A New Technique to Efficiently Entrap Leuprolide Acetate into Microcapsules of Polylactic Acid or Copoly(Lactic/Glycolic) Acid

• 小川 泰亮

  Pharmaceutical Development Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.,

• 山本 真樹

  Pharmaceutical Development Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.,

• 岡田 弘晃

  Pharmaceutical Development Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.,

• 矢敷 孝司

  Pharmaceutical Development Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.,

• 島本 次雄

  Pharmaceutical Development Laboratories, Central Research Division, Takeda Chemical Industries, Ltd.,

抄録

The aim of this work was to develop injectable microcapsules containing leuprolide acetate, that would deliver that drug at a zero-order rate over a period of about one month. A large amount of leuprolide acetate, a hydrophilic drug, was entrapped into polylactic aicd (PLA) and copoly-(lactic/glycolic) acid (PLGA) microcapsules prepared by an in-water dring method using a (w/o)/w emulsion. The basic techniques were designed to increase the viwcosities of the inner water phase and w/o emulsion. Under the conditions used, it was possible for the drug to be completely entrapped by the microcapsules in the range of 10 to 20% on the basis of the polymer. However, the release profiles of the drug in vitro were inadequate for controlled release for one month.

収録刊行物

• Chem. Pharm. Bull.

  Chem. Pharm. Bull. 36 1095-1103, 1988

  公益社団法人日本薬学会

キーワード

• injectable controlled-release formulation
• leuprolide acetate
• microencapsulation
• polylactic acid
• copoly(lactic
• glycolic)acid
• in-water drying process
• entrapment

詳細情報

• CRID: 1571698602412144000
• NII論文ID: 110003654771
• NII書誌ID: AA00602100
• ISSN: 00092363
• 本文言語コード: en
• データソース種別:
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