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Liposome preparation containing slightly water-soluble camptothecin

A technology of liposome preparations and poor water solubility, which is applied in the field of liposome preparations, can solve problems such as difficulty in maintaining the concentration of SN-38, achieve excellent blood retention, excellent drug sustained release, and maintain the effect of drug concentration

Inactive Publication Date: 2007-06-13
TERUMO KK +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] It has also been reported that it is difficult to maintain the concentration of SN-38 in canine plasma by using high performance liquid chromatography to quantitatively analyze the concentration of SN-38 in plasma (see Non-Patent Document 7)

Method used

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  • Liposome preparation containing slightly water-soluble camptothecin
  • Liposome preparation containing slightly water-soluble camptothecin
  • Liposome preparation containing slightly water-soluble camptothecin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0130] (1) Preparation of mixed materials

[0131] According to the specified molar ratio shown in Table 1, weigh hydrogenated soybean phosphatidylcholine (Lipoid company) (hereinafter referred to as HSPC), cholesterol (Solvay company) (hereinafter referred to as Chol), stearic acid (NOF Corporation) ( Hereinafter referred to as SA) and 7-ethyl-10-hydroxycamptothecin (SN-38, yakult head office) (hereinafter referred to as SN-38), which are dissolved in 200ml of tert-butanol heated to 60°C (Kanto Chemical ), cooled in an ice bath, and freeze-dried.

[0132] (2) scattered

[0133] 200 ml of physiological saline was added to the dried product obtained above, heated at 68° C., and pre-dispersed using Clearmix single (manufactured by M Technique Co.), the particle size was controlled using a microfluidizer (Microfluidics Co., Ltd.).

[0134] (3) Import of PEG-PE

[0135] Add 11.32mL of 36.74mg / mL physiological saline solution of polyethylene glycol (molecular weight 5000)-phosph...

Embodiment 4

[0162] As another mode of embodiment 3, the operation of embodiment 3 is repeated. The weighed value, the membrane composition of the obtained SN-38 liposome preparation, the drug load (medicine / lipid molar ratio, drug concentration), and the particle size are shown in Table 2.

[0163] [Table 2]

[0164] Table 2

[0165] Weighing value / g

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Abstract

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.

Description

technical field [0001] The present invention relates to a liposome preparation containing a poorly water-soluble camptothecin compound as a drug. Background technique [0002] In recent years, drug delivery systems (DDS) for safely and efficiently transporting and distributing drugs to target lesions have been actively studied, and as one of the methods, methods using liposomes as drug delivery tools (carriers) are being studied. Liposomes are aqueous dispersions of closed vesicles formed by a lipid bilayer membrane of phospholipids, the central compartment of which is an aqueous environment (inner aqueous phase). So far, studies on the liposome formation of various drugs are underway. In the liposomalization of drugs, water-soluble drugs are mainly held in the central chamber in the aqueous environment, while poorly water-soluble drugs are mainly carried and held in the lipid membrane layer in the oily environment. At the same time, studies on liposome membranes are also ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4745A61K9/127A61K47/12A61K47/24A61K47/28A61P35/00
CPCA61K9/1272A61K31/4745A61P35/00A61P43/00A61K47/24A61K47/28
Inventor 吉野敬亮野泽滋典绪方嘉贵黑崎靖夫泽田诚吾加藤几雄松崎健
Owner TERUMO KK
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