title: [Design and development of controlled release of drugs from injectable microcapsules].
abstract: Monolithic microcapsules were designed and developed for controlled release of leuprorelin for one month following a single injection. Copoly (DL-lactic/glycolic) acid (PLGA) of copolymer ratio of 75/25 and average molecular weight of 14,000 was suitable for achieving steady serum leuprorelin levels in rats and dogs for 4 weeks. The clinical efficacy of these injectable microcapsules of leuprorelin has been widely proved for prostate cancer, endometriosis, and other sex hormone dependent diseases in about sixty countries. The interaction between the basic functional group of the drug and the carboxylic end group of PLGA was found to be the most important factor in preparing the microcapsules with a small initial burst, as shown with thyrotropin releasing hormone (TRH) and a water-soluble GPIIb/IIIa antagonist (TAK-029).
authors.affiliation: DDS Research Laboratories, Takeda Chemical Industries, Ltd.
authors.forename: S
authors.initials: S
authors.lastname: Takada
authors.forename: Y
authors.initials: Y
authors.lastname: Ogawa
mesh_terms: D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000008:administration & dosage* / Q000493:pharmacokinetics; D001672:Biocompatible Materials; D002214:Capsules; D003692:Delayed-Action Preparations; D004285:Dogs; D016503:Drug Delivery Systems; D015195:Drug Design; D006801:Humans; D007267:Injections; D019344:Lactic Acid; D016729:Leuprolide / Q000008:administration & dosage* / Q000493:pharmacokinetics; D011100:Polyglycolic Acid; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers; D051381:Rats; D013973:Thyrotropin-Releasing Hormone / Q000008:administration & dosage / Q000493:pharmacokinetics
chemical_list: D018931:Antineoplastic Agents, Hormonal; D001672:Biocompatible Materials; D002214:Capsules; D003692:Delayed-Action Preparations; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D013973:Thyrotropin-Releasing Hormone; D016729:Leuprolide