A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 31/4745 (2006.01) A61K 9/127 (2006.01) A61K 47/12 (2006.01) A61K 47/24 (2006.01) A61K 47/28 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2570329
The invention aims at providing a slightly water-soluble camptothecin liposome preparation which permits long-term stable retention of a slightly water- soluble camptothecin therein to thereby inhibit the .alpha.-hydroxylactone ring from hydrolysis in blood and keep the camptothecin in the cyclic state contributing to the antitumor activity and which is improved in the releasability of the camptothecin from liposome and is therefore so excellent in the residence of the camptothecin in blood that the concentration of the camptothecin in plasma can be kept for a long time after administration. This aim is attained by a liposome preparation which contains a fatty acid and a phospholipid as the lipid components constituting the membrane and a slightly water-soluble camptothecin as the drug.
L'invention a pour objet une préparation de liposome contenant du camptothecin soluble dans l~eau qui permet une rétention stable á long terme d'un camptothecin soluble dans l'eau pour inhiber l'anneau .alpha.-hydroxylactone á partir de l'hydrolyse dans le sans et conserve le camptothecin dans l'état cyclique contribuant à l'activité antitumorale et qui améliore le dégagement du camptothecin du liposome et est par conséquent excellent dans le séjour du camptothecin dans le sang de sorte que la concentration du camptothecin dans le plasma peut être maintenue longtemps après l'administration. Cet objectif est atteint par une préparation de liposome qui contient un acide gras et un phospholipide comme composant lipide constituant la membrane et un camptothecin légèrement soluble dans l'eau comme médicament.
Kato Ikuo
Kurosaki Yasuo
Matsuzaki Takeshi
Nozawa Shigenori
Ogata Yoshitaka
Kabushiki Kaisha Yakult Honsha
Macrae & Co.
Terumo Kabushiki Kaisha
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