Drug – bio-affecting and body treating compositions – Solid synthetic organic polymer as designated organic active... – Ion exchange resin
Reexamination Certificate
2000-06-23
2001-08-21
Page, Thurman K. (Department: 1615)
Drug, bio-affecting and body treating compositions
Solid synthetic organic polymer as designated organic active...
Ion exchange resin
C424S078120, C424S468000, C424S078350
Reexamination Certificate
active
06277366
ABSTRACT:
TECHNICAL FIELD
This invention relates to a sustainedly releasing agent for medicines and a sustainedly released medicinal composition containing it. More particularly, the invention relates to a sustainedly releasing agent for medicines comprising a specific non-crosslinked type anion-exchange resin, as well as to a sustainedly released medicinal composition useful for the prevention or treatment of hyperlipidemia which contains the sustainedly releasing agent for medicines and a medicine having a hypolipidemic effect.
BACKGROUND ART
Hitherto, several patents have disclosed methods for binding active ingredients to ion-exchange resins. For example, active ingredients are immobilized to cationic or anionic polystyrene-divinyl benzene resins, as described in British Patent No. 857,193. Several other patents also describe methods for coating active ingredient/resin complexes. For example, U.S. Pat. No. 3,138,525 discloses a method for concealing the taste of amprotopine by forming a complex with a cationic resin and coating it with wax. Also, British Patent No. 1,218,102 describes a method for coating with a device such as an air-fluidized bed, a complex in which a cationic active ingredient is immobilized to an anionic resin. Further, Japanese Patent Application Laid-Open Gazette No. Hei 3-52824 describes a sustainedly releasing medicine capable of regulating the release rate of an active ingredient, which medicine comprises an active ingredient/ion-exchange resin complex coated with an ionic polymer having the polarity opposite to that of the resin.
DISCLOSURE OF THE INVENTION
However, where the active ingredients are anionic or liposoluble medicines, sustainedly releasing agents that exert a sufficient sustained release action have not yet been developed. Particularly, it has been hoped that sustainedly releasing agents useful for the sustained release of medicines for the prevention or treatment of hyperlipidemia be developed where in the past the combined use of plural hypolipidemic medicines was difficult while sufficiently avoiding their side effects.
This invention has been made in consideration of the problems inherent in the above-stated prior art; and it aims at providing a sustainedly releasing agent capable of exerting a sufficient sustained release action when the active ingredient is an anionic or liposoluble medicine, which is particularly useful for the sustained release of a medicine for the prevention or treatment of hyperlipidemia, as well as a sustainedly released medicinal composition containing the agent.
As a result of extensive investigations that were repeated with the aim of accomplishing the above-mentioned object, the present inventors have discovered the findings as described below and thus have come to completing the invention. Specifically, it has been discovered that non-crosslinked type anion-exchange resins represented by the following general formula (II):
wherein
R
1
represents benzyl group or an alkyl group of 1-20 carbons; R
2
and R
3
may be the same or different, and each represents a lower alkyl group of 1-4 carbons; R
4
represents a hydrogen atom or a lower alkyl group; X
−
represents a physiologically acceptable counter ion; n represents 1-3; and p represents a mean degree of polymerization of 10-10,000, respectively, as described in Japanese Patent Application Laid-Open Gazette No. Hei 8-208750 and which were developed by the present inventors as blood cholesterol lowering agents that solves the drawbacks of bile acid adsorbents are unexpectedly useful as sustainedly releasing agents for medicines particularly where anionic or liposoluble medicines are chosen as active ingredients, because they have hydrophobic groups while being non-crosslinked type anion-exchange resins; and the discovery has led to the invention.
The sustainedly releasing agent (sustained-releasing agent) for medicines of this invention is that comprising a non-crosslinked type anion-exchange resin (a nonbridged type anion-exchange resin) represented by the following general formula (I):
wherein
R
1
represents a moiety selected from the group consisting of aralkyl groups of 7-10 carbons and alkyl groups of 1-20 carbons; R
2
and R
3
may be the same or different, and each represents a lower alkyl group of 1-4 carbons; R
4
represents a hydrogen atom or a lower alkyl group; X
−
represents a physiologically acceptable counter ion; n represents 1-3; and p represents a mean degree of polymerization, respectively.
Further, the sustainedly released medicinal composition (sustained-releasing medicinal composition) of this invention is that comprising the sustainedly releasing agent that is comprised of the non-crosslinked type anion-exchange resin represented by the general formula (I) as described above and a medicine having a hypolipidemic effect.
Furthermore, this invention resides in the use of the non-crosslinked type anion-exchange resin represented by the above-mentioned general formula (I) as a sustainedly releasing agent for medicines.
REFERENCES:
patent: 3138525 (1964-06-01), Koff
patent: 4460577 (1984-07-01), Moro et al.
patent: 4814354 (1989-03-01), Ghebre-Sellassie et al.
patent: 5032393 (1991-07-01), Douglas et al.
patent: 5665348 (1997-09-01), Okayama et al.
patent: 5840339 (1998-11-01), Kunin
patent: 6022533 (2000-02-01), Goto et al.
patent: 857193 (1960-12-01), None
patent: 1218102 (1971-01-01), None
patent: 55-100313 (1980-07-01), None
patent: 2-111719 (1990-04-01), None
patent: 3-52824 (1991-03-01), None
patent: 8-208750 (1996-08-01), None
Goto Takeshi
Itoyama Toshio
Sorimachi Hiroshi
Yoshitake Kazuhisa
Fubara Blessing
Hisamitsu Pharmaceutical Co. Inc.
Page Thurman K.
Pillsbury & Winthrop LLP
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