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Liposome preparations

A liposome preparation and liposome technology, applied in the field of macrolide compounds, can solve the problem that liposome preparations cannot show fast enough action and the like

Inactive Publication Date: 2002-03-27
FUJISAWA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because liposome membranes are too stable, liposome preparations cannot show fast enough action like anticoagulants, fibrinolytics, and cerebral vasodilators used in the treatment of cerebral infarction

Method used

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  • Liposome preparations
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Examples

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preparation Embodiment 3

[0101] (3) Preparation Example 3 (high pressure emulsion method): A solution obtained by dissolving purified egg yolk lecithin (20 g) and tacrolimus (1 g) in ethanol (10 mL) was vacuum-dried to form a thin film. This film was roughly dispersed in a 10% maltose aqueous solution (2000 mL) with a magnetic stirrer. The dispersion was treated with a high-pressure emulsifier manufactured by Nanomizer Co. The formed liposome emulsion was filled into a vial of 10 mL, and then freeze-dried. The freeze-dried liposome preparation formed was redispersed in 9 mL of water for injection to obtain liposomes containing 0.5 mg / mL tacrolimus and an average particle diameter of 80 nm (measured by dynamic light scattering method, C370 type manufactured by NICOMP Co.) Dispersions.

preparation Embodiment 4

[0103] In the same manner as Preparation Example 1, the following formula was used to obtain freeze-dried liposomes, and a proper amount of water for injection was used to make a liposome dispersion.

[0104] Tacrolimus 3mg

[0105] Purified egg yolk lecithin 100mg

[0106] Lactose monohydrate 1000mg

[0107] Composition 1103mg

preparation Embodiment 5

[0109] In the same manner as in Preparation Example 3, the following formula was used to obtain a freeze-dried liposome preparation, and an appropriate amount of water for injection was used to make liposome preparations 1) and 2)

[0110] 1) Tacrolimus 3mg

[0111] Purified egg yolk lecithin 100mg

[0112] Alpha-fertility 0.3mg

[0113] Maltose 1000mg

[0114] Composition 1103.3mg2) Tacrolimus 5mg

[0115] Purified egg yolk lecithin 100mg

[0116] Alpha-Tocopherol 0.3mg

[0117] Maltose 1000mg

[0118] Composition 1105.3mg

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Abstract

Pipecolic acid derivative-containing liposome preparations which are excellent in the immediate action and thus usable in an urgent situation such as brain infarction. These preparations are characterized by containing pipecolic acid derivatives or pharmaceutically acceptable salts thereof, which comprise the components as described in the description, as the active ingredient and lecithin as the major component of lipids forming liposomes, without resort to cholesterol as a stabilizer.

Description

field of invention [0001] The present invention relates to a liposomal preparation for pharmaceutical use containing a 2-pipericolic acid derivative, especially a macrolide compound, which has recently received special attention for its excellent immunosuppressive activity, such as A tricyclic compound of tacrolimus (FK 506) or a pharmaceutically acceptable salt thereof, as an active ingredient. More specifically, the present invention relates to a liposome preparation, which contains the above-mentioned active components stably encapsulated in liposomes, so it can be dissolved in various media such as physiological saline, glucose solution for injection, water or body fluids. It can be used in various administration methods, including injection methods such as intravenous injection, intramuscular injection and local injection for intra-articular injection, etc., local administration methods such as application to the skin, eye drops Internal, nasal and inhalational administr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/407A61K31/436A61K31/7042A61P9/10A61P27/02A61P29/00A61P31/12A61P37/00
CPCA61K9/127A61K31/436A61K31/7042A61K31/407A61P27/02A61P29/00A61P31/12A61P37/00A61P39/00A61P9/00A61P9/10
Inventor 藤崎二郎绀野肇笠井昭宏大友和三
Owner FUJISAWA PHARMA CO LTD
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