Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Peptides containing saccharide radicals – e.g. – bleomycins – etc.
Patent
1993-02-16
1995-10-31
Warden, Jill
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
Peptides containing saccharide radicals, e.g., bleomycins, etc.
536 20, 536124, A61K 3800, C07K 900, C08B 3700, C07G 1700
Patent
active
054630223
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to novel N-acetylcarboxymethylchitosan derivatives or N-acetylated carboxymethylchitosan derivatives and processes for the preparation thereof. More specifically, the present invention is concerned with an in vivo targeting technique for medical or pharmaceutical compounds, and thus concerned with novel N-acetylcarboxymethylchitosan derivatives which are useful as polysaccharide-type of high-molecular carriers utilizable for enhancing the stability of pharmaceutical compounds in blood, the organotropism of pharmaceutical compound and the biodegradability of medicinal product prepared. This invention also pertains to novel N-acetylcarboxymethylchitosan derivatives in the form of complexes as linked to the pharmaceutical compounds.
BACKGROUND ART
Use of water-soluble, high-molecular substances as the carriers for drugs, namely, pharmaceutical compounds has been attempted to date especially in the field of pharmaceutical preparations, and a number of related techniques have been provided. These water-soluble, high-molecular substances as the drug carriers are already known widely. In many instances, a cellulose derivative such as carboxymethylcellulose, hydroxypropylcellulose or hydroxypropylmethylcellulose is used. However, these conventional techniques are concerned with so-called sustained release of drugs and have not been developed to techniques for delivery of a drug to a tissue where the drug is required, when necessary, only in an amount as needed. It is the current situation that no satisfactory technique has been developed yet for using a water-soluble, high-molecular substance as a carrier for delivery of the drug. For example, there are the below-described publications 1) and 2). The publication 1) discloses use of carboxymethylchitin as a fine particulate carrier of the implanted type, whereas the publication 2) discloses use of carboxylated dextran as a carrier for the formation of its complex with a drug.
Although the technique disclosed in the publication 1) perceived the gelling ability and the in vivo biodegradability of carboxymethylchitin and makes use of these properties, carboxymethylchitin is of the type which is implanted to a particular local site in the body so that this technique does not go beyond the boundary of the controlled release of a drug and is not expected to enhance the organotropism of a drug to a target cancer tissue or a target organ. On the other hand, the drug complexes disclosed in the publication 2) suggests the possibility of excellent drug-delivery, but functional groups of said carboxylated dextran which are usable for the molecular modification of drug-complexes to facilitate the delivery of drugs are limited to alcoholic hydroxyl groups.
Reflecting the development of an increasing number of the anticancer agents, brain disease-curing drugs and the like, there is an outstanding need for the urgent establishment of targeting technology for these drugs with using a water-soluble, high-molecular substance. Nevertheless, the prior art techniques have not brought about any fully satisfactory solution.
To complete a targeting technique for drugs, namely, pharmaceutical compounds, by using a water-soluble, high-molecular carrier, it is necessary as prerequisites therefor, firstly that a complex of carrier with a drug remains stable in blood after its administration by intravenous injection until its arrival at a target organ, in other words, the drug can be maintained at a necessary concentration in blood, secondly that the carrier is subjected to gradual degradation in the body and consequently the carrier does not remain for a long time in the human body, and thirdly that the carrier as linked to the drug in the form of the complex exhibits by itself the tendency of an organotropism in vivo. Therefore a carrier must be provided, first of all, as one being capable of meeting these requirements all together.
DISCLOSURE OF THE INVENTION
With a view toward overcoming such problems, the present inventors have proceeded with a
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patent: 4619995 (1986-10-01), Hayes
patent: 4760135 (1988-07-01), Diedrich et al.
Jolivet et al, New Engl. J. Med. vol. 309 p. 1094 (1983).
Macromolecules, "Studies on Chitin. 13. New Polysaccharide/Polypeptide Hybrid Materials Based on Chitin and Poly(y-methyl L-glutamate)", Kurita et al., vol. 21, No. 6, Jun. 1988.
JP-A-61236729 (Sumitomo) Oct. 22, 1986--Abstract.
Aono Katsutoshi
Inoue Kazuhiro
Ito Teruomi
Okuno Satoshi
Drug Delivery System Institute, Ltd.
Huff Sheela J.
Warden Jill
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