Liposome preparations

• US 20040028728A1
• Filed: 08/08/2003
• Published: 02/12/2004
• Est. Priority Date: 03/11/1999
• Status: Active Grant

• Current Assignee: Astellas Pharma Incorporated
• Original Assignee: Fujisawa Pharmaceutical Co., Ltd. (Astellas Pharma Incorporated)
• Inventors: Kasai, Akihiro, Fujisaki, Jiro, Konno, Hajime, Ohtomo, Kazumi
• Granted Patent: US 6,984,397 B2
• Time in Patent Office: Days
• US Class Current: 424/450
• CPC Class Codes: A61K 31/407 condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
• CPC Class Codes: A61K 31/436 the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
• CPC Class Codes: A61K 31/7042 Compounds having saccharide radicals and heterocyclic rings
• CPC Class Codes: A61K 9/127 Liposomes
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 31/12 Antivirals
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 39/00 General protective or antinoxious agents
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

The present invention provides a pipecolic acid derivative-containing liposome preparation having has an excellent rapid action capable of coping with an emergent situation such as cerebral infarction.

A liposome preparation characterized by comprising, as an active ingredient, a pipecolic acid derivative of the ingredient described in the present specification or a pharmaceutically acceptable salt thereof entrapped into liposomes, wherein lecithin is mainly used as the liposome-forming lipid, said liposome preparation containing no cholesterol as a stabilizer.

Claims

1. A pipecolic acid derivative-containing liposome preparation comprising a pipecolic acid derivative or a pharmaceutically acceptable salt thereof entrapped into liposomes.

2. The liposome preparation as defined in claim 1, wherein lecithin is mainly used as a lipid for forming the liposome.

3. The liposome preparation as defined in claim 2, wherein the liposome substantially contains no cholesterol.

4. The liposome preparation as defined in claim 1, wherein the pipecolic acid derivative is a macrolide compound of the following general formula (I) or a pharmaceutically acceptable salt thereof:

5. The liposome preparation as defined in claim 4, wherein the macrolide compound (I) is 17-allyl-1,14-dihydroxy-12-[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylvinyl]-23,25-dimethoxy-13,19,21,27-tetramethyl-11,28-dioxa-4-azatricyclo[22.3.1.0^4,9]octacos-18-ene-2,3,10,16-tetraone or its hydride.

6. A solid preparation in which the liposome preparation as defined in any one of claim 1 is dispersed in a pharmaceutically acceptable saccharide.

10. The liposome preparation as defined in claim 6, which is a freeze-dried product.

11. The liposome preparation as defined in claim 1, which is dispersed into distilled water for injection.

7. A solid preparation comprising a liposome preparation dispersed in a pharmaceutically acceptable saccharide, wherein the liposome preparation is composed of a liposome containing lecithin as a main component and free from cholesterol and a pipecolic acid derivative or a pharmaceutically acceptable salt thereof is entrapped in the liposome.

8. The liposome preparation as defined in claim 7, wherein a mass ratio among a pipecolic acid derivative or a pharmaceutically acceptable salt thereof, lecithin, and a pharmaceutically acceptable saccharide of the solid is 1:

1-500;

10-1000.

9. The solid preparation as defined in claim 7, wherein the saccharide is lactose or maltose.