Transdermal Permeation of Xanthan Gum Bases on the Water-soluble and Lipophilic Antihyperlipoproteinemic Drugs

수용성과 지용성 항고지단백혈증제에 대한 Xanthan Gum 기재에서의 경피투과

  • 이석우 (산업자원부 기술표준원 생물환경과) ;
  • 임윤택 (산업자원부 기술표준원 생물환경과) ;
  • 공승대 (명지대학교 화학공학과) ;
  • 황성규 (명지대학교 화학공학과) ;
  • 이우윤 (인천대학교 자연과학대학 화학생물학부)
  • Published : 2001.06.01

Abstract

Recently, there were many studies not only to enhance drug delivery effect but to reduce side effect. Drug delivery system(DDS) is able to improve efficiency with decreasing side effect of drug dosage. Among these application fields, DDS is often used as the method of drug dosage into the epidermic skin. We investigated characters of transdermal therapeutic system(TTS) and the skin permeability of that with applying DDS. We investigated the permeation of xanthan gum containing drug in rat skin using borizontal membrane cell model. Permeation properties of materials were investigated for water-soluble drug with oxiniacic acid and also for lipophilic drug with clofibrate. The permeation rate of lipophilic drug was found to be faster than that of water-soluble drug in vitro. The rate differences of both water-soluble drug and lipophilic drug according to drug content were negligible. We used glycerin, PEG 600 and oleic acid as enhancers. These results showed that skin permeation rate of each drug across the composite was mainly dependent on the property of base and chemical property of drug etc.. 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. This result suggests a possible use of natural polymer base as a transdermal delivery system of antihyperlipoproteinemic agent.

항고지단백혈증제제를 이용한 경펴투과제제흘 제조하고자 기 재로서 xathan gum을 사용하여 약물의 함량 및 투과 촉전제에 따라서 경피투과체제를 제조하고 경피투과 항고지단백혈증제의 가능성 등을 연구하였다. 기재로 사용한 xanthan gum의 체 타전위를륜 측정하여 응결, 침전이 나타나는 등천점으로부터 제타전위 값의 차이가 나타나 있으므로 피부와 접촉시 연고제제외 석출 가능성이 없다는 것을 확인할 수 있었다. 각각의 지용성과 수용성 항고지단백혈증제제를 함유한 정피투과제제를 사용하여 진행된 투과 실험에서는 자용성인 clofibrat$\xi$의 투파속도가 현저하게 빠르게 나타났는데 이는 지용성인 피부 각질과의 친화 즉 lipophilicity를 증가시킴으로써 지용성인 clofibrate의 경피투과를 촉진시키는 것이라 생각된다. 지용성 경피투과제제에 투과촉진제를 첨가했을 경우, 그렇지 않은 경우에 비해 lag time파 투과속도가 빠르게 나타냈다. 특히 PEG 600을 사용했윤 경우가 가장 빠른 투과속도흘 나타냈고 글리세린, 올레산의 순오로 투과속도의 증가를 나타냈다. PEG 600븐 다른 투과촉진제보다 지용성 약물인 clofibrate에 대해 피부내의 지방과 단백겔의 유동성(fluidity) 과 피부 각질의 lipophilicity를 증가시컴으로서 각질로의 약물분배를 촉진한다고 생각된다.

Keywords

References

  1. Medical Applications of Controlled Release v.2 Langer R. S.;Wise D. L.
  2. Drug Delivery Systems Johnson P.;Lioyd-Jones J.
  3. Pharmaceu. Res. v.15 no.6 Pharmacokinetics of the Transdermal Reservoir Membrane System Delivering β-Estradiol In vitro/In vivo-correlation Rohr U. D.;Altenburger R.;Kissel T.
  4. Pharmaceu. Res. v.15 no.9 Prodrug of Gestodene for Matrix-type Transdermal Drug Delivery System Lipp R.;Laurent H.;Gunther C.;Riedl R.;Esperling P.;Tauber U.
  5. Pharm. Res. v.15 no.8 Rat Control in Transdermal β-Estradiol the role of Membrane and Adhesive of layer Rohr U. D.;Altenburger R.
  6. Life Sci. v.39 Skin Permeability of Various Non-Steroidal AntiInflammatory Drug in Man Yano T.;Nakagawa A.;Noda K.
  7. Fertility and Sterility v.69 no.1 Effects of Short-term Transdermal Estradiol Administration on Plasma Levels of Nitric Oxide in Postmenopausal Woman Cicinelli E.;Ignarro L. T.;Maria L.;Baizano G.
  8. Life Sci. v.26 A Selective Drug Delivery System for the Topical Route of Administration, Lotion Dosage Form Mezei M.;Gulasekharam V.
  9. Colloid and Surface Engineering Application in the Process Industries v.14 Williams, R. A.
  10. Zeta Potential in Colloid Science Hunter, R. J.
  11. Dermatological Formulations Barry R. W.
  12. J. Pharm. Sci. v.77 Analysis of Drug Penetration through Skin Considering Doner Concentration Decrease Okamoto, H.;Hashida, M.;Sezaki, H.
  13. Current Concept in Cutaneous Toxicity The Skin as a Site of Drug and Chemical Metabolism Bickers, D. R.;Drilln V. A(eds.)
  14. Novel Drug Delivery Systems(2nd Ed.) Transdermal Drug Delivery and Delivery System Chien W. Y.
  15. Biol. Pharm. Bull. v.16 Effect of Hydrophilic and Lipophilic Vehicles on Skin Permeation of Tegafur with and without Permeation Enhancers Uchida T.;Kitagawa K.;Yagi A.