1159/000090239
  9. S.A. Qureshi, M. Jiang, K.K. Midha and J.P. Skelly, In vitro evaluation of percutaneous absorption of an acyclovir product using intact and tape-stripped human skin, J. Pharm. Pharm. Sci., 1, 102-107 (1998)
  10. G.R. Kinghorn, Topical acyclovir in the treatment of recurrent herpes simplex virus infections, Scand. J. Infect. Dis. Suppl., 47, 58-62 (1985)
  11. M. Ishida, Y. Machida, N. Nambu and T. Nagai, New mucosal dosage form of insulin, Chem. Pharm. Bull., 29, 810-816 (1981) https://doi.org/10.1248/cpb.29.810
  12. T. Nagai, Topical mucosal adhesive dosage forms, Med. Res. Rev., 6, 227-242 (1986) https://doi.org/10.1002/med.2610060205
  13. Y.W. Chien and H.J. Lambert, Controlled drug release from polymeric delivery devices. II. Differentiation between partition-controlled and matrix-controlled drug release mechanism, J. Pharm. Sci., 63, 515-519 (1974) https://doi.org/10.1002/jps.2600630405
  14. A.C. Williams and B.W. Barry, Terpenes and the lipid-protein partitioning theory of skin penetration enhancement, Pharm. Res., 8, 17-24 (1991) https://doi.org/10.1023/A:1015813803205