Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1996-10-15
1998-02-17
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424489, 424472, 424473, 424453, A61K 950
Patent
active
057189234
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/00753 filed Apr. 18, 1995
TECHNICAL FIELD
This invention relates to a sucralfate preparation and a process for its production. More particularly, the invention relates to a preparation produced by melt (adhesion) granulation of a finely divided sucralfate using a water-soluble, low-melting point wax, as well as a process for producing said preparation.
BACKGROUND ART
Sucralfate is a basic aluminum salt of sucrose sulfate, which is extensively used as a therapeutic of digestive ulcer having a substrate protein protective action (tunica mucosa ventriculi protecting action), a capability for suppressing the activity of pepsin in gastric juice and an anti-acid action. Since sucralfate is insoluble in water, the disintegration and dispersion of sucralfate preparations are important for the sucralfate to bind effectively to ulcer sites.
Conventional sucralfate preparations have been produced by mixing a yet to be dried sucralfate wet powder with additives and water and drying (spray drying) the mixture at elevated temperatures or granulating and drying the mixture. The preparations may be further mixed with additives to formulate subtilized granules or compacted into tablets.
The conventional sucralfate preparations contain so large sucralfate particles that when subtilized granules made from those preparations are administered internally, they present an off-flavor due to aluminum, graininess due to the large particle size, stickiness to the mucous membrane of the oral cavity connecting to the throat, and other minor troubles associated with administration. Making tablets of sucralfate preparations is not necessarily a preferred method since they are disintegrated into unduly large fragments upon administration.
Considering the protein binding capability which is the primary action of sucralfate, the sucralfate preparation should be divided as finely as possible in order to provide not only an increased surface area but also an enhanced dispersibility and this is effective in assuring the desired efficacy of the preparation if it is to be applied to the living body. On the other hand, sucralfate is highly cohesive and wets only poorly. This nature of sucralfate tends to become pronounced when it is finely divided and in the conventional process in which the undried sucralfate powder is mixed with additives and water, granulated and dried at elevated temperatures, the sucralfate particles agglomerate to grow in size during the evaporation of water; hence, it has been difficult to produce a sucralfate preparation that can be suspended or dispersed as fine particles on use.
DISCLOSURE OF INVENTION
The present invention has been accomplished under these circumstances and has as an object providing a sucralfate preparation that is easy to administer and which allows sucralfate to be applied in vivo in a finely divided form.
Another object of the invention is to provide a process for producing said sucralfate preparation.
In order to produce the desired sucralfate preparation, a dried sucralfate powder prepared by a prior art method is comminuted to a finer form, which is mixed with a water-soluble, low-melting point wax, with the mixture being then heated to effect melt (adhesion) granulation.
The dried sucralfate powder which is used as the starting material may typically be prepared by the method described in Japanese Patent Publication No. 11673/1969 or 16037/1969, according to which basic aluminum chloride is allowed to act on a polysulfated saccharide to form a yet to be dried sucralfate powder, which is subsequently dried, say, spray dried, at elevated temperatures. An example of the sucralfate that can be used in the invention is designated in the Pharmacopoeia of Japan.
The thus dried sucralfate powder is comminuted into a finer form. The comminuted sucralfate powder suffices to be such that at least 90% of the particles have a size not greater than 50 .mu.m; preferably, the particles have an average size of no more than 20 .mu.m and at least 90% of them have a
REFERENCES:
patent: 4940465 (1990-07-01), Theeuwes et al.
patent: 5196405 (1993-03-01), Packman
patent: 5417682 (1995-05-01), Wong et al.
Flanders et al, "The Control of Drug Release from Conventional Melt Granulation Matrices," Drug Development and Industrial Pharmacy, vol. 13(6), pp. 1001-1022, 1987.
Kenji Ukita et al, "Preparation of Essential Oils Loaded Granule by Melt Granulation," Drug Development and Industrial Pharmacy, vol. 20(6), pp. 981-992 1994.
Masaharu Miyajima et al, "Design of Substained-Release Granules prepared by Wax Melting Method," Pharm Tech Japan vol. 8 No. 9 pp. 81-87, 1992.
Yasuo Haramishi et al, "Study on Fluidized Melt-Granulation. I. Examination of the Factors on the Factors on the Granulation.sup.1)," Yakugaku Zasshi, vol. 111 (9) pp. 515-523, 1991.
Matsuda Katsuya
Ozawa Koichi
Benston, Jr. William E.
Chugai Seiyaku Kabushiki Kaisha
Page Thurman K.
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