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Controlled Release of Tamsulosin from Nanopore-Forming Granules

미세 다공성 과립을 이용한 탐스로신의 방출제어

  • Seo, Seong-Mi (Department of Polymer Engineering, Pukyong National University) ;
  • Lee, Hyun-Suk (Department of Information and Biomaterials, Hannam University) ;
  • Lee, Jae-Hwi (College of Pharmacy, Chung-Ang University) ;
  • Lee, Ha-Young (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology) ;
  • Lee, Bong (Department of Polymer Engineering, Pukyong National University) ;
  • Lee, Hai-Bang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology) ;
  • Cho, Sun-Hang (Nanobiomaterials Laboratory, Korea Research Institute of Chemical Technology)
  • 서성미 (부경대학교 고분자공학과) ;
  • 이현숙 (한남대학교 생명정보신소재공학과) ;
  • 이재휘 (중앙대학교 약학대학) ;
  • 이하영 (한국화학연구원 생체재료연구팀) ;
  • 이봉 (부경대학교 고분자공학과) ;
  • 이해방 (한국화학연구원 생체재료연구팀) ;
  • 조선행 (한국화학연구원 생체재료연구팀)
  • Published : 2006.02.20

Abstract

Tamsulosin or a salt thereof such as its hydrochloride salt has been known to have an adrenaline ${\alpha}$ receptor blocking action for urethra and prostate areas. It has been widely used as a drug which lowers the prostate pressure and improves urinary disturbance accompanied by prostate-grand enlargement, thus for the treatment of prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is essentially required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin granules and assess their formulation variables. We designed entric coated sustained-release tamsulosin granules for this purpose. Nano-pores in the outer controlled release membrane were needed in order to obtain initial tamsulosin release even in an acidic environment such as gastric region. In our sustained release osmotic granule system, hydroxypropylmethylcellulose in a drug-containing layer was used as a rate controller. The drug-containing granules were coated with hydroxypropylmethylcellulose phthalate (HPMCP) and Eudragit, along with glycerol triacetate as an aqueous nano-pore former. The release of tamsulosin depended heavily on the type of Eudragit such as RS, RL, NE 30D, used in the formulation of controlled release layer. These results obtained clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the Korean Food and Drug Administration.

Keywords

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