Process for increasing the antagonistic effect of peptidic...

A - Human Necessities – 61 – K

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167/154, 167/166

A61K 9/52 (2006.01) A61K 37/43 (1990.01)

Patent

CA 1335711

The antagonistic effect of the releasing hormone of LH and FSH or of one of its synthetic analogues selected from the group (pyro) Glu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 (pyro) Glu-His-Trp-Ser-Tyr-D-Phe-Leu-Arg-Pro-Gly-NH2 and (pyro) Glu-His-Trp-D-Ser-Tyr-D-Leu-Leu-Arg-Pro-NHR1 (R1 being an alkyl group) on hormone-dependent diseases can be increased by coating such compounds by micro-encapsulation or by matrix formation with a copolymer of a lactide and a glycolide. The initial stimulating effect of the above-mentioned compounds is increased by this coating, with about 23 to 50% of the active principle of the analog being released within about 1-5 days after injection to a human, with the remainder released over a period of between about 3 weeks and two months.

566908

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