Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1996-01-25
1998-07-28
Kumar, Shailendra
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514558, 514563, 514616, 424450, 424484, 436 71, 554 35, 554 36, 554 37, 554 61, 554 63, 554 64, 554213, 554219, 554227, 564153, A61K 31225, A61K 3123, C07C 59235, C07C23305
Patent
active
057863873
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/US95/00535, filed Mar. 23, 1995.
BACKGROUND OF THE INVENTION
1. Field of the Invention
The present invention relates to a lipid double-chain derivative containing a polyoxyethylene ("POE"). More specifically, it relates to a lipid double-chain derivative containing a polyoxyethylene which can be utilized as a fine particle drug carrier such as a mixed micell or a lipid emulsion or a liposome.
2. Description of the Related Art
In recent years, research and development have been conducted on a passive or an active target directional type drug delivery system in which an emulsified composition such as a liposome or a lipid emulsion containing a drug can be delivered. The research aims to selectively deliver a drug with a carrier to a target tissue, thereby heightening the concentration of the drug in the pathological tissue and reducing a side effect of the drug in the other tissues. Therefore, the efficacy of the drug can be enhanced. With regard to a fine particle carrier such as a lipid emulsion, the technical development of the following two points (a) and (b) is important.
(a) The development of a means for avoiding a reticuloendothelial system and improving circulation time in blood in order to enhance a drug delivery efficiency to a pathological tissue.
(b) The development of super fine particles which are stable in blood and capable of efficiently leaking a drug from a site, where vascular permeability is accelerated, to a pathological tissue outside blood vessels.
There has been, for example, proposed a liposome using a compound obtained by amide-bonding a carboxylic acid derivative of a polyoxyethylene to the amine moiety of phosphatidyl ethanolamine to improve its half-life period 29 (1991)!. However, it is difficult to obtain stable and super-fine particles having an average particle diameter of 100 nm or less because of its high curvature. Further, the liposome has a drawback that the amount of the drug which can be delivered is limited.
With regard to the lipid emulsion, Japanese Patent Laid-open Publication No. 161430/1991 has disclosed that stable and super-fine particles having an average particle diameter of 50 nm or less can be obtained by the use of a water-soluble POE-containing lipid single-chain emulsion. However, it has been presumed that the effective circulation time in blood cannot always be obtained in blood by the single-chain surface active agent. Furthermore, Japanese Patent Laid-open Publication No. 203/1990 has disclosed that super-fine lipid emulsion particles can be obtained by adjusting the content ratio of a composite lipid such as lecithin which is a surface active component to a high level of 15 to 70%. However, this lipid emulsion does not always have a long circulation time in blood Pharmaceutical Society of Japan, 108th Annual Meeting, P. 590 (1988)!.
In addition, it is, in general, difficult to obtain the super-fine lipid emulsion particles which have a high curvature but which, on the other hand, have a high stability during storage and a high stability in blood only by the use of a lipid double-chain surface active substance (particularly a conical molecule-like surface active component).
As the fine particle carriers, in particular the liposomes, having the good circulation time in blood, there have been researched and developed a (1988)!, and the above POE derivatives of phosphatidyl ethanolamine that in all of these carriers, room for improvement still remains from the viewpoints of an industrial productivity and usefulness such as mass-productivity and cost.
SUMMARY OF THE INVENTION
We have now found that a certain kind of lipid derivative is useful as a fine particle drug carrier.
Accordingly, an object of the present invention is to provide a novel compound useful as a fine particle drug carrier.
Another object of the present invention is to provide a novel compound which efficiently avoids a reticuloendothelial system and which has a long circulation time in blood, when used as the fine particle drug carrier.
Still anot
REFERENCES:
patent: 4803010 (1989-02-01), Ogino et al.
Ando Takashi
Nakabayashi Satoru
Taniguchi Kumi
Udagawa Chikako
Watanabe Hiroshi
Kumar Shailendra
Meiji Seika Kabushiki Kaisha
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