[Once-a-month injectable microcapsules of leuprorelin acetate].
Leuprorelin (leuprolide, D-Leu6-(des-Gly10-NH2)-LH-RH ethylamide) acetate is a super-active agonist of luteinizing hormone-releasing hormone (LH-RH). We developed once-a-month injectable microcapsules of this agonist by our novel in-water drying method. This depot formulation can release the drug at an apparent zero-order rate over one month with bioerosion of copoly (lactic/glycolic acid) utilized as a wall material of the polycore microcapsules. A dramatic prolonged depression of pituitary-gonadal axis, chemical castration, was achieved by the once-a-month injection in experimental animals; it expects a reliable efficacy for treating hormone-dependent prostatic, breast cancers and endometriosis. Studies on the dosage design of this new delivery system of leuprorelin are summarized.
Toguchi
H
H
Pharmaceutics Research Laboratories, Takeda Chemical Industries, Ltd., Osaka, Japan.
Ogawa
Y
Y
Okada
H
H
Yamamoto
M
M
D000595:Amino Acid Sequence; D000818:Animals; D001943:Breast Neoplasms / Q000188:drug therapy; D002214:Capsules; D003692:Delayed-Action Preparations; D016503:Drug Delivery Systems; D004715:Endometriosis / Q000188:drug therapy; D006016:Glycolates; D006801:Humans; D007267:Injections; D007773:Lactates; D019344:Lactic Acid; D016729:Leuprolide / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D008297:Male; D008969:Molecular Sequence Data; D011108:Polymers; D011471:Prostatic Neoplasms / Q000188:drug therapy
D002214:Capsules; D003692:Delayed-Action Preparations; D006016:Glycolates; D007773:Lactates; D011108:Polymers; C031149:glycolic acid; D019344:Lactic Acid; D016729:Leuprolide