Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Implant or insert
Patent
1996-12-17
1998-08-04
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Implant or insert
424422, 424489, 5147723, 514774, 514776, A61K 908
Patent
active
057889783
ABSTRACT:
An injectable ivermectin composition having a programmable release rate and providing multiple concentration peaks of active ivermectin to produce a sequence of ivermectin release pulses into the blood of cattle and horses. The composition comprises a solution of 0.2%-10% w/w of ivermectin in a solvent selected from propyleneglycol and a mixture of glycerile caprylate, caproate and caprate, such as glycerides of caproic, caprilic and capric acids in equal parts. The solution is used as a vehicle for suspending microspheres 100 nm-200 .mu.m in diameter of a degradable polymer containing between 0.5% and 50% of ivermectin. The microspheres may be formed from polylactic acid, polyglycolic acid or a copolymer of polylactic-polyglycolic acid. The programmable multi-pulse release system may also be obtained with a biodegradable matrix selected from hardenable natural polymers, such as gelatin or albumin, apart from the copolymers of lactic and gycolic acids. The polymers may be subjected to a hardening process to increase resistance to biological agents, for example, a solution of glutaraldehyde or alum or by heating the proteins up to coagulation temperature. In one embodiment, gelatin microspheres loaded with ivermectin are treated in an acqueous solution of glutaraldehyde at 25% during 24 hours and then suspended in the solvent. Another embodiment includes a suspension of ivermectin-loaded microspheres of DL-lactic-glycolic 1:1 copolymer. This monomer ratio may be altered to enhance resistance to erosion.
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Gellon Alberto Atilio
Passeron Eduardo Julio
Taroni Elbio Humberto
Faulkner D.
Page Thurman K.
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