A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/50 (2006.01) A61K 31/05 (2006.01) A61K 31/455 (2006.01) A61K 31/496 (2006.01) A61K 31/5383 (2006.01) A61K 31/545 (2006.01) A61K 31/546 (2006.01) A61K 31/65 (2006.01) A61K 31/706 (2006.01) A61P 11/00 (2006.01) A61P 29/00 (2006.01) A61P 31/00 (2006.01) A61L 2/08 (2006.01)
Patent
CA 2315975
The present invention relates to pharmaceutical composi-tions for the sustained release of pharmacologically active com-pounds, and methods of their manufacture and use. The phar-maceutical compositions contain microcrystals of pharmacologically active compounds which are encapsulated within a phos-pholipid layer which contains a unique combination of phos-pholipids. The pharmaceutical compositions may be rendered suitable for injection. The microcrystals are of varying sizes. At least 50 percent of the microcrystals are from 0.5 µm and 3.0 µm in diameter, at least ten percent of the microcrystals are from 3.0 µm to 10 µm in diameter, and the composition contains microcrystals which are greater than 10 µm in diameter. The methods disclosed contain the steps of forming a lipid suspen-sion which contains the pharmacologically active compound and passing the lipid suspension with the pharmacologically active compound through a homogenizer at high pressure to coat the compound with the lipid suspension, thereby producing water insoluble drugs coated with the lipid suspension. The method is applicable to antibiotics, anti-inflammatory agents, anesthetics, anti-protozoa agents or any compound, including water soluble compounds, which can be modified so as to behave more like water insoluble compounds. The compositions and methods are useful for treating respiratory diseases in a variety of mammals. The compounds and methods are also able to sharply reduce the toxicity of drug compounds.
La présente invention concerne, d'une part des compositions pharmaceutiques permettant une libération prolongée de composés pharmacologiquement actifs, et d'autre part des procédés des rapportant à l'élaboration et l'utilisation de ces compositions. Ces compositions, qui contiennent des microcristaux de composés pharmacologiquement actifs encapsulés dans une couche d'une combinaison unique de phospholipides, peuvent être rendues injectables. Ces microcristaux sont de différents calibres, le diamètre d'au moins 50 % d'entre eux étant compris entre 0,5 mu m et 3,0 mu m, pour moins de 10 % dont le diamètre est compris entre 3,0 mu m et 10 mu m, la composition contenant en outre des microcristaux d'un diamètre supérieur à 10 mu m. Le procédé de l'invention consiste à réaliser une suspension lipidique du composé pharmacologiquement actif, et à faire passer cette suspension à haute pression dans un homogénéisateur où le composé vient s'encapsuler dans la suspension lipidique, donnant ainsi un médicament non hydrosoluble encapsulé dans la suspension lipidique. Ce procédé convient aux antibiotiques, anti-inflammatoires, anesthésiques, anti-protozoaires ou tous autres composés, y compris les composés hydrosolubles, que l'on peut ainsi modifier pour que leur comportement se rapproche de celui de composés non hydrosolubles. Ces compositions et procédés, qui conviennent au traitement de maladies respiratoires chez divers mammifères, permettent également de réduire considérablement la toxicité de composés médicamenteux.
Campbell William R.
Hepler Douglas I.
Larson Kenneth A.
Idexx Laboratories Inc.
Smart & Biggar
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